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23 pages, 1826 KiB

Open AccessArticle

Comparative Methods to Evaluate the Antioxidant Capacity of Propolis: An Attempt to Explain the Differences

by Vanessa B. Paula, Letícia M. Estevinho, Susana M. Cardoso and Luís G. Dias

Molecules 2023, 28(12), 4847; https://doi.org/10.3390/molecules28124847 - 19 Jun 2023

Cited by 4 | Viewed by 1835

Abstract

Propolis is a natural product produced by bees that contains a complex mixture of compounds, including phenolic compounds and flavonoids. These compounds contribute to its biological activities, such as antioxidant capacity. This study analysed the pollen profile, total phenolic content (TPC), antioxidant properties, [...] Read more.

Propolis is a natural product produced by bees that contains a complex mixture of compounds, including phenolic compounds and flavonoids. These compounds contribute to its biological activities, such as antioxidant capacity. This study analysed the pollen profile, total phenolic content (TPC), antioxidant properties, and phenolic compound profile of four propolis samples from Portugal. The total phenolic compounds in the samples were determined by six different techniques: four different Folin–Ciocalteu (F-C) methods, spectrophotometry (SPECT), and voltammetry (SWV). Of the six methods, SPECT allowed the highest quantification, while SWV achieved the lowest. The mean TPC values for these methods were 422 ± 98 and 47 ± 11 mg GAE/g sample, respectively. Antioxidant capacity was determined by four different methods: DPPH, FRAP, original ferrocyanide (OFec), and modified ferrocyanide (MFec). The MFec method gave the highest antioxidant capacity for all samples, followed by the DPPH method. The study also investigated the correlation between TPC and antioxidant capacity with the presence of hydroxybenzoic acid (HBA), hydroxycinnamic acid (HCA), and flavonoids (FLAV) in propolis samples. The results showed that the concentrations of specific compounds in propolis samples can significantly impact their antioxidant capacity and TPC quantification. Analysis of the profile of phenolic compounds by the UHPLC-DAD-ESI-MS technique identified chrysin, caffeic acid isoprenyl ester, pinocembrin, galangin, pinobanksin-3-O-acetate, and caffeic acid phenyl ester as the major compounds in the four propolis samples. In conclusion, this study shows the importance of the choice of method for determining TPC and antioxidant activity in samples and the contribution of HBA and HCA content to their quantification. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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22 pages, 1128 KiB

Open AccessArticle

Characterization and Biological Activities of In Vitro Digested Olive Pomace Polyphenols Evaluated on Ex Vivo Human Immune Blood Cells

by Claudio Alimenti, Mariacaterina Lianza, Fabiana Antognoni, Laura Giusti, Onelia Bistoni, Luigi Liotta, Cristina Angeloni, Giulio Lupidi and Daniela Beghelli

Molecules 2023, 28(5), 2122; https://doi.org/10.3390/molecules28052122 - 24 Feb 2023

Cited by 3 | Viewed by 2208

Abstract

Olive pomace (OP) represents one of the main by-products of olive oil production, which still contains high quantities of health-promoting bioactive compounds. In the present study, three batches of sun-dried OP were characterized for their profile in phenolic compounds (by HPLC-DAD) and in [...] Read more.

Olive pomace (OP) represents one of the main by-products of olive oil production, which still contains high quantities of health-promoting bioactive compounds. In the present study, three batches of sun-dried OP were characterized for their profile in phenolic compounds (by HPLC-DAD) and in vitro antioxidant properties (ABTS, FRAP and DPPH assays) before (methanolic extracts) and after (aqueous extracts) their simulated in vitro digestion and dialysis. Phenolic profiles, and, accordingly, the antioxidant activities, showed significant differences among the three OP batches, and most compounds showed good bioaccessibility after simulated digestion. Based on these preliminary screenings, the best OP aqueous extract (OP-W) was further characterized for its peptide composition and subdivided into seven fractions (OP-F). The most promising OP-F (characterized for its metabolome) and OP-W samples were then assessed for their potential anti-inflammatory properties in ex vivo human peripheral mononuclear cells (PBMCs) triggered or not with lipopolysaccharide (LPS). The levels of 16 pro-and anti-inflammatory cytokines were measured in PBMC culture media by multiplex ELISA assay, whereas the gene expressions of interleukin-6 (IL-6), IL-10 and TNF-α were measured by real time RT-qPCR. Interestingly, OP-W and PO-F samples had a similar effect in reducing the expressions of IL-6 and TNF-α, but only OP-W was able to reduce the release of these inflammatory mediators, suggesting that the anti-inflammatory activity of OP-W is different from that of OP-F. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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18 pages, 4838 KiB

Open AccessArticle

Ultrasound-Assisted Extraction of Total Phenolic Compounds and Antioxidant Activity Evaluation from Oregano (Origanum vulgare ssp. hirtum) Using Response Surface Methodology and Identification of Specific Phenolic Compounds with HPLC-PDA and Q-TOF-MS/MS

by Afroditi Michalaki, Haralabos C. Karantonis, Anastasia S. Kritikou, Nikolaos S. Thomaidis and Marilena E. Dasenaki

Molecules 2023, 28(5), 2033; https://doi.org/10.3390/molecules28052033 - 21 Feb 2023

Cited by 11 | Viewed by 2909

Abstract

Oregano is native to the Mediterranean region and it has been reported to contain several phenolic compounds particularly flavonoids that have been related with multiple bioactivities towards certain diseases. Oregano is cultivated in the island of Lemnos where the climate promotes its growth [...] Read more.

Oregano is native to the Mediterranean region and it has been reported to contain several phenolic compounds particularly flavonoids that have been related with multiple bioactivities towards certain diseases. Oregano is cultivated in the island of Lemnos where the climate promotes its growth and thus it could be further used in promoting local economy. The aim of the present study was to establish a methodology for the extraction of total phenolic content along with the antioxidant capacity of oregano by using response surface methodology. A Box–Behnken design was applied to optimize the extraction conditions with regard to the extraction time, temperature, and solvent mixture with the use of ultrasound-assisted extraction. For the optimized extracts, identification of the most abundant flavonoids (luteolin, kaempferol, and apigenin) was performed with an analytical HPLC-PDA and UPLC-Q-TOF MS methodology. The predicted optimal conditions of the statistical model were identified, and the predicted values confirmed. The linear factors evaluated, temperature, time, and ethanol concentration, all showed significant effect (p < 0.05), and the regression coefficient (R²) presented a good correlation between predicted and experimental data. Actual values under optimum conditions were 362.1 ± 1.8 and 108.6 ± 0.9 mg/g dry oregano with regard to total phenolic content and antioxidant activity based on 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay, respectively. Additionally, further antioxidant activities by 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) (115.2 ± 1.2 mg/g dry oregano), Ferric Reducing Antioxidant Power (FRAP) (13.7 ± 0.8 mg/g dry oregano), and Cupric Reducing Antioxidant Capacity (CUPRAC) (1.2 ± 0.2 mg/g dry oregano) assays were performed for the optimized extract. The extract acquired under the optimum conditions contain an adequate quantity of phenolic compounds that could be used in the production of functional foods by food enrichment procedure. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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15 pages, 2211 KiB

Open AccessArticle

Brain Targeting by Intranasal Drug Delivery: Effect of Different Formulations of the Biflavone “Cupressuflavone” from Juniperus sabina L. on the Motor Activity of Rats

by El-Sayed Khafagy, Gamal A. Soliman, Ahmad Abdul-Wahhab Shahba, Mohammed F. Aldawsari, Khalid M. Alharthy, Maged S. Abdel-Kader and Hala H. Zaatout

Molecules 2023, 28(3), 1354; https://doi.org/10.3390/molecules28031354 - 31 Jan 2023

Cited by 2 | Viewed by 2466

Abstract

The polar fractions of the Juniperus species are rich in bioflavonoid contents. Phytochemical study of the polar fraction of Juniperus sabina aerial parts resulted in the isolation of cupressuflavone (CPF) as the major component in addition to another two bioflavonoids, amentoflavone and robustaflavone. [...] Read more.

The polar fractions of the Juniperus species are rich in bioflavonoid contents. Phytochemical study of the polar fraction of Juniperus sabina aerial parts resulted in the isolation of cupressuflavone (CPF) as the major component in addition to another two bioflavonoids, amentoflavone and robustaflavone. Biflavonoids have various biological activities, such as antioxidant, anti-inflammatory, antibacterial, antiviral, hypoglycemic, neuroprotective, and antipsychotic effects. Previous studies have shown that the metabolism and elimination of biflavonoids in rats are fast, and their oral bioavailability is very low. One of the methods to improve the bioavailability of drugs is to alter the route of administration. Recently, nose-to-brain drug delivery has emerged as a reliable method to bypass the blood–brain barrier and treat neurological disorders. To find the most effective CPF formulation for reaching the brain, three different CPF formulations (A, B and C) were prepared as self-emulsifying drug delivery systems (SEDDS). The formulations were administered via the intranasal (IN) route and their effect on the spontaneous motor activity in addition to motor coordination and balance of rats was observed using the activity cage and rotarod, respectively. Moreover, pharmacokinetic investigation was used to determine the blood concentrations of the best formulation after 12 h. of the IN dose. The results showed that formulations B and C, but not A, decreased the locomotor activity and balance of rats. Formula C at IN dose of 5 mg/kg expressed the strongest effect on the tested animals. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 2309 KiB

Open AccessArticle

A Comparative UHPLC-Q-Trap-MS/MS-Based Metabolomics Analysis to Distinguish Foeniculum vulgare Cultivars’ Antioxidant Extracts

by Maria Assunta Crescenzi, Gilda D’Urso, Sonia Piacente and Paola Montoro

Molecules 2023, 28(2), 900; https://doi.org/10.3390/molecules28020900 - 16 Jan 2023

Cited by 3 | Viewed by 2126

Abstract

Among the environmental factors, seasonality is the one which most affects the metabolome of a plant. Depending on the harvest season, the plant may have a variable content of certain metabolites and thus may have different biological properties. Foeniculum vulgare is an annual plant [...] Read more.

Among the environmental factors, seasonality is the one which most affects the metabolome of a plant. Depending on the harvest season, the plant may have a variable content of certain metabolites and thus may have different biological properties. Foeniculum vulgare is an annual plant whose cultivation creates large amounts of waste rich in bioactive compounds. The present investigation was performed with the aim of determining the amount of biologically active compounds in F. vulgare wastes obtained from varieties of different seasonality. Ten polyphenolic compounds were quantified in the little stems and leaves of Tiziano, Pegaso, and Preludio cultivars by ultra performance liquid chromatography (UPLC) hyphenated to QTRAP mass spectrometry by using the MRM (multiple reaction monitoring) method. The antioxidant activity of hydroalcoholic extracts was then evaluated using TEAC and DPPH spectrophotometric assays, followed by a multivariate statistical analysis to determine the correlation between metabolite expression and antioxidant activity. The Preludio variety, grown in summer, showed a higher content of bioactive compounds, which guarantees it a better antioxidant power; kaempferol 3-O-glucuronide, quercetin 3-O-glucuronide, and quercetin 3-O-glucoside are the polyphenolic compounds that could be mainly responsible for the antioxidant effect of fennel. The PLS chemometric model, which correlated quantitative data obtained by a sensitive and selective LC-ESI-QTrap-MS/MS analysis of antioxidant activity, resulted in a selective tool to detect the compounds responsible for the activity shown by the extracts in chemical tests. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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20 pages, 1451 KiB

Open AccessArticle

Evaluation of Antioxidant and Anticancer Activity of Mono- and Polyfloral Moroccan Bee Pollen by Characterizing Phenolic and Volatile Compounds

by Volkan Aylanc, Samar Larbi, Ricardo Calhelha, Lillian Barros, Feriel Rezouga, María Shantal Rodríguez-Flores, María Carmen Seijo, Asmae El Ghouizi, Badiaa Lyoussi, Soraia I. Falcão and Miguel Vilas-Boas

Molecules 2023, 28(2), 835; https://doi.org/10.3390/molecules28020835 - 13 Jan 2023

Cited by 16 | Viewed by 3101

Abstract

Bee pollen is frequently characterized as a natural source of bioactive components, such as phenolic compounds, which are responsible for its pharmaceutical potential and nutritional properties. In this study, we evaluated the bioactive compound contents of mono- and polyfloral bee pollen samples using [...] Read more.

Bee pollen is frequently characterized as a natural source of bioactive components, such as phenolic compounds, which are responsible for its pharmaceutical potential and nutritional properties. In this study, we evaluated the bioactive compound contents of mono- and polyfloral bee pollen samples using spectroscopic and chromatographic methods and established links with their antioxidant and antitumor activity. The findings demonstrated that the botanical origin of bee pollen has a remarkable impact on its phenolic (3–17 mg GAE/g) and flavonoid (0.5–3.2 mg QE/g) contents. Liquid chromatography–mass spectrometry analysis revealed the presence of 35 phenolic and 13 phenylamide compounds in bee pollen, while gas chromatography–mass spectrometry showed its richness in volatiles, such as hydrocarbons, fatty acids, alcohols, ketones, etc. The concentration of bioactive compounds in each sample resulted in a substantial distinction in their antioxidant activity, DPPH (EC₅₀: 0.3–0.7 mg/mL), ABTS (0.8–1.3 mM Trolox/mg), and reducing power (0.03–0.05 mg GAE/g), with the most bioactive pollens being the monofloral samples from Olea europaea and Ononis spinosa. Complementarily, some samples revealed a moderate effect on cervical carcinoma (GI₅₀: 495 μg/mL) and breast adenocarcinoma (GI₅₀: 734 μg/mL) cell lines. This may be associated with compounds such as quercetin-O-diglucoside and kaempferol-3-O-rhamnoside, which are present in pollens from Olea europaea and Coriandrum, respectively. Overall, the results highlighted the potentiality of bee pollen to serve health-promoting formulations in the future. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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19 pages, 1460 KiB

Open AccessArticle

Grain Germination Changes the Profile of Phenolic Compounds and Benzoxazinoids in Wheat: A Study on Hard and Soft Cultivars

by Julia Baranzelli, Sabrina Somacal, Camila Sant’Anna Monteiro, Renius de Oliveira Mello, Eliseu Rodrigues, Osmar Damian Prestes, Rosalía López-Ruiz, Antonia Garrido Frenich, Roberto Romero-González, Martha Zavariz de Miranda and Tatiana Emanuelli

Molecules 2023, 28(2), 721; https://doi.org/10.3390/molecules28020721 - 11 Jan 2023

Cited by 8 | Viewed by 2777

Abstract

Pre-harvest sprouting is a frequent problem for wheat culture that can be simulated by laboratory-based germination. Despite reducing baking properties, wheat sprouting has been shown to increase the bioavailability of some nutrients. It was investigated whether wheat cultivars bearing distinct grain texture characteristics [...] Read more.

