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18 pages, 2102 KiB

Open AccessArticle

Identification of Marker Compounds and In Vitro Toxicity Evaluation of Two Portuguese Asphodelus Leaf Extracts

by Maryam Malmir, Katelene Lima, Sérgio Póvoas Camões, Vera Manageiro, Maria Paula Duarte, Joana Paiva Miranda, Rita Serrano, Isabel Moreira da Silva, Beatriz Silva Lima, Manuela Caniça and Olga Silva

Molecules 2023, 28(5), 2372; https://doi.org/10.3390/molecules28052372 - 4 Mar 2023

Cited by 6 | Viewed by 2505

Abstract

The leaves of Asphodelus bento-rainhae subsp. bento-rainhae, an endemic Portuguese species, and Asphodelus macrocarpus subsp. macrocarpus have been used as food, and traditionally as medicine, for treating ulcers, urinary tract, and inflammatory disorders. The present study aims to establish the phytochemical profile of [...] Read more.

The leaves of Asphodelus bento-rainhae subsp. bento-rainhae, an endemic Portuguese species, and Asphodelus macrocarpus subsp. macrocarpus have been used as food, and traditionally as medicine, for treating ulcers, urinary tract, and inflammatory disorders. The present study aims to establish the phytochemical profile of the main secondary metabolites, together with the antimicrobial, antioxidant and toxicity assessments of both Asphodelus leaf 70% ethanol extracts. Phytochemical screenings were conducted by the TLC and LC-UV/DAD-ESI/MS chromatographic technique, and quantification of the leading chemical classes was performed by spectrophotometric methods. Liquid-liquid partitions of crude extracts were obtained using ethyl ether, ethyl acetate, and water. For in vitro evaluations of antimicrobial activity, the broth microdilution method, and for the antioxidant activity, the FRAP and DPPH methods were used. Genotoxicity and cytotoxicity were assessed by Ames and MTT tests, respectively. Twelve known compounds including neochlorogenic acid, chlorogenic acid, caffeic acid, isoorientin, p-coumaric acid, isovitexin, ferulic acid, luteolin, aloe-emodin, diosmetin, chrysophanol, and β-sitosterol were identified as the main marker compounds, and terpenoids and condensed tannins were found to be the major class of secondary metabolites of both medicinal plants. The ethyl ether fractions demonstrated the highest antibacterial activity against all the Gram-positive microorganisms, (MIC value of 62 to 1000 µg/mL), with aloe-emodin as one of the main marker compounds highly active against Staphylococcus epidermidis (MIC value of 0.8 to 1.6 µg/mL). Ethyl acetate fractions exhibited the highest antioxidant activity (IC₅₀ of 800 to 1200 µg/mL, respectively). No cytotoxicity (up to 1000 µg/mL) or genotoxicity/mutagenicity (up to 5 mg/plate, with/without metabolic activation) were detected. The obtained results contribute to the knowledge of the value and safety of the studied species as herbal medicines. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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16 pages, 1960 KiB

Open AccessArticle

Antimicrobial Activity of the Secondary Metabolites Isolated from a South African Red Seaweed, Laurencia corymbosa

by Jameel Fakee, John J. Bolton, Marilize Le Roes-Hill, Kim A. Durrell, Edith Antunes and Denzil R. Beukes

Molecules 2023, 28(5), 2063; https://doi.org/10.3390/molecules28052063 - 22 Feb 2023

Viewed by 2101

Abstract

South Africa’s highly diverse marine biota includes several endemic marine red algae of the Laurencia genus. Cryptic species and morphological variability make the taxonomy of Laurencia plant challenging, and a record of the secondary metabolites isolated from South African Laurencia spp. can be [...] Read more.

South Africa’s highly diverse marine biota includes several endemic marine red algae of the Laurencia genus. Cryptic species and morphological variability make the taxonomy of Laurencia plant challenging, and a record of the secondary metabolites isolated from South African Laurencia spp. can be used to assess their chemotaxonomic significance. In addition, the rapid development of resistance against antibiotics, coupled with the inherent ability of seaweeds to resist pathogenic infection, supported this first phycochemical investigation of Laurencia corymbosa J. Agardh. A new tricyclic keto-cuparane (7) and two new cuparanes (4, 5) were obtained alongside known acetogenins, halo-chamigranes, and additional cuparanes. These compounds were screened against Acinetobacter baumannii, Enterococcus faecalis, Escherichia coli, Staphylococcus aureus, and Candida albicans, with 4 exhibiting excellent activity against the Gram-negative A. baumanii (minimum inhibitory concentration (MIC) 1 μg/mL) strain. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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14 pages, 1276 KiB

Open AccessArticle

Ulvophyte Green Algae Caulerpa lentillifera: Metabolites Profile and Antioxidant, Anticancer, Anti-Obesity, and In Vitro Cytotoxicity Properties

by Fahrul Nurkolis, Nurpudji Astuti Taslim, Faqrizal Ria Qhabibi, Sojin Kang, Myunghan Moon, Jinwon Choi, Min Choi, Moon Nyeo Park, Nelly Mayulu and Bonglee Kim

Molecules 2023, 28(3), 1365; https://doi.org/10.3390/molecules28031365 - 31 Jan 2023

Cited by 27 | Viewed by 5726

Abstract

Marine algae have excellent bioresource properties with potential nutritional and bioactive therapeutic benefits, but studies regarding Caulerpa lentillifera are limited. This study aims to explore the metabolites profile and the antioxidant, anticancer, anti-obesity, and in vitro cytotoxicity properties of fractionated ethanolic extract of [...] Read more.

Marine algae have excellent bioresource properties with potential nutritional and bioactive therapeutic benefits, but studies regarding Caulerpa lentillifera are limited. This study aims to explore the metabolites profile and the antioxidant, anticancer, anti-obesity, and in vitro cytotoxicity properties of fractionated ethanolic extract of C. lentillifera using two maceration and soxhlet extraction methods. Dried simplicia of C. lentillifera was mashed and extracted in ethanol solvent, concentrated and evaporated, then sequentially partitioned with equal volumes of ethyl acetate and n-Hexane. Six samples were used in this study, consisting of ME (Maceration—Ethanol), MEA (Maceration—Ethyl Acetate), MH (Maceration—n-Hexane), SE (Soxhletation—Ethanol), SEA (Soxhletation—Ethyl Acetate), and SH (Soxhletation—n-Hexane). Non-targeted metabolomic profiling was determined using LC-HRMS, while antioxidant, anti-obesity, and anticancer cytotoxicity were determined using DPPH and ABTS, lipase inhibition, and MTT assay, respectively. This study demonstrates that C. lentillifera has several functional metabolites, antioxidant capacity (EC₅₀ MH is very close to EC₅₀ of Trolox), as well as anti-obesity properties (EC₅₀ MH < EC₅₀ orlistat, an inhibitor of lipid hydrolyzing enzymes), which are useful as precursors for new therapeutic approaches in improving obesity-related diseases. More interestingly, ME, MH, and SE are novel bioresource agents for anticancer drugs, especially for hepatoma, breast, colorectal, and leukemia cancers. Finally, C. lentillifera can be a nutraceutical with great therapeutic benefits. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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8 pages, 1073 KiB

Open AccessCommunication

Catechol-O-methyltransferase Inhibitors from Calendula officinalis Leaf

by Wataru Kadowaki, Ryo Miyata, Misa Fujinami, Yoshizumi Sato and Shigenori Kumazawa

Molecules 2023, 28(3), 1333; https://doi.org/10.3