Pre-harvest sprouting is a frequent problem for wheat culture that can be simulated by laboratory-based germination. Despite reducing baking properties, wheat sprouting has been shown to increase the bioavailability of some nutrients. It was investigated whether wheat cultivars bearing distinct grain texture characteristics (BRS Guaraim, soft vs. BRS Marcante, hard texture) would have different behavior in terms of the changes in phytochemical compounds during germination. Using LC-Q-TOF-MS, higher contents of benzoxazinoids and flavonoids were found in the hard cultivar than in the soft one. Free phytochemicals, mainly benzoxazinoids, increased during germination in both cultivars. Before germination, soft and hard cultivars had a similar profile of matrix-bound phytochemicals, but during germination, these compounds have been shown to decrease only in the hard-texture cultivar, due to decreased levels of phenolic acids (trans-ferulic acid) and flavonoids (apigenin) that were bound to the cell wall through ester-type bonds. These findings confirm the hypothesis that hard and soft wheat cultivars have distinct behavior during germination concerning the changes in phytochemical compounds, namely the matrix-bound compounds. In addition, germination has been shown to remarkably increase the content of benzoxazinoids and the antioxidant capacity, which could bring a health-beneficial appeal for pre-harvested sprouted grains. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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16 pages, 1379 KiB

Open AccessArticle

Comparative Effects of Two Forms of Chitosan on Selected Phytochemical Properties of Plectranthus amboinicus (Lour.)

by Maria Stasińska-Jakubas, Barbara Hawrylak-Nowak, Magdalena Wójciak and Sławomir Dresler

Molecules 2023, 28(1), 376; https://doi.org/10.3390/molecules28010376 - 2 Jan 2023

Cited by 10 | Viewed by 2150

Abstract

In response to stress factors, plants produce a wide range of biologically active substances, from a group of secondary metabolites, which are applied in medicine and health prophylaxis. Chitosan is a well-known elicitor affecting secondary metabolism in plants, but its effect on the [...] Read more.

In response to stress factors, plants produce a wide range of biologically active substances, from a group of secondary metabolites, which are applied in medicine and health prophylaxis. Chitosan is a well-known elicitor affecting secondary metabolism in plants, but its effect on the phytochemical profile of Plectranthus amboinicus has not been assessed yet. In the present experiment, the effectiveness of the foliar application of two forms of chitosan (chitosan suspension or chitosan lactate) was compared in order to evaluate their potential to induce the accumulation of selected polyphenolic compounds in the aboveground parts of P. amboinicus. It was shown that chitosan lactate had substantially higher elicitation efficiency, as the use of this form exerted a beneficial effect on the analysed quality parameters of the raw material, especially the content of selected polyphenolic compounds (total content of polyphenols, flavonols, anthocyanins, and caffeic acid derivatives) and the free radical-scavenging activity of extracts from elicited plants. Concurrently, it had no phytotoxic effects. Hence, chitosan lactate-based elicitation can be an effective method for optimisation of the production of high-quality P. amboinicus raw material characterised by an increased concentration of health-promoting and antioxidant compounds. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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11 pages, 1467 KiB

Open AccessArticle

Enhancement of the Functional Properties of Mead Aged with Oak (Quercus) Chips at Different Toasting Levels

by Juciane Prois Fortes, Fernanda Wouters Franco, Julia Baranzelli, Gustavo Andrade Ugalde, Cristiano Augusto Ballus, Eliseu Rodrigues, Márcio Antônio Mazutti, Sabrina Somacal and Claudia Kaehler Sautter

Molecules 2023, 28(1), 56; https://doi.org/10.3390/molecules28010056 - 21 Dec 2022

Cited by 3 | Viewed by 2252

Abstract

Consumers increasingly prefer and seek functional beverages, which, given their characteristics, provide important bioactive compounds that help prevent and treat chronic diseases. Mead is a traditional fermented alcoholic beverage made from honey solution. The aging process of mead with oak chips is innovative [...] Read more.

Consumers increasingly prefer and seek functional beverages, which, given their characteristics, provide important bioactive compounds that help prevent and treat chronic diseases. Mead is a traditional fermented alcoholic beverage made from honey solution. The aging process of mead with oak chips is innovative and bestows functional characteristics to this beverage. Thus, in this study, we sought to develop and characterize a novel functional beverage by combining the health benefits of honey with the traditional aging process of alcoholic beverages in wood. Phenolic compounds, flavonoids, and antioxidant capacity were analyzed in mead using oak chips at different toasting levels and aged for 360 days. LC-ESI-QTOF-MS/MS was used to analyze the chemical profile of different meads. Over time, the aging process with oak chips showed a higher total phenolic and flavonoid content and antioxidant capacity. Eighteen compounds belonging to the classes of organic acids, phenolic acids, flavonoids, and tannins were identified in meads after 360 days. Our findings revealed that the addition of oak chips during aging contributed to p-coumaric, ellagic, abscisic, and chlorogenic acids, and naringenin, vanillin, and tiliroside significantly impacted the functional quality of mead. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 3299 KiB

Open AccessArticle

Salvianolic Acid B Strikes Back: New Evidence in the Modulation of Expression and Activity of Matrix Metalloproteinase 9 in MDA-MB-231 Human Breast Cancer Cells

by Andrea Ianni, Pierdomenico Ruggeri, Pierangelo Bellio, Francesco Martino, Giuseppe Celenza, Giuseppe Martino and Nicola Franceschini

Molecules 2022, 27(23), 8514; https://doi.org/10.3390/molecules27238514 - 3 Dec 2022

Cited by 1 | Viewed by 1696

Abstract

Salvianolic acid B (SalB) is a bioactive compound from Salviae miltiorrhizae, one of the most important traditional herbal medicines widely used in several countries for the treatment of cardiovascular diseases. The aim of this study was to evaluate the in vitro effect [...] Read more.

Salvianolic acid B (SalB) is a bioactive compound from Salviae miltiorrhizae, one of the most important traditional herbal medicines widely used in several countries for the treatment of cardiovascular diseases. The aim of this study was to evaluate the in vitro effect of SalB on the expression and the activity of matrix metalloproteinase 9 (MMP-9), a zinc-dependent proteolytic enzyme, in human MDA-MB-231 breast cancer cells. This cellular model is characterized by a marked invasive phenotype, supported by a high constitutive expression of MMPs, especially gelatinases. SalB was first of all evaluated by in silico approaches primarily aimed at predicting the main pharmacokinetic parameters. The most favorable interaction between the natural compound and MMP-9 was instead tested by molecular docking analysis that was subsequently verified by an enzymatic inhibition assay. MDA-MB-231 cells were treated with SalB 5 µM and 50 µM for 24 h and 48 h. The conditioned media obtained from treated cells were then analyzed by gelatin zymography and reverse zymography to, respectively, evaluate the MMP-9 activity and the presence of TIMP-1. The expression of the enzyme was then evaluated by Western blot on conditioned media and by analysis of transcripts through reverse transcriptase-polymerase chain reaction (RT-PCR). The in silico approach showed the ability of SalB to interact with the catalytic zinc ion of the enzyme, with a plausible competitive mode of action. The analysis of conditioned culture media showed a reduction in MMP-9 activity and the concomitant decrease in the enzyme concentration, partially confirmed by analysis of transcripts. SalB showed the ability to modulate the function of MMP-9 in MDA-MB-231 cells. To our knowledge, this is the first time in which the role of SalB on MMP-9 in a highly invasive cellular model is investigated. The obtained results impose further and more specific evaluations in order to obtain a better understanding of the biochemical mechanisms that regulate the interaction between this natural compound and the MMP-9. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 1270 KiB

Open AccessArticle

Metabolite Profiling of Alocasia gigantea Leaf Extract and Its Potential Anticancer Effect through Autophagy in Hepatocellular Carcinoma

by Hend Okasha, Tarek Aboushousha, Manuel A. Coimbra, Susana M. Cardoso and Mosad A. Ghareeb

Molecules 2022, 27(23), 8504; https://doi.org/10.3390/molecules27238504 - 3 Dec 2022

Cited by 3 | Viewed by 2082

Abstract

Hepatocellular carcinoma (HCC) is a poor-prognosis type of cancer with high resistance to chemotherapy, making the search for safe drugs a mandatory issue. Plant-derived products have potential to reduce negative side effects of cancer treatments. In this work, ability of a defatted methanolic [...] Read more.

Hepatocellular carcinoma (HCC) is a poor-prognosis type of cancer with high resistance to chemotherapy, making the search for safe drugs a mandatory issue. Plant-derived products have potential to reduce negative side effects of cancer treatments. In this work, ability of a defatted methanolic extract of Alocasia gigantea leaves to fight HCC was evaluated in an animal model. Overall, treatment of HCC-induced mice with the methanolic extract at 150 mg/kg body weight for four consecutive weeks caused induction of autophagy through silencing of the relative expression of autophagy suppressor (mTOR) and inducement of autophagy markers (AMPK, Beclin-1, and LC-3). Moreover, it improved preservation of the hepatic histological architecture of the animals, with minor hepatocytic changes but scattered foci of hepatocytic apoptosis. Chemical profiling of the methanolic extract via ultra-high-performance liquid chromatography coupled to a diode array detector and an electrospray mass spectrometer (UHPLC–DAD–ESI–MS/MS) allowed identification of di-C-glycosyl flavones, mostly represented by 6-C-hexosyl-8-C-pentosyl apigenin isomers, which may possibly be associated with inducement of the autophagy pathway in HCC. Overall, these outcomes gave an initial visualization of the operative effect of some compounds in A. gigantea leaves that are potential treatment for HCC. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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18 pages, 758 KiB

Open AccessArticle

Selection of Enzymatic Treatments for Upcycling Lentil Hulls into Ingredients Rich in Oligosaccharides and Free Phenolics

by Sara Bautista-Expósito, Albert Vandenberg, Montserrat Dueñas, Elena Peñas, Juana Frias and Cristina Martínez-Villaluenga

Molecules 2022, 27(23), 8458; https://doi.org/10.3390/molecules27238458 - 2 Dec 2022

Cited by 2 | Viewed by 1935

Abstract

In this study, the comprehensive chemical characterization of red lentil hulls obtained from the industrial production of football and split lentils was described. The lentil hulls were rich in dietary fiber (78.43 g/100 g dry weight with an insoluble to soluble fiber ratio [...] Read more.

In this study, the comprehensive chemical characterization of red lentil hulls obtained from the industrial production of football and split lentils was described. The lentil hulls were rich in dietary fiber (78.43 g/100 g dry weight with an insoluble to soluble fiber ratio of 4:1) and polyphenols (49.3 mg GAE/g dry weight, of which 55% was bound phenolics), which revealed the suitability of this lentil by-product as a source of bioactive compounds with recognized antioxidant and prebiotic properties. The release of oligosaccharides and phenolic compounds was accomplished by enzymatic hydrolysis, microwave treatment and a combination of both technologies. The key role played by the selection of a suitable enzymatic preparation was highlighted to maximize the yield of bioactive compounds and the functional properties of the lentil hull hydrolysates. Out of seven commercial preparations, the one with the most potential for use in a commercial context was Pectinex^® Ultra Tropical, which produced the highest yields of oligosaccharides (14 g/100 g lentil hull weight) and free phenolics (45.5 mg GAE/100 g lentil hull weight) and delivered a four-fold increase in terms of the original antioxidant activity. Finally, this enzyme was selected to analyze the effect of a microwave-assisted extraction pretreatment on the yield of enzymatic hydrolysis and the content of free phenolic compounds and oligosaccharides. The integrated microwave and enzymatic hydrolysis method, although it increased the solubilization yield of the lentil hulls (from 25% to 34%), it slightly decreased the content of oligosaccharides and proanthocyanidins and reduced the antioxidant activity. Therefore, the enzymatic hydrolysis treatment alone was more suitable for producing a lentil hull hydrolysate enriched in potential prebiotics and antioxidant compounds. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 1024 KiB

Open AccessFeature PaperArticle

Bioavailability Assessment of Yarrow Phenolic Compounds Using an In Vitro Digestion/Caco-2 Cell Model: Anti-Inflammatory Activity of Basolateral Fraction

by Marisol Villalva, Laura Jaime, María de las Nieves Siles-Sánchez and Susana Santoyo

Molecules 2022, 27(23), 8254; https://doi.org/10.3390/molecules27238254 - 26 Nov 2022

Cited by 6 | Viewed by 1983

Abstract

In this study, a combined in vitro digestion/Caco-2 model was performed with the aim to determine the phenolic compounds bioavailability of two yarrow extracts. HPLC-PAD characterisation indicated that the main components in both extracts were 3,5-dicaffeoylquinic acid (DCQA) and luteolin-7-O-glucoside. Analyses [...] Read more.

In this study, a combined in vitro digestion/Caco-2 model was performed with the aim to determine the phenolic compounds bioavailability of two yarrow extracts. HPLC-PAD characterisation indicated that the main components in both extracts were 3,5-dicaffeoylquinic acid (DCQA) and luteolin-7-O-glucoside. Analyses after the simulated digestion process revealed that phenolic composition was not affected during the oral phase, whereas gastric and intestinal phases represented critical steps for some individual phenolics, especially intestinal step. The transition from gastric medium to intestinal environment caused an important degradation of 3,5-DCQA (63–67% loss), whereas 3,4-DCQA and 4,5-DCQA increased significantly, suggesting an isomeric transformation within these caffeic acid derivatives. However, an approx. 90% of luteolin-7-O-glucoside was recovered after intestinal step. At the end of Caco-2 absorption experiments, casticin, diosmetin and centaureidin represented the most abundant compounds in the basolateral fraction. Moreover, this fraction presented anti-inflammatory activity since was able to inhibit the secretion of IL-1β and IL-6 pro-inflammatory cytokines. Thus, the presence in the basolateral fraction of flavonoid-aglycones from yarrow, could be related with the observed anti-inflammatory activity from yarrow extract. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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20 pages, 6832 KiB

Open AccessArticle

Resveratrol Inhibits Proliferation and Induces Autophagy by Blocking SREBP1 Expression in Oral Cancer Cells

by Masakatsu Fukuda, Yudai Ogasawara, Hiroyasu Hayashi, Katsuyuki Inoue and Hideaki Sakashita

Molecules 2022, 27(23), 8250; https://doi.org/10.3390/molecules27238250 - 26 Nov 2022

Cited by 24 | Viewed by 2100

Abstract

Resveratrol is a polyphenolic antioxidant found in grapes, red wine, and peanuts and has been reported to have anti-neoplastic effects on various cancer types. However, the exact mechanism of its anti-cancer effects in oral cancer is not fully understood and remains controversial. Resveratrol [...] Read more.

Resveratrol is a polyphenolic antioxidant found in grapes, red wine, and peanuts and has been reported to have anti-neoplastic effects on various cancer types. However, the exact mechanism of its anti-cancer effects in oral cancer is not fully understood and remains controversial. Resveratrol exhibits strong hypolipidemic effects; therefore, we examined its effect on lipid metabolism in oral cancer. Resveratrol significantly reduced cell viability and induced autophagic cell death in oral cancer cells but not in normal cells. This selective effect was accompanied by significantly reduced lipogenesis, which is caused by downregulation of the transcription factor sterol regulatory element-binding protein 1 (SREBP1) gene, followed by downregulation of the epidermal fatty acid-binding protein (E-FABP). It was strongly suggested that resveratrol-induced autophagy resulted from the inhibition of SREBP1-mediated cell survival signaling. Luciferase reporter assay further indicated that resveratrol has a potent and specific inhibitory effect on SREBP1-dependent transactivation. Importantly, resveratrol markedly suppressed the growth of oral cancer cells in an animal xenograft model, without exhibiting apparent cytotoxicity. In conclusion, resveratrol induces autophagy in oral cancer cells by suppressing lipid metabolism through the regulation of SREBP1 expression, which highlights a novel mechanism of the anti-cancer effect of resveratrol. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 2355 KiB

Open AccessArticle

Phenolic Compounds Recovery from Blood Orange Peels Using a Novel Green Infrared Technology Ired-Irrad^®, and Their Effect on the Inhibition of Aspergillus flavus Proliferation and Aflatoxin B1 Production

by Sally El Kantar, Hiba N. Rajha, André El Khoury, Mohamed Koubaa, Simon Nachef, Espérance Debs, Richard G. Maroun and Nicolas Louka

Molecules 2022, 27(22), 8061; https://doi.org/10.3390/molecules27228061 - 20 Nov 2022

Cited by 5 | Viewed by 2005

Abstract

The intensification of total phenolic compound (TPC) extraction from blood orange peels was optimized using a novel green infrared-assisted extraction technique (IRAE, Ired-Irrad^®) and compared to the conventional extraction using a water bath (WB). Response surface methodology (RSM) allowed for the [...] Read more.

The intensification of total phenolic compound (TPC) extraction from blood orange peels was optimized using a novel green infrared-assisted extraction technique (IRAE, Ired-Irrad^®) and compared to the conventional extraction using a water bath (WB). Response surface methodology (RSM) allowed for the optimization of ethanol concentration (E), time (t), and temperature (T) in terms of extracted TPC and their antiradical activity, for both WB extraction and IRAE. Using WB extraction, the multiple response optimums as obtained after 4 h at 73 °C and using 79% ethanol/water were 1.67 g GAE/100 g for TPC and 59% as DPPH inhibition percentage. IRAE increased the extraction of TPC by 18% using 52% ethanol/water after less than 1 h at 79 °C. This novel technology has the advantage of being easily scalable for industrial usage. HPLC analysis showed that IRAE enhanced the recovery of gallic acid, resveratrol, quercetin, caffeic acid, and hesperidin. IR extracts exhibited high bioactivity by inhibiting the production of Aflatoxin B1 by 98.9%. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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12 pages, 6938 KiB

Open AccessArticle

Fast Screening of Protein Tyrosine Phosphatase 1B Inhibitor from Salvia miltiorrhiza Bge by Cell Display-Based Ligand Fishing

by Xiaolin Bai, Wenqin Fan, Yingjie Luo, Yipei Liu, Yongmei Zhang and Xun Liao

Molecules 2022, 27(22), 7896; https://doi.org/10.3390/molecules27227896 - 15 Nov 2022

Cited by 4 | Viewed by 1843

Abstract

Salvia miltiorrhiza Bge is a medicinal plant (Chinese name “Danshen”) widely used for the treatment of hyperglycemia in traditional Chinese medicine. Protein tyrosine phosphatase 1B (PTP1B) has been recognized as a potential target for insulin sensitizing for the treatment of diabetes. In this [...] Read more.

Salvia miltiorrhiza Bge is a medicinal plant (Chinese name “Danshen”) widely used for the treatment of hyperglycemia in traditional Chinese medicine. Protein tyrosine phosphatase 1B (PTP1B) has been recognized as a potential target for insulin sensitizing for the treatment of diabetes. In this work, PTP1B was displayed at the surface of E. coli cells (EC-PTP1B) to be used as a bait for fishing of the enzyme’s inhibitors present in the aqueous extract of S. miltiorrhiza. Salvianolic acid B, a polyphenolic compound, was fished out by EC-PTP1B, which was found to inhibit PTP1B with an IC₅₀ value of 23.35 µM. The inhibitory mechanism of salvianolic acid B was further investigated by enzyme kinetic experiments and molecular docking, indicating salvianolic acid B was a non-competitive inhibitor for PTP1B (with Ki and Kis values of 31.71 µM and 20.08 µM, respectively) and its binding energy was −7.89 kcal/mol. It is interesting that in the comparative work using a traditional ligand fishing bait of PTP1B-immobilized magnetic nanoparticles (MNPs-PTP1B), no ligands were extracted at all. This study not only discovered a new PTP1B inhibitor from S. miltiorrhiza which is significant to understand the chemical basis for the hypoglycemic activity of this plant, but also indicated the effectiveness of cell display-based ligand fishing in screening of active compounds from complex herbal extracts. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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15 pages, 2152 KiB

Open AccessArticle

Camel Grass Phenolic Compounds: Targeting Inflammation and Neurologically Related Conditions

by Graciliana Lopes, Elisabete Gomes, Mariana Barbosa, João Bernardo and Patrícia Valentão

Molecules 2022, 27(22), 7707; https://doi.org/10.3390/molecules27227707 - 9 Nov 2022

Cited by 4 | Viewed by 2146

Abstract

Background: The use of plants for therapeutic purposes has been supported by growing scientific evidence. Methods: This work consisted of (i) characterizing the phenolic compounds present in both aqueous and hydroethanol (1:1, v/v) extracts of camel grass, by hyphenated liquid [...] Read more.

Background: The use of plants for therapeutic purposes has been supported by growing scientific evidence. Methods: This work consisted of (i) characterizing the phenolic compounds present in both aqueous and hydroethanol (1:1, v/v) extracts of camel grass, by hyphenated liquid chromatographic techniques, (ii) evaluating their anti-inflammatory, antioxidant, and neuromodulation potential, through in vitro cell and cell-free models, and (iii) establishing a relationship between the chemical profiles of the extracts and their biological activities. Results: Several caffeic acid and flavonoid derivatives were determined in both extracts. The extracts displayed scavenging capacity against the physiologically relevant nitric oxide (^•NO) and superoxide anion (O₂^•−) radicals, significantly reduced NO production in lipopolysaccharide (LPS)-stimulated macrophages (RAW 264.7), and inhibited the activity of hyaluronidase (HAase), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Some of these bioactivities were found to be related with the chemical profile of the extracts, namely with 3-caffeoylquinic, 4-caffeoylquinic, chlorogenic, and p-coumaric acids, as well as with luteolin and apigenin derivatives. Conclusions: This study reports, for the first time, the potential medicinal properties of aqueous and hydroethanol extracts of camel grass in the RAW 264.7 cell model of inflammation, and in neurologically related conditions. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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19 pages, 917 KiB

Open AccessArticle

Characterization of Sideritis clandestina subsp. peloponnesiaca Polar Glycosides and Phytochemical Comparison to Other Mountain Tea Populations

by Virginia D. Dimaki, Konstantina Zeliou, Fotini Nakka, Michaela Stavreli, Ioannis Bakratsas, Ligeri Papaioannou, Gregoris Iatrou and Fotini N. Lamari

Molecules 2022, 27(21), 7613; https://doi.org/10.3390/molecules27217613 - 6 Nov 2022

Cited by 9 | Viewed by 2812

Abstract

Sideritis clandestina (Bory & Chaub.) Hayek subsp. peloponnesiaca (Boiss. & Heldr.) Baden (SCP) is endemic to the mountains of the Northern Peloponnese (Greece). This and other Sideritis taxa, collectively known as mountain tea, are widely ingested as beverages for refreshment or medicinal purposes. [...] Read more.

Sideritis clandestina (Bory & Chaub.) Hayek subsp. peloponnesiaca (Boiss. & Heldr.) Baden (SCP) is endemic to the mountains of the Northern Peloponnese (Greece). This and other Sideritis taxa, collectively known as mountain tea, are widely ingested as beverages for refreshment or medicinal purposes. We describe a methodology for the characterization of SCP. Four iridoid glycosides (monomelittoside, melittoside, ajugoside, and 7-O-acetyl-8-epiloganic acid), two phenolic acid glycosides (vanillic and salicylic acid glycosides), and three caffeoyl ester glycosides (chlorogenic acid, verbascoside, and isoverbascoside) were isolated from SCP for the first time. We used ultrasound-assisted extraction of 3 g of plant material to produce petroleum ether and aqueous extracts, which we then analyzed using GC/MS and LC/MS. This was applied to eight samples from four different taxa. In total, 70 volatile and 27 polar metabolites were determined. The S. clandestina samples had a lower phenolic content and weaker antioxidant properties than S. raeseri and S. scardica. However, S. clandestina ssp. clandestina seemed to be the most aromatic taxon, with almost double the number of volatiles as the others. Τhis study could contribute to authentication and chemotaxonomic studies of Sideritis taxa. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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21 pages, 5244 KiB

Open AccessArticle

Anti-Inflammatory, Antioxidative, and Nitric Oxide-Scavenging Activities of a Quercetin Nanosuspension with Polyethylene Glycol in LPS-Induced RAW 264.7 Macrophages

by Sang Gu Kang, Gi Baek Lee, Ramachandran Vinayagam, Geum Sook Do, Se Yong Oh, Su Jin Yang, Jun Bum Kwon and Mahendra Singh

Molecules 2022, 27(21), 7432; https://doi.org/10.3390/molecules27217432 - 1 Nov 2022

Cited by 16 | Viewed by 3794

Abstract

Quercetin (Qu) is a dietary antioxidant and a member of flavonoids in the plant polyphenol family. Qu has a high ability to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS) molecules; hence, exhibiting beneficial effects in preventing obesity, diabetes, cancer, cardiovascular [...] Read more.

Quercetin (Qu) is a dietary antioxidant and a member of flavonoids in the plant polyphenol family. Qu has a high ability to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS) molecules; hence, exhibiting beneficial effects in preventing obesity, diabetes, cancer, cardiovascular diseases, and inflammation. However, quercetin has low bioavailability due to poor water solubility, low absorption, and rapid excretion from the body. To address these issues, the usage of Qu nanosuspensions can improve physical stability, solubility, and pharmacokinetics. Therefore, we developed a Qu and polyethylene glycol nanosuspension (Qu-PEG NS) and confirmed its interaction by Fourier transform infrared analysis. Qu-PEG NS did not show cytotoxicity to HaCaT and RAW 264.7 cells. Furthermore, Qu-PEG NS effectively reduced the nitrogen oxide (NO) production in lipopolysaccharide (LPS)-induced inflammatory RAW 264.7 cells. Additionally, Qu-PEG NS effectively lowered the levels of COX-2, NF-κB p65, and IL-1β in the LPS-induced inflammatory RAW 264.7 cells. Specifically, Qu-PEG NS exhibited anti-inflammatory properties by scavenging the ROS and RNS and mediated the inhibition of NF-κB signaling pathways. In addition, Qu-PEG NS had a high antioxidant effect and antibacterial activity against Escherichia coli and Bacillus cereus. Therefore, the developed novel nanosuspension showed comparable antioxidant, anti-inflammatory, and antibacterial functions and may also improve solubility and physical stability compared to raw quercetin. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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25 pages, 4165 KiB

Open AccessFeature PaperArticle

The Potential Neuroprotective Effect of Cyperus esculentus L. Extract in Scopolamine-Induced Cognitive Impairment in Rats: Extensive Biological and Metabolomics Approaches

by Marwa M. Saeed, Álvaro Fernández-Ochoa, Fatema R. Saber, Rabab H. Sayed, María de la Luz Cádiz-Gurrea, Amira K. Elmotayam, Francisco Javier Leyva-Jiménez, Antonio Segura-Carretero and Rania I. Nadeem

Molecules 2022, 27(20), 7118; https://doi.org/10.3390/molecules27207118 - 21 Oct 2022

Cited by 8 | Viewed by 2668

Abstract

The aim of the present study is to investigate the phytochemical composition of tiger nut (TN) (Cyperus esculentus L.) and its neuroprotective potential in scopolamine (Scop)-induced cognitive impairment in rats. The UHPLC-ESI-QTOF-MS analysis enabled the putative annotation of 88 metabolites, such as [...] Read more.

The aim of the present study is to investigate the phytochemical composition of tiger nut (TN) (Cyperus esculentus L.) and its neuroprotective potential in scopolamine (Scop)-induced cognitive impairment in rats. The UHPLC-ESI-QTOF-MS analysis enabled the putative annotation of 88 metabolites, such as saccharides, amino acids, organic acids, fatty acids, phenolic compounds and flavonoids. Treatment with TN extract restored Scop-induced learning and memory impairments. In parallel, TN extract succeeded in lowering amyloid beta, β-secretase protein expression and acetylcholine esterase (AChE) activity in the hippocampus of rats. TN extract decreased malondialdehyde levels, restored antioxidant levels and reduced proinflammatory cytokines as well as the Bax/Bcl2 ratio. Histopathological analysis demonstrated marked neuroprotection in TN-treated groups. In conclusion, the present study reveals that TN extract attenuates Scop-induced memory impairments by diminishing amyloid beta aggregates, as well as its anti-inflammatory, antioxidant, anti-apoptotic and anti-AChE activities. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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18 pages, 3364 KiB

Open AccessArticle

Synthesis and Characterization of Curcumin-Loaded Nanoparticles of Poly(Glycerol Sebacate): A Novel Highly Stable Anticancer System

by Alessio Massironi, Stefania Marzorati, Alessandra Marinelli, Marta Toccaceli, Stefano Gazzotti, Marco Aldo Ortenzi, Daniela Maggioni, Katia Petroni and Luisella Verotta

Molecules 2022, 27(20), 6997; https://doi.org/10.3390/molecules27206997 - 18 Oct 2022

Cited by 10 | Viewed by 2303

Abstract

The research for alternative administration methods for anticancer drugs, towards enhanced effectiveness and selectivity, represents a major challenge for the scientific community. In the last decade, polymeric nanostructured delivery systems represented a promising alternative to conventional drug administration since they ensure secure transport [...] Read more.

The research for alternative administration methods for anticancer drugs, towards enhanced effectiveness and selectivity, represents a major challenge for the scientific community. In the last decade, polymeric nanostructured delivery systems represented a promising alternative to conventional drug administration since they ensure secure transport to the selected target, providing active compounds protection against elimination, while minimizing drug toxicity to non-target cells. In the present research, poly(glycerol sebacate), a biocompatible polymer, was synthesized and then nanostructured to allow curcumin encapsulation, a naturally occurring polyphenolic phytochemical isolated from the powdered rhizome of Curcuma longa L. Curcumin was selected as an anticancer agent in virtue of its strong chemotherapeutic activity against different cancer types combined with good cytocompatibility within healthy cells. Despite its strong and fascinating biological activity, its possible exploitation as a novel chemotherapeutic has been hampered by its low water solubility, which results in poor absorption and low bioavailability upon oral administration. Hence, its encapsulation within nanoparticles may overcome such issues. Nanoparticles obtained through nanoprecipitation, an easy and scalable technique, were characterized in terms of size and stability over time using dynamic light scattering and transmission electron microscopy, confirming their nanosized dimensions and spherical shape. Finally, biological investigation demonstrated an enhanced cytotoxic effect of curcumin-loaded PGS-NPs on human cervical cancer cells compared to free curcumin. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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11 pages, 2213 KiB

Open AccessArticle

Antiglycation Effects of Adlay Seed and Its Active Polyphenol Compounds: An In Vitro Study

by Cheng-Pei Chung, Shih-Min Hsia, Wen-Szu Chang, Din-Wen Huang, Wen-Chang Chiang, Mohamed Ali, Ming-Yi Lee and Chi-Hao Wu

Molecules 2022, 27(19), 6729; https://doi.org/10.3390/molecules27196729 - 9 Oct 2022

Cited by 4 | Viewed by 2044

Abstract

This study aimed to evaluate the antiglycation effects of adlay on protein glycation using in vitro glycation assays. Adlay seed was divided into the following four parts: the hull (AH), testa (AT), bran (AB), and polished adlay (PA). A solvent extraction technique and [...] Read more.

This study aimed to evaluate the antiglycation effects of adlay on protein glycation using in vitro glycation assays. Adlay seed was divided into the following four parts: the hull (AH), testa (AT), bran (AB), and polished adlay (PA). A solvent extraction technique and column chromatography were utilized to investigate the active fractions and components of adlay. Based on a BSA-glucose assay, the ethanolic extracts of AT (ATE) and AB (ABE) revealed a greater capacity to inhibit protein glycation. ATE was further consecutively partitioned into four solvent fractions with n-hexane, ethyl acetate (ATE-Ea), 1-butanol (ATE-BuOH), and water. ATE-BuOH and -Ea show marked inhibition of glucose-mediated glycation. Medium–high polarity subfractions eluted from ATE-BuOH below 50% methanol with Diaion HP-20, ATE-BuOH-c to -f, exhibited superior antiglycation activity, with a maximum inhibitory percentage of 88%. Two phenolic compounds, chlorogenic acid and ferulic acid, identified in ATE-BuOH with HPLC, exhibited potent inhibition of the individual stage of protein glycation and its subsequent crosslinking, as evaluated by the BSA-glucose assay, BS-methylglyoxal (MGO) assay, and G.K. peptide-ribose assay. In conclusion, this study demonstrated the antiglycation properties of ATE in vitro that suggest a beneficial effect in targeting hyperglycemia-mediated protein modification. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 1827 KiB

Open AccessArticle

Comprehensive Lichenometabolomic Exploration of Ramalina conduplicans Vain Using UPLC-Q-ToF-MS/MS: An Identification of Free Radical Scavenging and Anti-Hyperglycemic Constituents

by Tatapudi Kiran Kumar, Bandi Siva, Ajay Anand, Komati Anusha, Satish Mohabe, Araveeti Madhusudana Reddy, Françoise Le Devehat, Ashok Kumar Tiwari, Joël Boustie and Katragadda Suresh Babu

Molecules 2022, 27(19), 6720; https://doi.org/10.3390/molecules27196720 - 9 Oct 2022

Cited by 4 | Viewed by 2382

Abstract

In this study, we propose ultra-performance liquid chromatography coupled with quadrupole/time-of-flight mass spectrometry (UPLC-QToF-MS/MS)-guided metabolite isolation as a choice analytical approach to the ongoing structure–activity investigations of chemical isolates from the edible lichen, Ramalina conduplicans Vain. This strategy led to the isolation and [...] Read more.

In this study, we propose ultra-performance liquid chromatography coupled with quadrupole/time-of-flight mass spectrometry (UPLC-QToF-MS/MS)-guided metabolite isolation as a choice analytical approach to the ongoing structure–activity investigations of chemical isolates from the edible lichen, Ramalina conduplicans Vain. This strategy led to the isolation and identification of a new depside (5) along with 13 known compounds (1–4, 6–14), most of which being newly described in this lichen species. The structures of the isolates were established by detailed analysis of their spectral data (IR, NMR, and Mass). The acetone extract was further analyzed by UPLC-Q-ToF-MS/MS in a negative ionization mode, which facilitated the identification and confirmation of 18 compounds based on their fragmentation patterns. The antioxidant capacities of the lichen acetone extract (AE) and isolates were measured by tracking DPPH and ABTS free radical scavenging activities. Most isolates displayed marked radical scavenging activities against ABTS while moderate activities were observed against DPPH radical scavenging. Except for atranol (14), oxidative DNA damage was limited by all the tested compounds, with a marked protection for the novel isolated compound (5), as previously noted for the acetone extract (p < 0.001). Furthermore, compound (4) and acetone extract (AE) have inhibited intestinal α-glucosidase enzyme significantly (p < 0.01). Although some phytochemical studies were already performed on this lichen, this study provided new insights into the isolation and identification of bioactive compounds, illustrating interest in future novel analytical techniques. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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16 pages, 2508 KiB

Open AccessArticle

Lichen Extracts from Cetrarioid Clade Provide Neuroprotection against Hydrogen Peroxide-Induced Oxidative Stress

by Isabel Ureña-Vacas, Elena González-Burgos, Pradeep Kumar Divakar and María Pilar Gómez-Serranillos

Molecules 2022, 27(19), 6520; https://doi.org/10.3390/molecules27196520 - 2 Oct 2022

Cited by 9 | Viewed by 2310

Abstract

Oxidative stress is involved in the pathophysiology of many neurodegenerative diseases. Lichens have antioxidant properties attributed to their own secondary metabolites with phenol groups. Very few studies delve into the protective capacity of lichens based on their antioxidant properties and their action mechanism. [...] Read more.

Oxidative stress is involved in the pathophysiology of many neurodegenerative diseases. Lichens have antioxidant properties attributed to their own secondary metabolites with phenol groups. Very few studies delve into the protective capacity of lichens based on their antioxidant properties and their action mechanism. The present study evaluates the neuroprotective role of Dactylina arctica, Nephromopsis stracheyi, Tuckermannopsis americana and Vulpicida pinastri methanol extracts in a hydrogen peroxide (H₂O₂) oxidative stress model in neuroblastoma cell line “SH-SY5Y cells”. Cells were pretreated with different concentrations of lichen extracts (24 h) before H₂O₂ (250 µM, 1 h). Our results showed that D. arctica (10 µg/mL), N. stracheyi (25 µg/mL), T. americana (50 µg/mL) and V. pinastri (5 µg/mL) prevented cell death and morphological changes. Moreover, these lichens significantly inhibited reactive oxygen species (ROS) production and lipid peroxidation and increased superoxide dismutase (SOD) and catalase (CAT) activities and glutathione (GSH) levels. Furthermore, they attenuated mitochondrial membrane potential decline and calcium homeostasis disruption. Finally, high-performance liquid chromatography (HPLC) analysis revealed that the secondary metabolites were gyrophoric acid and lecanoric acid in D. artica, usnic acid, pinastric acid and vulpinic acid in V. pinastri, and alectoronic acid in T. americana. In conclusion, D. arctica and V. pinastri are the most promising lichens to prevent and to treat oxidative stress-related neurodegenerative diseases. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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19 pages, 4077 KiB

Open AccessArticle

Phytochemicals from Red Onion, Grown with Eco-Sustainable Fertilizers, Protect Mammalian Cells from Oxidative Stress, Increasing Their Viability

by Maria Laura Matrella, Alessio Valletti, Federica Marra, Carmelo Mallamaci, Tiziana Cocco and Adele Muscolo

Molecules 2022, 27(19), 6365; https://doi.org/10.3390/molecules27196365 - 27 Sep 2022

Cited by 6 | Viewed by 2313

Abstract

Red onion, a species of great economic importance rich in phytochemicals (bioactive compounds) known for its medicinal properties, was fertilized with sulphur-bentonite enriched with orange residue or olive pomace, with the aim of producing onion enriched in health beneficial compounds. There is a [...] Read more.

Red onion, a species of great economic importance rich in phytochemicals (bioactive compounds) known for its medicinal properties, was fertilized with sulphur-bentonite enriched with orange residue or olive pomace, with the aim of producing onion enriched in health beneficial compounds. There is a worldwide great demand of minimally processed food or food ingredients with functional properties because of a new awareness of how important healthy functional nutrition is in life. Phytochemicals have the capacity to regulate most of the metabolic processes resulting in health benefits. Red onion bioactive compound quantity and quality can vary according to cultivation practices. The main aims of the current research were to determine the chemical characteristics of the crude extracts from red onion bulbs differently fertilized and to evaluate their biological activity in normal and oxidative stress conditions. The lyophilized onion bulbs have been tested in vitro on two cellular models, i.e., the H9c2 rat cardiomyoblast cell line and primary human dermal fibroblasts, in terms of viability and oxygen radical homeostasis. The results evidenced different phytochemical compositions and antioxidant activities of the extracts obtained from red onions differently fertilized. Sulphur-bentonite fertilizers containing orange waste and olive pomace positively affected the red onion quality with respect to the red onion control, evidencing that sulphur-bentonite-organic fertilization was able to stimulate plant a secondary metabolism inducing the production of phytochemicals with healthy functions. A positive effect of the extracts from red onions treated with fertilizers—in particular, with those containing orange waste, such as the reduction of oxidative stress and induction of cell viability of H9c2 and human fibroblasts—was observed, showing a concentration- and time-dependent profile. The results evidenced that the positive effects were related to the phenols and, in particular, to chlorogenic and p-coumaric acids and to the flavonol kaempferol, which were more present in red onion treated with low orange residue than in the other treated ones. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 2813 KiB

Open AccessArticle

Cytotoxic Effect of Rosmarinus officinalis Extract on Glioblastoma and Rhabdomyosarcoma Cell Lines

by Eleni Kakouri, Olti Nikola, Charalabos Kanakis, Kyriaki Hatziagapiou, George I. Lambrou, Panayiotis Trigas, Christina Kanaka-Gantenbein and Petros A. Tarantilis

Molecules 2022, 27(19), 6348; https://doi.org/10.3390/molecules27196348 - 26 Sep 2022

Cited by 8 | Viewed by 1946

Abstract

Rosmarinus officinalis is a well-studied plant, known for its therapeutic properties. However, its biological activity against several diseases is not known in detail. The aim of this study is to present new data regarding the cytotoxic activity of a hydroethanolic extract of Rosmarinus [...] Read more.

Rosmarinus officinalis is a well-studied plant, known for its therapeutic properties. However, its biological activity against several diseases is not known in detail. The aim of this study is to present new data regarding the cytotoxic activity of a hydroethanolic extract of Rosmarinus officinalis on glioblastoma (A172) and rhabdomyosarcoma (TE671) cancer cell lines. The chemical composition of the extract is evaluated using liquid chromatography combined with time-of-flight mass spectrometry, alongside its total phenolic content and antioxidant activity. The extract showed a promising time- and dose-dependent cytotoxic activity against both cell lines. The lowest IC₅₀ values for both cell lines were calculated at 72 h after treatment and correspond to 0.249 ± 1.09 mg/mL for TE671 cell line and 0.577 ± 0.98 mg/mL for A172 cell line. The extract presented high phenolic content, equal to 35.65 ± 0.03 mg GAE/g of dry material as well as a strong antioxidant activity. The IC₅₀ values for the antioxidant assays were estimated at 12.8 ± 2.7 μg/mL (DPPH assay) and 6.98 ± 1.9 μg/mL (ABTS assay). The compound detected in abundance was carnosol, a phenolic diterpene, followed by the polyphenol rosmarinic acid, while the presence of phenolic compounds such as rhamnetin glucoside, hesperidin, cirsimaritin was notable. These preliminary results suggest that R. officinalis is a potential, alternative source of bioactive compounds to further examine for abilities against glioblastoma and rhabdomyosarcoma. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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15 pages, 3025 KiB

Open AccessArticle

Protective Effects of PollenAid Plus Soft Gel Capsules’ Hydroalcoholic Extract in Isolated Prostates and Ovaries Exposed to Lipopolysaccharide

by Annalisa Chiavaroli, Simonetta Cristina Di Simone, Alessandra Acquaviva, Maria Loreta Libero, Claudia Campana, Lucia Recinella, Sheila Leone, Luigi Brunetti, Giustino Orlando, Nilofar, Irene Vitale, Stefania Cesa, Gokhan Zengin, Luigi Menghini and Claudio Ferrante

Molecules 2022, 27(19), 6279; https://doi.org/10.3390/molecules27196279 - 23 Sep 2022

Cited by 7 | Viewed by 2464

Abstract

Pollen extract represents an innovative approach for the management of the clinical symptoms related to prostatitis and pelvic inflammatory disease (PID). In this context, the aims of the present work were to analyze the phenolic composition of a hydroalcoholic extract of PollenAid Plus [...] Read more.

Pollen extract represents an innovative approach for the management of the clinical symptoms related to prostatitis and pelvic inflammatory disease (PID). In this context, the aims of the present work were to analyze the phenolic composition of a hydroalcoholic extract of PollenAid Plus soft gel capsules, and to evaluate the extract’s cytotoxic effects, in human prostate cancer PC3 cells and human ovary cancer OVCAR-3 cells. Additionally, protective effects were investigated in isolated prostate and ovary specimens exposed to lipopolysaccharide (LPS). The phytochemical investigation identified catechin, chlorogenic acid, gentisic acid, and 3-hydroxytyrosol as the prominent phenolics. The extract did not exert a relevant cytotoxic effect on PC3 and OVCAR-3 cells. However, the extract showed a dose-dependent inhibition of pro-inflammatory IL-6 and TNF-α gene expression in prostate and ovary specimens, and the extract was effective in preventing the LPS-induced upregulation of CAT and SOD gene expression, which are deeply involved in tissue antioxidant defense systems. Finally, a docking approach suggested the capability of catechin and chlorogenic acid to interact with the TRPV1 receptor, playing a master role in prostate inflammation. Overall, the present findings demonstrated anti-inflammatory and antioxidant effects of this formulation; thus, suggesting its capability in the management of the clinical symptoms related to prostatitis and PID. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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9 pages, 2685 KiB

Open AccessArticle

Comparison of the Antihypertensive Activity of Phenolic Acids

by Myeongnam Yu, Hyun Joo Kim, Huijin Heo, Minjun Kim, Yesol Jeon, Hana Lee and Junsoo Lee

Molecules 2022, 27(19), 6185; https://doi.org/10.3390/molecules27196185 - 21 Sep 2022

Cited by 16 | Viewed by 2011

Abstract

Phenolic acids, found in cereals, legumes, vegetables, and fruits, have various biological functions. We aimed to compare the antihypertensive potential of different phenolic acids by evaluating their ACE inhibitory activity and cytoprotective capacity in EA.hy 926 endothelial cells. In addition, we explored the [...] Read more.

Phenolic acids, found in cereals, legumes, vegetables, and fruits, have various biological functions. We aimed to compare the antihypertensive potential of different phenolic acids by evaluating their ACE inhibitory activity and cytoprotective capacity in EA.hy 926 endothelial cells. In addition, we explored the mechanism underlying the antihypertensive activity of sinapic acid. Of all the phenolic acids studied, sinapic acid, caffeic acid, coumaric acid, and ferulic acid significantly inhibited ACE activity. Moreover, gallic acid, sinapic acid, and ferulic acid significantly enhanced intracellular NO production. Based on the results of GSH depletion, ROS production, and MDA level analyses, sinapic acid was selected to study the mechanism underlying the antihypertensive effect. Sinapic acid decreases endothelial dysfunction by enhancing the expression of antioxidant-related proteins. Sinapic acid increased phosphorylation of eNOS and Akt in a dose-dependent manner. These findings indicate the potential of sinapic acid as a treatment for hypertension. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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25 pages, 3633 KiB

Open AccessArticle

Selectivity Tuning by Natural Deep Eutectic Solvents (NADESs) for Extraction of Bioactive Compounds from Cytinus hypocistis—Studies of Antioxidative, Enzyme-Inhibitive Properties and LC-MS Profiles

by Gokhan Zengin, María de la Luz Cádiz-Gurrea, Álvaro Fernández-Ochoa, Francisco Javier Leyva-Jiménez, Antonio Segura Carretero, Malwina Momotko, Evren Yildiztugay, Refik Karatas, Sharmeen Jugreet, Mohamad Fawzi Mahomoodally and Grzegorz Boczkaj

Molecules 2022, 27(18), 5788; https://doi.org/10.3390/molecules27185788 - 7 Sep 2022

Cited by 15 | Viewed by 2415

Abstract

In the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. [...] Read more.

In the present study, the extracts of Cytinus hypocistis (L.) L using both traditional solvents (hexane, ethyl acetate, dichloromethane, ethanol, ethanol/water, and water) and natural deep eutectic solvents (NADESs) were investigated in terms of their total polyphenolic contents and antioxidant and enzyme-inhibitive properties. The extracts were found to possess total phenolic and total flavonoid contents in the ranges of 26.47–186.13 mg GAE/g and 0.68–12.55 mg RE/g, respectively. Higher total phenolic contents were obtained for NADES extracts. Compositional differences were reported in relation to antioxidant potential studied by several assays (DPPH: 70.19–939.35 mg TE/g, ABTS: 172.56–4026.50 mg TE/g; CUPRAC: 97.41–1730.38 mg TE/g, FRAP: 84.11–1534.85 mg TE/g). Application of NADESs (choline chloride—urea 1:2, a so-called Reline) allowed one to obtain the highest number of extracts having antioxidant potential in the radical scavenging and reducing assays. NADES-B (protonated by HCl L-proline-xylitol 5:1) was the only extractant from the studied solvents that isolated a specific fraction without chelating activity. Reline extract exhibited the highest acetylcholinesterase inhibition compared to NADES-B and NADES-C (protonated by H₂SO₄ L-proline-xylitol 5:1) extracts, which showed no inhibition. The NADES extracts were observed to have higher tyrosinase inhibitory properties compared to extracts obtained by traditional organic solvents. Furthermore, the NADES extracts were relatively better inhibitors of the diabetic enzymes. These findings provided an interesting comparison in terms of total polyphenolic content yields, antioxidant and enzyme inhibitory properties (cholinesterase, amylase, glucosidase, and tyrosinase) between traditional solvent extracts and NADES extracts, used as an alternative. While the organic solvents showed better antioxidant activity, the NADES extracts were found to have some other improved properties, such as higher total phenolic content and enzyme-inhibiting properties, suggesting functional prospects for their use in phytonutrient extraction and fractionation. The obtained results could also be used to give a broad overview of the different biological potentials of C. hypocistis. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 3158 KiB

Open AccessArticle

Wistin Exerts an Anti-Inflammatory Effect via Nuclear Factor-κB and p38 Signaling Pathways in Lipopolysaccharide-Stimulated RAW264.7 Cells

by Jangeun An, Gyoungah Ryu, Seong-Ah Shin, Huiji Kim, Mi-Jeong Ahn, Jun Hyuck Lee and Chang Sup Lee

Molecules 2022, 27(17), 5719; https://doi.org/10.3390/molecules27175719 - 5 Sep 2022

Cited by 6 | Viewed by 2171

Abstract

Inflammation is an immune response to cellular damage caused by various stimuli (internal or external) and is essential to human health. However, excessive inflammatory responses may be detrimental to the host. Considering that the existing drugs for the treatment of inflammatory diseases have [...] Read more.

Inflammation is an immune response to cellular damage caused by various stimuli (internal or external) and is essential to human health. However, excessive inflammatory responses may be detrimental to the host. Considering that the existing drugs for the treatment of inflammatory diseases have various side effects, such as allergic reactions, stomach ulcers, and cardiovascular problems, there is a need for research on new anti-inflammatory agents with low toxicity and fewer side effects. As 4′,6-dimethoxyisoflavone-7-O-β-d-glucopyranoside (wistin) is a phytochemical that belongs to an isoflavonoid family, we investigated whether wistin could potentially serve as a novel anti-inflammatory agent. In this study, we found that wistin significantly reduced the production of nitric oxide and intracellular reactive oxygen species in lipopolysaccharide-stimulated RAW 264.7 cells. Moreover, wistin reduced the mRNA levels of pro-inflammatory enzymes (inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2)) and cytokines (interleukin (IL)-1β and IL-6) and significantly reduced the protein expression of pro-inflammatory enzymes (iNOS and COX-2). Furthermore, wistin reduced the activation of the nuclear factor-κB and p38 signaling pathways. Together, these results suggest that wistin is a prospective candidate for the development of anti-inflammatory drugs. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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15 pages, 1625 KiB

Open AccessArticle

Pomegranate Wastes Are Rich in Bioactive Compounds with Potential Benefit on Human Health

by Federica Marra, Beatrix Petrovicova, Francesco Canino, Angela Maffia, Carmelo Mallamaci and Adele Muscolo

Molecules 2022, 27(17), 5555; https://doi.org/10.3390/molecules27175555 - 29 Aug 2022

Cited by 19 | Viewed by 2555

Abstract

Pomegranate use is increasing worldwide, as it is considered a tasteful healthy food. It is mainly used as fruit, juice, and jam. The pomegranate peel represents about 40–50% of the total fruit weight and contains numerous and diverse bioactive substances. The aim of [...] Read more.

Pomegranate use is increasing worldwide, as it is considered a tasteful healthy food. It is mainly used as fruit, juice, and jam. The pomegranate peel represents about 40–50% of the total fruit weight and contains numerous and diverse bioactive substances. The aim of this research was to analyze the pomegranate peel chemical composition of Wonderful cultivated in Southern Italy and treated with an innovative physic dry concentration procedure in comparison with the peel composition of freeze-dried Wonderful cultivated in Southern Italy, freeze-dried Wonderful cultivated in South Africa, and freeze-dried pomegranate cultivated in India. The specific aim was to verify how much the growth area, cultivar type, and dry procedure influenced the chemical composition of the peels in terms of valuable bioactive compounds. Spectrophotometric and HPLC identification methods were used to detect antioxidants, antioxidant activities, and phenolic and flavonoid components. Results evidenced that in pomegranate peels of Wonderful cultivated in Calabria and dried with the innovative process, total phenolic substances, total flavonoids, vitamin C, vitamin E, and antioxidant activities were the highest. Great amounts of single phenolic acids and flavonoids were found in Calabrian Wonderful peels dried with the innovative process. Overall, it emerged that a great amount of bioactive and diverse compounds found in Calabrian Wonderful pomegranate peel comes from the niche pedoclimatic conditions, and the physic drying innovative methodology turned out to be an advantageous procedure to concentrate and conserve biocompounds. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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12 pages, 739 KiB

Open AccessArticle

Determination of the Phenolic Profile, and Evaluation of Biological Activities of Hydroethanolic Extract from Aerial Parts of Origanum compactum from Morocco

by Mounia Chroho, Aziz Bouymajane, Mustapha Aazza, Yassine Oulad El Majdoub, Francesco Cacciola, Luigi Mondello, Touriya Zair and Latifa Bouissane

Molecules 2022, 27(16), 5189; https://doi.org/10.3390/molecules27165189 - 15 Aug 2022

Cited by 9 | Viewed by 2691

Abstract

Origanum compactum belonging to the family Lamiaceae is widely used in food and pharmaceutical fields due to its biologically active substances. We aimed to investigate the total phenol and flavonoid contents and the phenolic composition, and to evaluate the antioxidant and antibacterial properties [...] Read more.

Origanum compactum belonging to the family Lamiaceae is widely used in food and pharmaceutical fields due to its biologically active substances. We aimed to investigate the total phenol and flavonoid contents and the phenolic composition, and to evaluate the antioxidant and antibacterial properties of hydroethanolic extract from of Origanum compactum. Total phenol and flavonoid contents were evaluated using gallic acid and quercetin as standards, respectively, and the phenolic profile was characterized using high-performance liquid chromatography coupled to a photodiode array and electrospray ionization mass spectrometry (HPLC-PDA-ESI/MS). The antioxidant activity was determined by two methods: ferric reducing power (FRAP) assay and the phosphomolybdate method. The antibacterial effect was evaluated against four bacteria (Escherichia coli, Salmonella typhimurium, Staphylococcus aureus and Listeria monocytogenes) using the broth microdilution method. The findings show that the total phenolic and flavonoid contents were 107.789 ± 5.39 mg GAE/g dm and 14,977 ± 0.79 mg QE/g dm, respectively. A total of sixteen phenolic compounds belonging to phenolic acids and flavonoids were detected. Furthermore, the extract showed strong antioxidant activity, and displayed a bacteriostatic effect against Escherichia coli and Salmonella typhimuriumn, and a bactericidal effect against Staphylococcus aureus and Listeria monocytogenes. Therefore, this study reveals that Origanum compactum extracts display potential as antibacterial and natural antioxidant agents for fighting against pathogenic bacteria and preventing oxidative stress. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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16 pages, 5482 KiB

Open AccessArticle

In Silico and In Vitro Studies of Alchemilla viridiflora Rothm—Polyphenols’ Potential for Inhibition of SARS-CoV-2 Internalization

by Relja Suručić, Jelena Radović Selgrad, Tatjana Kundaković-Vasović, Biljana Lazović, Maja Travar, Ljiljana Suručić and Ranko Škrbić

Molecules 2022, 27(16), 5174; https://doi.org/10.3390/molecules27165174 - 14 Aug 2022

Cited by 5 | Viewed by 2013

Abstract

Since the outbreak of the COVID-19 pandemic, it has been obvious that virus infection poses a serious threat to human health on a global scale. Certain plants, particularly those rich in polyphenols, have been found to be effective antiviral agents. The effectiveness of [...] Read more.

Since the outbreak of the COVID-19 pandemic, it has been obvious that virus infection poses a serious threat to human health on a global scale. Certain plants, particularly those rich in polyphenols, have been found to be effective antiviral agents. The effectiveness of Alchemilla viridiflora Rothm. (Rosaceae) methanol extract to prevent contact between virus spike (S)-glycoprotein and angiotensin-converting enzyme 2 (ACE2) and neuropilin-1 (NRP1) receptors was investigated. In vitro results revealed that the tested samples inhibited 50% of virus-receptor binding interactions in doses of 0.18 and 0.22 mg/mL for NRP1 and ACE2, respectively. Molecular docking studies revealed that the compounds from A. viridiflora ellagitannins class had a higher affinity for binding with S-glycoprotein whilst flavonoid compounds more significantly interacted with the NRP1 receptor. Quercetin 3-(6″-ferulylglucoside) and pentagalloylglucose were two compounds with the highest exhibited interfering potential for selected target receptors, with binding energies of −8.035 (S-glycoprotein) and −7.685 kcal/mol (NRP1), respectively. Furthermore, computational studies on other SARS-CoV-2 strains resulting from mutations in the original wild strain (V483A, N501Y-K417N-E484K, N501Y, N439K, L452R-T478K, K417N, G476S, F456L, E484K) revealed that virus internalization activity was maintained, but with different single compound contributions. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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23 pages, 2495 KiB

Open AccessArticle

Anti-Obesity Evaluation of Averrhoa carambola L. Leaves and Assessment of Its Polyphenols as Potential α-Glucosidase Inhibitors

by Nehal S. Ramadan, Nabil H. El-Sayed, Sayed A. El-Toumy, Doha Abdou Mohamed, Zeinab Abdel Aziz, Mohamed Sobhy Marzouk, Tuba Esatbeyoglu, Mohamed A. Farag and Kuniyoshi Shimizu

Molecules 2022, 27(16), 5159; https://doi.org/10.3390/molecules27165159 - 12 Aug 2022

Cited by 10 | Viewed by 2972

Abstract

Averrhoa carambola L. is reported for its anti-obese and anti-diabetic activities. The present study aimed to investigate its aqueous methanol leaf extract (CLL) in vivo anti-obese activity along with the isolation and identification of bioactive compounds and their in vitro α-glucosidase inhibition assessment. [...] Read more.

Averrhoa carambola L. is reported for its anti-obese and anti-diabetic activities. The present study aimed to investigate its aqueous methanol leaf extract (CLL) in vivo anti-obese activity along with the isolation and identification of bioactive compounds and their in vitro α-glucosidase inhibition assessment. CLL improved all obesity complications and exhibited significant activity in an obese rat model. Fourteen compounds, including four flavone glycosides (1–4) and ten dihydrochalcone glycosides (5–12), were isolated and identified using spectroscopic techniques. New compounds identified in planta included (1) apigenin 6-C-(2-deoxy-β-D-galactopyranoside)-7-O-β-D-quinovopyranoside, (8) phloretin 3′-C-(2-O-(E)-cinnamoyl-3-O-β-D-fucopyranosyl-4-O-acetyl)-β-D-fucopyranosyl-6′-O-β-D fucopyranosyl-(1/2)-α-L arabinofuranoside, (11a) phloretin3′-C-(2-O-(E)-p-coumaroyl-3-O-β-D-fucosyl-4-O-acetyl)-β-D-fucosyl-6′-O-(2-O-β-D-fucosyl)-α-L-arabinofuranoside, (11b) phloretin3′-C-(2-O-(Z)-p-coumaroyl-3-O-β-D-fucosyl-4-O-acetyl)-β-D-fucosyl-6′-O-(2-O-β-D-fucosyl)-α-L-arabinofuranoside. Carambolaside M (5), carambolaside Ia (6), carambolaside J (7), carambolaside I (9), carambolaside P (10a), carambolaside O (10b), and carambolaside Q (12), which are reported for the first time from A. carambola L. leaves, whereas luteolin 6-C-α-L-rhamnopyranosyl-(1-2)-β-D-fucopyranoside (2), apigenin 6-C-β-D-galactopyranoside (3), and apigenin 6-C-α-L-rhamnopyranosyl-(1-2)-β-L-fucopyranoside (4) are isolated for the first time from Family. Oxalidaceae. In vitro α-glucosidase inhibitory activity revealed the potential efficacy of flavone glycosides, viz., 1, 2, 3, and 4 as antidiabetic agents. In contrast, dihydrochalcone glycosides (5–11) showed weak activity, except for compound 12, which showed relatively strong activity. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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12 pages, 1374 KiB

Open AccessArticle

Thermal Control Using Far-Infrared Irradiation for Producing Deglycosylated Bioactive Compounds from Korean Ginseng Leaves

by Shucheng Duan, Jia Rui Liu, Xin Wang, Xue Mei Sun, Han Sheng Gong, Cheng Wu Jin and Seok Hyun Eom

Molecules 2022, 27(15), 4782; https://doi.org/10.3390/molecules27154782 - 26 Jul 2022

Cited by 3 | Viewed by 1855

Abstract

Although ginseng leaf is a good source of health-beneficial phytochemicals, such as polyphenols and ginsenosides, few studies have focused on the variation in compounds and bioactivities during leaf thermal processing. The efficiency of far-infrared irradiation (FIR) between 160 °C and 200 °C on [...] Read more.

Although ginseng leaf is a good source of health-beneficial phytochemicals, such as polyphenols and ginsenosides, few studies have focused on the variation in compounds and bioactivities during leaf thermal processing. The efficiency of far-infrared irradiation (FIR) between 160 °C and 200 °C on the deglycosylation of bioactive compounds in ginseng leaves was analyzed. FIR treatment significantly increased the total polyphenol content (TPC) and kaempferol production from panasenoside conversion. The highest content or conversion ratio was observed at 180 °C (FIR-180). Major ginsenoside contents gradually decreased as the FIR temperature increased, while minor ginsenoside contents significantly increased. FIR exhibited high efficiency to produce dehydrated minor ginsenosides, of which F4, Rg6, Rh4, Rk3, Rk1, and Rg5 increased to their highest levels at FIR-190, by 278-, 149-, 176-, 275-, 64-, and 81-fold, respectively. Moreover, significantly increased antioxidant activities were also observed in FIR-treated leaves, particularly FIR-180, mainly due to the breakage of phenolic polymers to release antioxidants. These results suggest that FIR treatment is a rapid and efficient processing method for producing various health-beneficial bioactive compounds from ginseng leaves. After 30 min of treatment without leaf burning, FIR-190 was the optimum temperature for producing minor ginsenosides, whereas FIR-180 was the optimum temperature for producing polyphenols and kaempferol. In addition, the results suggested that the antioxidant benefits of ginseng leaves are mainly due to polyphenols rather than ginsenosides. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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18 pages, 1761 KiB

Open AccessArticle

Protective Effect of Resveratrol against Hexavalent Chromium-Induced Genotoxic Damage in Hsd:ICR Male Mice

by Tonancy Nicolás-Méndez, Sam Kacew, Alda Rocío Ortiz-Muñiz, Víctor Manuel Mendoza-Núñez and María del Carmen García-Rodríguez

Molecules 2022, 27(13), 4028; https://doi.org/10.3390/molecules27134028 - 23 Jun 2022

Cited by 4 | Viewed by 2115

Abstract

The aim of this study is to examine the ability of resveratrol to counteract hexavalent chromium [Cr(VI)]-induced genetic damage, as well as the possible pathways associated with this protection. Hsd:ICR male mice are divided into groups of the following five individuals each: (a) [...] Read more.

The aim of this study is to examine the ability of resveratrol to counteract hexavalent chromium [Cr(VI)]-induced genetic damage, as well as the possible pathways associated with this protection. Hsd:ICR male mice are divided into groups of the following five individuals each: (a) control 1, distilled water; (b) control 2, ethanol 30%; (c) resveratrol, 50 mg/kg by gavage; (d) CrO₃, 20 mg/kg intraperitoneally; (e) resveratrol + CrO₃, resveratrol administered 4 h prior to CrO₃. The assessment is performed on peripheral blood. Micronuclei (MN) kinetics are measured from 0 to 72 h, while 8-hydroxydeoxyguanosine (8-OHdG) adduct repair levels, endogenous antioxidant system biomarkers, and apoptosis frequency were quantified after 48 h. Resveratrol reduces the frequency of Cr(VI)-induced MN and shows significant effects on the 8-OHdG adduct levels, suggesting that cell repair could be enhanced by this polyphenol. Concomitant administration of resveratrol and Cr(VI) results in a return of the activities of glutathione peroxidase and catalase to control levels, accompanied by modifications of superoxide dismutase activity and glutathione levels. Thus, antioxidant properties might play an important role in resveratrol-mediated inhibition of Cr(VI)-induced oxidant genotoxicity. The increase in apoptotic cells and the decrease in necrosis further confirmed that resveratrol effectively blocks the actions of Cr(VI). Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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17 pages, 2266 KiB

Open AccessArticle

Determination of the Phenolic Profile by Liquid Chromatography, Evaluation of Antioxidant Activity and Toxicity of Moroccan Erica multiflora, Erica scoparia, and Calluna vulgaris (Ericaceae)

by Douaa Bekkai, Yassine Oulad El Majdoub, Hamid Bekkai, Francesco Cacciola, Natalizia Miceli, Maria Fernanda Taviano, Emilia Cavò, Tomader Errabii, Roberto Laganà Vinci, Luigi Mondello and Mohammed L’Bachir El Kbiach

Molecules 2022, 27(13), 3979; https://doi.org/10.3390/molecules27133979 - 21 Jun 2022

Cited by 6 | Viewed by 2381

Abstract

This study aimed to investigate the phenolic profile and selected biological activities of the leaf and aerial extracts of three Ericaceae species, namely Erica multiflora, Erica scoparia, and Calluna vulgaris, collected from three different places in the north of Morocco. [...] Read more.

This study aimed to investigate the phenolic profile and selected biological activities of the leaf and aerial extracts of three Ericaceae species, namely Erica multiflora, Erica scoparia, and Calluna vulgaris, collected from three different places in the north of Morocco. The phenolic composition of all extracts was determined by LC coupled with photodiode array and mass spectrometry detection. Among the investigated extracts, that of E. scoparia aerial parts was the richest one, with a total amount of polyphenols of 9528.93 mg/kg. Up to 59 phenolic compounds were detected: 52 were positively identified and 49 quantified—11 in C. vulgaris, 14 in E. multiflora, and 24 in E. scoparia. In terms of chemical classes, nine were phenolic acids and 43 were flavonoids, and among them, the majority belonged to the class of flavonols. The antioxidant activity of all extracts was investigated by three different in vitro methods, namely DPPH, reducing power, and Fe²⁺ chelating assays; E. scoparia aerial part extract was the most active, with an IC₅₀ of 0.142 ± 0.014 mg/mL (DPPH test) and 1.898 ± 0.056 ASE/mL (reducing power assay). Further, all extracts were non-toxic against Artemia salina, thus indicating their potential safety. The findings attained in this work for such Moroccan Ericaceae species, never investigated so far, bring novelty to the field and show them to be valuable sources of phenolic compounds with interesting primary antioxidant properties. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 2707 KiB

Open AccessArticle

Transcriptome Profiling of HCT-116 Colorectal Cancer Cells with RNA Sequencing Reveals Novel Targets for Polyphenol Nano Curcumin

by Hewa Jalal Azeez, Francesco Neri, Mohammad Ali Hosseinpour Feizi and Esmaeil Babaei

Molecules 2022, 27(11), 3470; https://doi.org/10.3390/molecules27113470 - 27 May 2022

Cited by 5 | Viewed by 2966

Abstract

Colorectal cancer is one of the leading causes of cancer-related deaths worldwide. The gemini nanoparticle formulation of polyphenolic curcumin significantly inhibits the viability of cancer cells. However, the molecular mechanisms and pathways underlying its toxicity in colon cancer are unclear. Here, we aimed [...] Read more.

Colorectal cancer is one of the leading causes of cancer-related deaths worldwide. The gemini nanoparticle formulation of polyphenolic curcumin significantly inhibits the viability of cancer cells. However, the molecular mechanisms and pathways underlying its toxicity in colon cancer are unclear. Here, we aimed to uncover the possible novel targets of gemini curcumin (Gemini-Cur) on colorectal cancer and related cellular pathways. After confirming the cytotoxic effect of Gemini-Cur by MTT and apoptotic assays, RNA sequencing was employed to identify differentially expressed genes (DEGs) in HCT-116 cells. On a total of 3892 DEGs (padj < 0.01), 442 genes showed a log2 FC >|2| (including 244 upregulated and 198 downregulated). Gene ontology (GO) enrichment analysis was performed. Protein–protein interaction (PPI) and gene-pathway networks were constructed by using STRING and Cytoscape. The pathway analysis showed that Gemini-Cur predominantly modulates pathways related to the cell cycle. The gene network analysis revealed five central genes, namely GADD45G, ATF3, BUB1B, CCNA2 and CDK1. Real-time PCR and Western blotting analysis confirmed the significant modulation of these genes in Gemini-Cur-treated compared to non-treated cells. In conclusion, RNA sequencing revealed novel potential targets of curcumin on cancer cells. Further studies are required to elucidate the molecular mechanism of action of Gemini-Cur regarding the modulation of the expression of hub genes. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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13 pages, 1906 KiB

Open AccessArticle

Anti-Inflammatory Effects of Mitrephora sirikitiae Leaf Extract and Isolated Lignans in RAW 264.7 Cells

by Supachoke Mangmool, Chayaporn Limpichai, Khine Kyi Han, Vichai Reutrakul and Natthinee Anantachoke

Molecules 2022, 27(10), 3313; https://doi.org/10.3390/molecules27103313 - 21 May 2022

Cited by 5 | Viewed by 2514

Abstract

Mitrephora sirikitiae Weeras., Chalermglin & R.M.K. Saunders has been reported as a rich source of lignans that contribute to biological activities and health benefits. However, cellular anti-inflammatory effects of M. sirikitiae leaves and their lignan compounds have not been fully elucidated. Therefore, this [...] Read more.

Mitrephora sirikitiae Weeras., Chalermglin & R.M.K. Saunders has been reported as a rich source of lignans that contribute to biological activities and health benefits. However, cellular anti-inflammatory effects of M. sirikitiae leaves and their lignan compounds have not been fully elucidated. Therefore, this study aimed to investigate the anti-inflammatory activities of methanol extract of M. sirikitiae leaves and their lignan constituents on lipopolysaccharide (LPS)-induced inflammation in RAW 264.7 mouse macrophage cells. Treatment of RAW 264.7 cells with the methanol extract of M. sirikitiae leaves and its isolated lignans, including (−)-phylligenin (2) and 3′,4-O-dimethylcedrusin (6) significantly decreased LPS-induced prostaglandin E₂ (PGE₂) and nitric oxide (NO) productions. These inhibitory effects of the extract and isolated lignans on LPS-induced upregulation of PGE₂ and NO productions were derived from the suppression of cyclooxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS) production, respectively. In addition, treatment with 2-(3,4-dimethoxyphenyl)-6-(3,5-dimethoxyphenyl)-3,7-dioxabicyclo[3.3.0]octane (3) and mitrephoran (5) was able to suppress LPS-induced tumor necrosis factor alpha (TNF-α) secretion and synthesis in RAW 264.7 cells. These results demonstrated that M. sirikitiae leaves and some isolated lignans exhibited potent anti-inflammatory activity through the inhibition of secretion and synthesis of PGE₂, NO, and TNF-α. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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13 pages, 2222 KiB

Open AccessArticle

Mucuna pruriens Seed Aqueous Extract Improved Neuroprotective and Acetylcholinesterase Inhibitory Effects Compared with Synthetic L-Dopa

by Narisa Kamkaen, Chuda Chittasupho, Suwanna Vorarat, Sarin Tadtong, Watoo Phrompittayarat, Siriporn Okonogi and Pakakrong Kwankhao

Molecules 2022, 27(10), 3131; https://doi.org/10.3390/molecules27103131 - 13 May 2022

Cited by 11 | Viewed by 7164

Abstract

L-dopa, a dopaminergic agonist, is the gold standard for the treatment of Parkinson’s disease. However, due to the long-term toxicity and adverse effects of using L-dopa as the first-line therapy for Parkinson’s disease, a search for alternative medications is an important current challenge. [...] Read more.

L-dopa, a dopaminergic agonist, is the gold standard for the treatment of Parkinson’s disease. However, due to the long-term toxicity and adverse effects of using L-dopa as the first-line therapy for Parkinson’s disease, a search for alternative medications is an important current challenge. Traditional Ayurvedic medicine has suggested the use of Mucuna pruriens Linn. (Fabaceae) as an anti-Parkinson’s agent. The present study aimed to quantify the amount of L-dopa in M. pruriens seed extract by HPLC analysis. The cytotoxicity and neuroprotective properties of M. pruriens aqueous extract were investigated by two in vitro models including the serum deprivation method and co-administration of hydrogen peroxide assay. The results showed the significant neuroprotective activities of M. pruriens seed extracts at a concentration of 10 ng/mL. In addition, the effects of L-dopa and M. pruriens seed extract on in vitro acetylcholinesterase activities were studied. M. pruriens seed extract demonstrated acetylcholinesterase inhibitory activity, while synthetic L-dopa enhanced the activity of the enzyme. It can be concluded that the administration of M. pruriens seed might be effective in protecting the brain against neurodegenerative disorders such as Parkinson’s and Alzheimer’s diseases. M. prurience seed extract containing L-dopa has shown less acetylcholinesterase activity stimulation compared with L-dopa, suggesting that the extract might have a superior benefit for use in the treatment of Parkinson’s disease. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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10 pages, 2412 KiB

Open AccessArticle

Nanoformulation of Polyphenol Curcumin Enhances Cisplatin-Induced Apoptosis in Drug-Resistant MDA-MB-231 Breast Cancer Cells

by Parastoo Karami, Goran Othman, Zjwan Housein, Abbas Salihi, Mohammad Ali Hosseinpour Feizi, Hewa Jalal Azeez and Esmaeil Babaei

Molecules 2022, 27(9), 2917; https://doi.org/10.3390/molecules27092917 - 3 May 2022

Cited by 11 | Viewed by 3034

Abstract

Triple Negative Breast Cancer (TNBC) is the aggressive and lethal type of breast malignancy that develops resistance to current therapies. Combination therapy has proven to be an effective strategy on TNBC. We aimed to study whether the nano-formulation of polyphenolic curcumin (Gemini-Cur) would [...] Read more.

Triple Negative Breast Cancer (TNBC) is the aggressive and lethal type of breast malignancy that develops resistance to current therapies. Combination therapy has proven to be an effective strategy on TNBC. We aimed to study whether the nano-formulation of polyphenolic curcumin (Gemini-Cur) would affect the cisplatin-induced toxicity in MDA-MB-231 breast cancer cells. MDA-MB-231 cells were treated with Gemini-Cur, cisplatin and combination of Gemini-Cur/Cisplatin in a time- and dose-dependent manner. Cell viability was studied by using MTT, fluorescence microscopy and cell cycle assays. The mode of death was also determined by Hoechst staining and annexin V-FITC. Real-time PCR and western blotting were employed to detect the expression of BAX and BCL-2 genes. Our data demonstrated that Gemini-Cur significantly sensitizes cancer cells to cisplatin (combination index ≤ 1) and decreases IC50 values in comparison with Gemini-cur or cisplatin. Further studies confirmed that Gemini-Cur/Cisplatin suppresses cancer cell growth through induction of apoptosis (p < 0.001). In conclusion, the data confirm the synergistic effect of polyphenolic curcumin on cisplatin toxicity and provide attractive strategy to attain its apoptotic effect on TNBC. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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Review

Jump to: Research

16 pages, 545 KiB

Open AccessReview

Edible Insects an Alternative Nutritional Source of Bioactive Compounds: A Review

by Donatella Aiello, Marcella Barbera, David Bongiorno, Matteo Cammarata, Valentina Censi, Serena Indelicato, Fabio Mazzotti, Anna Napoli, Daniela Piazzese and Filippo Saiano

Molecules 2023, 28(2), 699; https://doi.org/10.3390/molecules28020699 - 10 Jan 2023

Cited by 24 | Viewed by 4984

Abstract

Edible insects have the potential to become one of the major future foods. In fact, they can be considered cheap, highly nutritious, and healthy food sources. International agencies, such as the Food and Agriculture Organization (FAO), have focused their attention on the consumption [...] Read more.

Edible insects have the potential to become one of the major future foods. In fact, they can be considered cheap, highly nutritious, and healthy food sources. International agencies, such as the Food and Agriculture Organization (FAO), have focused their attention on the consumption of edible insects, in particular, regarding their nutritional value and possible biological, toxicological, and allergenic risks, wishing the development of analytical methods to verify the authenticity, quality, and safety of insect-based products. Edible insects are rich in proteins, fats, fiber, vitamins, and minerals but also seem to contain large amounts of polyphenols able to have a key role in specific bioactivities. Therefore, this review is an overview of the potential of edible insects as a source of bioactive compounds, such as polyphenols, that can be a function of diet but also related to insect chemical defense. Currently, insect phenolic compounds have mostly been assayed for their antioxidant bioactivity; however, they also exert other activities, such as anti-inflammatory and anticancer activity, antityrosinase, antigenotoxic, and pancreatic lipase inhibitory activities. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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21 pages, 1760 KiB

Open AccessReview

Treatment of High-Polyphenol-Content Waters Using Biotechnological Approaches: The Latest Update

by Barbara Muñoz-Palazon, Susanna Gorrasi, Aurora Rosa-Masegosa, Marcella Pasqualetti, Martina Braconcini and Massimiliano Fenice

Molecules 2023, 28(1), 314; https://doi.org/10.3390/molecules28010314 - 30 Dec 2022

Cited by 5 | Viewed by 2971

Abstract

Polyphenols and their intermediate metabolites are natural compounds that are spread worldwide. Polyphenols are antioxidant agents beneficial for human health, but exposure to some of these compounds can be harmful to humans and the environment. A number of industries produce and discharge polyphenols [...] Read more.

Polyphenols and their intermediate metabolites are natural compounds that are spread worldwide. Polyphenols are antioxidant agents beneficial for human health, but exposure to some of these compounds can be harmful to humans and the environment. A number of industries produce and discharge polyphenols in water effluents. These emissions pose serious environmental issues, causing the pollution of surface or groundwater (which are used to provide drinking water) or harming wildlife in the receiving ecosystems. The treatment of high-polyphenol-content waters is mandatory for many industries. Nowadays, biotechnological approaches are gaining relevance for their low footprint, high efficiency, low cost, and versatility in pollutant removal. Biotreatments exploit the diversity of microbial metabolisms in relation to the different characteristics of the polluted water, modifying the design and the operational conditions of the technologies. Microbial metabolic features have been used for full or partial polyphenol degradation since several decades ago. Nowadays, the comprehensive use of biotreatments combined with physical-chemical treatments has enhanced the removal rates to provide safe and high-quality effluents. In this review, the evolution of the biotechnological processes for treating high-polyphenol-content water is described. A particular emphasis is given to providing a general concept, indicating which bioprocess might be adopted considering the water composition and the economic/environmental requirements. The use of effective technologies for environmental phenol removal could help in reducing/avoiding the detrimental effects of these chemicals. In addition, some of them could be employed for the recovery of beneficial ones. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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14 pages, 1496 KiB

Open AccessReview

Dihydrochalcones in Sweet Tea: Biosynthesis, Distribution and Neuroprotection Function

by Yong-Kang Wang, Si-Yi Hu, Feng-Yi Xiao, Zhan-Bo Dong, Jian-Hui Ye, Xin-Qiang Zheng, Yue-Rong Liang and Jian-Liang Lu

Molecules 2022, 27(24), 8794; https://doi.org/10.3390/molecules27248794 - 12 Dec 2022

Cited by 8 | Viewed by 2480

Abstract

Sweet tea is a popular herbal drink in southwest China, and it is usually made from the shoots and tender leaves of Lithocarpus litseifolius. The sweet taste is mainly attributed to its high concentration of dihydrochalcones. The distribution and biosynthesis of dihydrochaldones in [...] Read more.

Sweet tea is a popular herbal drink in southwest China, and it is usually made from the shoots and tender leaves of Lithocarpus litseifolius. The sweet taste is mainly attributed to its high concentration of dihydrochalcones. The distribution and biosynthesis of dihydrochaldones in sweet tea, as well as neuroprotective effects in vitro and in vivo tests, are reviewed in this paper. Dihydrochalones are mainly composed of phloretin and its glycosides, namely, trilobatin and phloridzin, and enriched in tender leaves with significant geographical specificity. Biosynthesis of the dihydrochalones follows part of the phenylpropanoid and a branch of flavonoid metabolic pathways and is regulated by expression of the genes, including phenylalanine ammonia-lyase, 4-coumarate: coenzyme A ligase, trans-cinnamic acid-4-hydroxylase and hydroxycinnamoyl-CoA double bond reductase. The dihydrochalones have been proven to exert a significant neuroprotective effect through their regulation against Aβ deposition, tau protein hyperphosphorylation, oxidative stress, inflammation and apoptosis. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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21 pages, 1441 KiB

Open AccessReview

Recent Advances in Natural Polyphenol Research

by Irene Dini and Lucia Grumetto

Molecules 2022, 27(24), 8777; https://doi.org/10.3390/molecules27248777 - 11 Dec 2022

Cited by 49 | Viewed by 5988

Abstract

Polyphenols are secondary metabolites produced by plants, which contribute to the plant’s defense against abiotic stress conditions (e.g., UV radiation and precipitation), the aggression of herbivores, and plant pathogens. Epidemiological studies suggest that long-term consumption of plant polyphenols protects against cardiovascular disease, cancer, [...] Read more.

Polyphenols are secondary metabolites produced by plants, which contribute to the plant’s defense against abiotic stress conditions (e.g., UV radiation and precipitation), the aggression of herbivores, and plant pathogens. Epidemiological studies suggest that long-term consumption of plant polyphenols protects against cardiovascular disease, cancer, osteoporosis, diabetes, and neurodegenerative diseases. Their structural diversity has fascinated and confronted analytical chemists on how to carry out unambiguous identification, exhaustive recovery from plants and organic waste, and define their nutritional and biological potential. The food, cosmetic, and pharmaceutical industries employ polyphenols from fruits and vegetables to produce additives, additional foods, and supplements. In some cases, nanocarriers have been used to protect polyphenols during food processing, to solve the issues related to low water solubility, to transport them to the site of action, and improve their bioavailability. This review summarizes the structure-bioactivity relationships, processing parameters that impact polyphenol stability and bioavailability, the research progress in nanocarrier delivery, and the most innovative methodologies for the exhaustive recovery of polyphenols from plant and agri-waste materials. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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22 pages, 1974 KiB

Open AccessReview

Natural Polyphenol Recovery from Apple-, Cereal-, and Tomato-Processing By-Products and Related Health-Promoting Properties

by Katalin Szabo, Laura Mitrea, Lavinia Florina Călinoiu, Bernadette-Emőke Teleky, Gheorghe Adrian Martău, Diana Plamada, Mihaela Stefana Pascuta, Silvia-Amalia Nemeş, Rodica-Anita Varvara and Dan Cristian Vodnar

Molecules 2022, 27(22), 7977; https://doi.org/10.3390/molecules27227977 - 17 Nov 2022

Cited by 40 | Viewed by 4405

Abstract

Polyphenols of plant origin are a broad family of secondary metabolites that range from basic phenolic acids to more complex compounds such as stilbenes, flavonoids, and tannins, all of which have several phenol units in their structure. Considerable health benefits, such as having [...] Read more.

Polyphenols of plant origin are a broad family of secondary metabolites that range from basic phenolic acids to more complex compounds such as stilbenes, flavonoids, and tannins, all of which have several phenol units in their structure. Considerable health benefits, such as having prebiotic potential and cardio-protective and weight control effects, have been linked to diets based on polyphenol-enriched foods and plant-based products, indicating the potential role of these substances in the prevention or treatment of numerous pathologies. The most representative phenolic compounds in apple pomace are phloridzin, chlorogenic acid, and epicatechin, with major health implications in diabetes, cancer, and cardiovascular and neurocognitive diseases. The cereal byproducts are rich in flavonoids (cyanidin 3-glucoside) and phenolic acids (ferulic acid), all with significant results in reducing the incidence of noncommunicable diseases. Quercetin, naringenin, and rutin are the predominant phenolic molecules in tomato by-products, having important antioxidant and antimicrobial activities. The present understanding of the functionality of polyphenols in health outcomes, specifically, noncommunicable illnesses, is summarized in this review, focusing on the applicability of this evidence in three extensive agrifood industries (apple, cereal, and tomato processing). Moreover, the reintegration of by-products into the food chain via functional food products and personalized nutrition (e.g., 3D food printing) is detailed, supporting a novel direction to be explored within the circular economy concept. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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19 pages, 4516 KiB

Open AccessReview

Overview of the Polyphenols in Salicornia: From Recovery to Health-Promoting Effect

by Francesco Limongelli, Pasquale Crupi, Maria Lisa Clodoveo, Filomena Corbo and Marilena Muraglia

Molecules 2022, 27(22), 7954; https://doi.org/10.3390/molecules27227954 - 17 Nov 2022

Cited by 15 | Viewed by 3125

Abstract

Nowadays, there has been considerable attention paid toward the recovery of waste plant matrices as possible sources of functional compounds with healthy properties. In this regard, we focus our attention on Salicornia, a halophyte plant that grows abundantly on the coasts of the [...] Read more.

Nowadays, there has been considerable attention paid toward the recovery of waste plant matrices as possible sources of functional compounds with healthy properties. In this regard, we focus our attention on Salicornia, a halophyte plant that grows abundantly on the coasts of the Mediterranean area. Salicornia is used not only as a seasoned vegetable but also in traditional medicine for its beneficial effects in protecting against diseases such as obesity, diabetes, and cancer. In numerous research studies, Salicornia consumption has been highly suggested due to its high level of bioactive molecules, among which, polyphenols are prevalent. The antioxidant and antiradical activity of polyphenols makes Salicornia a functional food candidate with potential beneficial activities for human health. Therefore, this review provides specific and compiled information for optimizing and developing new extraction processes for the recovery of bioactive compounds from Salicornia; focusing particular attention on polyphenols and their health benefits. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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13 pages, 1467 KiB

Open AccessReview

Effects of Natural Polyphenols on Skin and Hair Health: A Review

by Mang Sun, Ya Deng, Xining Cao, Lu Xiao, Qian Ding, Fuqing Luo, Peng Huang, Yuanyuan Gao, Mengqi Liu and Hengguang Zhao

Molecules 2022, 27(22), 7832; https://doi.org/10.3390/molecules27227832 - 14 Nov 2022

Cited by 23 | Viewed by 7847

Abstract

The skin is the largest organ of the body and plays multiple essential roles, ranging from regulating temperature, preventing infections, to ultimately affecting human health. A hair follicle is a complex cutaneous appendage. Skin diseases and hair loss have a significant effect on [...] Read more.

The skin is the largest organ of the body and plays multiple essential roles, ranging from regulating temperature, preventing infections, to ultimately affecting human health. A hair follicle is a complex cutaneous appendage. Skin diseases and hair loss have a significant effect on the quality of life and psychosocial adjustment of individuals. However, the available traditional drugs for treating skin and hair diseases may have some insufficiencies; therefore, a growing number of researchers are interested in natural materials that could achieve satisfactory results and minimize adverse effects. Natural polyphenols, named for the multiple phenolic hydroxyl groups in their structures, are promising candidates and continue to be of scientific interest due to their multifunctional biological properties and safety. Polyphenols have a wide range of pharmacological effects. In addition to the most common effect, antioxidation, polyphenols have anti-inflammatory, bacteriostatic, antitumor, and other biological effects associated with reduced risk of a number of chronic diseases. Various polyphenols have also shown efficacy against different types of skin and hair diseases, both in vitro and in vivo, via different mechanisms. Thus, this paper reviews the research progress in natural polyphenols for the protection of skin and hair health, especially focusing on their potential therapeutic mechanisms against skin and hair disorders. A deep understanding of natural polyphenols provides a new perspective for the safe treatment of skin diseases and hair loss. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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18 pages, 1875 KiB

Open AccessReview

Ferulic Acid: A Natural Phenol That Inhibits Neoplastic Events through Modulation of Oncogenic Signaling

by Hardeep Singh Tuli, Ajay Kumar, Seema Ramniwas, Renuka Coudhary, Diwakar Aggarwal, Manoj Kumar, Ujjawal Sharma, Nidarshana Chaturvedi Parashar, Shafiul Haque and Katrin Sak

Molecules 2022, 27(21), 7653; https://doi.org/10.3390/molecules27217653 - 7 Nov 2022

Cited by 28 | Viewed by 3856

Abstract

Despite the immense therapeutic advances in the field of health sciences, cancer is still to be found among the global leading causes of morbidity and mortality. Ethnomedicinally, natural bioactive compounds isolated from various plant sources have been used for the treatment of several [...] Read more.

Despite the immense therapeutic advances in the field of health sciences, cancer is still to be found among the global leading causes of morbidity and mortality. Ethnomedicinally, natural bioactive compounds isolated from various plant sources have been used for the treatment of several cancer types and have gained notable attention. Ferulic acid, a natural compound derived from various seeds, nuts, leaves, and fruits, exhibits a variety of pharmacological effects in cancer, including its proapoptotic, cell-cycle-arresting, anti-metastatic, and anti-inflammatory activities. This review study presents a thorough overview of the molecular targets and cellular signaling pathways modulated by ferulic acid in diverse malignancies, showing high potential for this phenolic acid to be developed as a candidate agent for novel anticancer therapeutics. In addition, current investigations to develop promising synergistic formulations are also discussed. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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22 pages, 2920 KiB

Open AccessReview

Uncovering the Anticancer Potential of Polydatin: A Mechanistic Insight

by Muhammad Ajmal Shah, Ayesha Hamid, Hafiza Ishmal Faheem, Azhar Rasul, Tourki A. S. Baokbah, Muhammad Haris, Rimsha Yousaf, Uzma Saleem, Shabnoor Iqbal, Maria Silvana Alves, Zahid Khan, Ghulam Hussain, Ifat Alsharfi, Haroon Khan and Philippe Jeandet

Molecules 2022, 27(21), 7175; https://doi.org/10.3390/molecules27217175 - 23 Oct 2022

Cited by 11 | Viewed by 3663

Abstract

Polydatin or 3-O-β-d-resveratrol-glucopyranoside (PD), a stilbenoid component of Polygonum cuspicadum (Polygonaceae), has a variety of biological roles. In traditional Chinese medicine, P. cuspicadum extracts are used for the treatment of infections, inflammation, and cardiovascular disorders. Polydatin possesses a broad [...] Read more.

Polydatin or 3-O-β-d-resveratrol-glucopyranoside (PD), a stilbenoid component of Polygonum cuspicadum (Polygonaceae), has a variety of biological roles. In traditional Chinese medicine, P. cuspicadum extracts are used for the treatment of infections, inflammation, and cardiovascular disorders. Polydatin possesses a broad range of biological activities including antioxidant, anti-inflammatory, anticancer, and hepatoprotective, neuroprotective, and immunostimulatory effects. Currently, a major proportion of the population is victimized with cervical lung cancer, ovarian cancer and breast cancer. PD has been recognized as a potent anticancer agent. PD could effectively inhibit the migration and proliferation of ovarian cancer cells, as well as the expression of the PI3K protein. The malignancy of lung cancer cells was reduced after PD treatments via targeting caspase 3, arresting cancer cells at the S phase and inhibiting NLRP3 inflammasome by downregulation of the NF-κB pathway. This ceases cell cycle, inhibits VEGF, and counteracts ROS in breast cancer. It also prevents cervical cancer by regulating epithelial-to-mesenchymal transition (EMT), apoptosis, and the C-Myc gene. The objective of this review is thus to unveil the polydatin anticancer potential for the treatment of various tumors, as well as to examine the mechanisms of action of this compound. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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28 pages, 608 KiB

Open AccessReview

Selected Plant-Derived Polyphenols as Potential Therapeutic Agents for Peripheral Artery Disease: Molecular Mechanisms, Efficacy and Safety

by Guglielmina Froldi and Eugenio Ragazzi

Molecules 2022, 27(20), 7110; https://doi.org/10.3390/molecules27207110 - 21 Oct 2022

Cited by 10 | Viewed by 2714

Abstract

Vascular diseases, such as peripheral artery disease (PAD), are associated with diabetes mellitus and a higher risk of cardiovascular disease and even death. Surgical revascularization and pharmacological treatments (mainly antiplatelet, lipid-lowering drugs, and antidiabetic agents) have some effectiveness, but the response and efficacy [...] Read more.

Vascular diseases, such as peripheral artery disease (PAD), are associated with diabetes mellitus and a higher risk of cardiovascular disease and even death. Surgical revascularization and pharmacological treatments (mainly antiplatelet, lipid-lowering drugs, and antidiabetic agents) have some effectiveness, but the response and efficacy of therapy are overly dependent on the patient’s conditions. Thus, the demand for new cures exists. In this regard, new studies on natural polyphenols that act on key points involved in the pathogenesis of vascular diseases and, thus, on PAD are of great urgency. The purpose of this review is to take into account the mechanisms that lead to endothelium dysfunction, such as the glycoxidation process and the production of advanced glycation end-products (AGEs) that result in protein misfolding, and to suggest plant-derived polyphenols that could be useful in PAD. Thus, five polyphenols are considered, baicalein, curcumin, mangiferin, quercetin and resveratrol, reviewing the literature in PubMed. The key molecular mechanisms and preclinical and clinical studies of each selected compound are examined. Furthermore, the safety profiles of the polyphenols are outlined, together with the unwanted effects reported in humans, also by searching the WHO database (VigiBase). Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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23 pages, 1026 KiB

Open AccessReview

Grape Pomace Polyphenols as a Source of Compounds for Management of Oxidative Stress and Inflammation—A Possible Alternative for Non-Steroidal Anti-Inflammatory Drugs?

by Veronica Sanda Chedea, Ștefan Octavian Macovei, Ioana Corina Bocșan, Dan Claudiu Măgureanu, Antonia Mihaela Levai, Anca Dana Buzoianu and Raluca Maria Pop

Molecules 2022, 27(20), 6826; https://doi.org/10.3390/molecules27206826 - 12 Oct 2022

Cited by 18 | Viewed by 3915

Abstract

Flavonoids, stilbenes, lignans, and phenolic acids, classes of polyphenols found in grape pomace (GP), were investigated as an important alternative source for active substances that could be used in the management of oxidative stress and inflammation. The benefic antioxidant and anti-inflammatory actions of [...] Read more.

Flavonoids, stilbenes, lignans, and phenolic acids, classes of polyphenols found in grape pomace (GP), were investigated as an important alternative source for active substances that could be used in the management of oxidative stress and inflammation. The benefic antioxidant and anti-inflammatory actions of GP are presented in the literature, but they are derived from a large variety of experimental in vitro and in vivo settings. In these in vitro works, the decrease in reactive oxygen species, malondialdehyde, and thiobarbituric acid reactive substances levels and the increase in glutathione levels show the antioxidant effects. The inhibition of nuclear factor kappa B and prostaglandin E2 inflammatory pathways and the decrease of some inflammatory markers such as interleukin-8 (IL-8) demonstrate the anti-inflammatory actions of GP polyphenols. The in vivo studies further confirmed the antioxidant (increase in catalase, superoxide dismutase and glutathione peroxidase levels and a stimulation of endothelial nitric oxide synthase -eNOS gene expression) and anti-inflammatory (inhibition of IL-1𝛼, IL-1β, IL-6, interferon-𝛾, TNF-α and C-reactive protein release) activities. Grape pomace as a whole extract, but also different individual polyphenols that are contained in GP can modulate the endogenous pathway responsible in reducing oxidative stress and chronic inflammation. The present review analyzed the effects of GP in oxidative stress and inflammation, suggesting that it could become a valuable therapeutic candidate capable to reduce the aforementioned pathological processes. Grape pomace extract could become an adjuvant treatment in the attempt to reduce the side effects of the classical anti-inflammatory medication like non-steroidal anti-inflammatory drugs (NSAIDs). Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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25 pages, 1373 KiB

Open AccessReview

Grape Polyphenols in the Treatment of Human Skeletal Muscle Damage Due to Inflammation and Oxidative Stress during Obesity and Aging: Early Outcomes and Promises

by Adriana Capozzi, Cédric Saucier, Catherine Bisbal and Karen Lambert

Molecules 2022, 27(19), 6594; https://doi.org/10.3390/molecules27196594 - 5 Oct 2022

Cited by 8 | Viewed by 3576

Abstract

Today, inactivity and high-calorie diets contribute to the development of obesity and premature aging. In addition, the population of elderly people is growing due to improvements in healthcare management. Obesity and aging are together key risk factors for non-communicable diseases associated with several [...] Read more.

Today, inactivity and high-calorie diets contribute to the development of obesity and premature aging. In addition, the population of elderly people is growing due to improvements in healthcare management. Obesity and aging are together key risk factors for non-communicable diseases associated with several co-morbidities and increased mortality, with a major impact on skeletal muscle defect and/or poor muscle mass quality. Skeletal muscles contribute to multiple body functions and play a vital role throughout the day, in all our activities. In our society, limiting skeletal muscle deterioration, frailty and dependence is not only a major public health challenge but also a major socio-economic issue. Specific diet supplementation with natural chemical compounds such as grape polyphenols had shown to play a relevant and direct role in regulating metabolic and molecular pathways involved in the prevention and treatment of obesity and aging and their related muscle comorbidities in cell culture and animal studies. However, clinical studies aiming to restore skeletal muscle mass and function with nutritional grape polyphenols supplementation are still very scarce. There is an urgent need for clinical studies to validate the very encouraging results observed in animal models. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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25 pages, 4383 KiB

Open AccessReview

Polyphenol-Rich Ginger (Zingiber officinale) for Iron Deficiency Anaemia and Other Clinical Entities Associated with Altered Iron Metabolism

by Soo Liang Ooi, Sok Cheon Pak, Ron Campbell and Arumugam Manoharan

Molecules 2022, 27(19), 6417; https://doi.org/10.3390/molecules27196417 - 28 Sep 2022

Cited by 6 | Viewed by 7150

Abstract

Ginger (Zingiber officinale) is rich in natural polyphenols and may potentially complement oral iron therapy in treating and preventing iron deficiency anaemia (IDA). This narrative review explores the benefits of ginger for IDA and other clinical entities associated with altered iron [...] Read more.

Ginger (Zingiber officinale) is rich in natural polyphenols and may potentially complement oral iron therapy in treating and preventing iron deficiency anaemia (IDA). This narrative review explores the benefits of ginger for IDA and other clinical entities associated with altered iron metabolism. Through in vivo, in vitro, and limited human studies, ginger supplementation was shown to enhance iron absorption and thus increase oral iron therapy’s efficacy. It also reduces oxidative stress and inflammation and thus protects against excess free iron. Ginger’s bioactive polyphenols are prebiotics to the gut microbiota, promoting gut health and reducing the unwanted side effects of iron tablets. Moreover, ginger polyphenols can enhance the effectiveness of erythropoiesis. In the case of iron overload due to comorbidities from chronic inflammatory disorders, ginger can potentially reverse the adverse impacts and restore iron balance. Ginger can also be used to synthesise nanoparticles sustainably to develop newer and more effective oral iron products and functional ingredients for IDA treatment and prevention. Further research is still needed to explore the applications of ginger polyphenols in iron balance and anaemic conditions. Specifically, long-term, well-designed, controlled trials are required to validate the effectiveness of ginger as an adjuvant treatment for IDA. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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27 pages, 2720 KiB

Open AccessReview

New Insights into Dietary Pterostilbene: Sources, Metabolism, and Health Promotion Effects

by Sanjushree Nagarajan, Sundhar Mohandas, Kumar Ganesan, Baojun Xu and Kunka Mohanram Ramkumar

Molecules 2022, 27(19), 6316; https://doi.org/10.3390/molecules27196316 - 25 Sep 2022

Cited by 53 | Viewed by 5471

Abstract

Pterostilbene (PTS), a compound most abundantly found in blueberries, is a natural analog of resveratrol. Several plant species, such as peanuts and grapes, produce PTS. While resveratrol has been extensively studied for its antioxidant properties, recent evidence also points out the diverse therapeutic [...] Read more.

Pterostilbene (PTS), a compound most abundantly found in blueberries, is a natural analog of resveratrol. Several plant species, such as peanuts and grapes, produce PTS. While resveratrol has been extensively studied for its antioxidant properties, recent evidence also points out the diverse therapeutic potential of PTS. Several studies have identified the robust pharmacodynamic features of PTS, including better intestinal absorption and elevated hepatic stability than resveratrol. Indeed, due to its higher bioavailability paired with reduced toxicity compared to other stilbenes, PTS has become an attractive drug candidate for the treatment of several disease conditions, including diabetes, cancer, cardiovascular disease, neurodegenerative disorders, and aging. This review article provides an extensive summary of the nutraceutical potential of PTS in various disease conditions while discussing the crucial mechanistic pathways implicated. In particular, we share insights from our studies about the Nrf2-mediated effect of PTS in diabetes and associated complications. Moreover, we elucidate the important sources of PTS and discuss in detail its pharmacokinetics and the range of formulations and routes of administration used across experimental studies and human clinical trials. Furthermore, this review also summarizes the strategies successfully used to improve dietary availability and the bio-accessibility of PTS. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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25 pages, 2624 KiB

Open AccessReview

A Comprehensive Literature Review on Cardioprotective Effects of Bioactive Compounds Present in Fruits of Aristotelia chilensis Stuntz (Maqui)

by Lyanne Rodríguez, Andrés Trostchansky, Hermine Vogel, Irene Wood, Iván Palomo, Sergio Wehinger and Eduardo Fuentes

Molecules 2022, 27(19), 6147; https://doi.org/10.3390/molecules27196147 - 20 Sep 2022

Cited by 6 | Viewed by 3052

Abstract

Some fruits and vegetables, rich in bioactive compounds such as polyphenols, flavonoids, and anthocyanins, may inhibit platelet activation pathways and therefore reduce the risk of suffering from CVD when consumed regularly. Aristotelia chilensis Stuntz (Maqui) is a shrub or tree native to Chile [...] Read more.

Some fruits and vegetables, rich in bioactive compounds such as polyphenols, flavonoids, and anthocyanins, may inhibit platelet activation pathways and therefore reduce the risk of suffering from CVD when consumed regularly. Aristotelia chilensis Stuntz (Maqui) is a shrub or tree native to Chile with outstanding antioxidant activity, associated with its high content in anthocyanins, polyphenols, and flavonoids. Previous studies reveal different pharmacological properties for this berry, but its cardioprotective potential has been little studied. Despite having an abundant composition, and being rich in bioactive products with an antiplatelet role, there are few studies linking this berry with antiplatelet activity. This review summarizes and discusses relevant information on the cardioprotective potential of Maqui, based on its composition of bioactive compounds, mainly as a nutraceutical antiplatelet agent. Articles published between 2000 and 2022 in the following bibliographic databases were selected: PubMed, ScienceDirect, and Google Scholar. Our search revealed that Maqui is a promising cardiovascular target since extracts from this berry have direct effects on the reduction in cardiovascular risk factors (glucose index, obesity, diabetes, among others). Although studies on antiplatelet activity in this fruit are recent, its rich chemical composition clearly shows that the presence of chemical compounds (anthocyanins, flavonoids, phenolic acids, among others) with high antiplatelet potential can provide this berry with antiplatelet properties. These bioactive compounds have antiplatelet effects with multiple targets in the platelet, particularly, they have been related to the inhibition of thromboxane, thrombin, ADP, and GPVI receptors, or through the pathways by which these receptors stimulate platelet aggregation. Detailed studies are needed to clarify this gap in the literature, as well as to specifically evaluate the mechanism of action of Maqui extracts, due to the presence of phenolic compounds. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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20 pages, 1195 KiB

Open AccessReview

Polysaccharides as Carriers of Polyphenols: Comparison of Freeze-Drying and Spray-Drying as Encapsulation Techniques

by Ivana Buljeta, Anita Pichler, Josip Šimunović and Mirela Kopjar

Molecules 2022, 27(16), 5069; https://doi.org/10.3390/molecules27165069 - 9 Aug 2022

Cited by 39 | Viewed by 5183

Abstract

Polyphenols have received great attention as important phytochemicals beneficial for human health. They have a protective effect against cardiovascular disease, obesity, cancer and diabetes. The utilization of polyphenols as natural antioxidants, functional ingredients and supplements is limited due to their low stability caused [...] Read more.

Polyphenols have received great attention as important phytochemicals beneficial for human health. They have a protective effect against cardiovascular disease, obesity, cancer and diabetes. The utilization of polyphenols as natural antioxidants, functional ingredients and supplements is limited due to their low stability caused by environmental and processing conditions, such as heat, light, oxygen, pH, enzymes and so forth. These disadvantages are overcome by the encapsulation of polyphenols by different methods in the presence of polyphenolic carriers. Different encapsulation technologies have been established with the purpose of decreasing polyphenol sensitivity and the creation of more efficient delivery systems. Among them, spray-drying and freeze-drying are the most common methods for polyphenol encapsulation. This review will provide an overview of scientific studies in which polyphenols from different sources were encapsulated using these two drying methods, as well as the impact of different polysaccharides used as carriers for encapsulation. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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17 pages, 1854 KiB

Open AccessReview

Phenolic Compounds’ Occurrence in Opuntia Species and Their Role in the Inflammatory Process: A Review

by Walid Zeghbib, Fares Boudjouan, Vitor Vasconcelos and Graciliana Lopes

Molecules 2022, 27(15), 4763; https://doi.org/10.3390/molecules27154763 - 25 Jul 2022

Cited by 26 | Viewed by 4398

Abstract

Within the Cactaceae family, Opuntia comprises the most widespread species, with a recognized importance in human life, including feeding, domestic use as home natural barriers, and as a traditional remedy for diverse diseases and conditions such asthma, edema, and burns. Indeed, scientific reports [...] Read more.

Within the Cactaceae family, Opuntia comprises the most widespread species, with a recognized importance in human life, including feeding, domestic use as home natural barriers, and as a traditional remedy for diverse diseases and conditions such asthma, edema, and burns. Indeed, scientific reports have stated that these health benefits may be due to various active compounds, particularly polyphenols, which are ubiquitously found in plants and have proven their pharmacological efficiency by displaying antimicrobial, anti-cancer, and anti-inflammatory activities, among others. Opuntia species contain different classes of phenolic compounds that are recognized for their anti-inflammatory potential. Among them, quercetin, isorhamnetin, and kaempferol derivates were reported to greatly contribute to modulate cells’ infiltration and secretion of soluble inflammatory mediators, with key implications in the inflammatory process. In this review, we make a summary of the different classes of phenolic compounds reported in Opuntia species so far and explore their implications in the inflammatory process, reported by in vitro and in vivo bioassays, supporting the use of cactus in folk medicine and valorizing them from the socio-economic point of view. Full article

(This article belongs to the Special Issue Natural Polyphenols in Human Health)

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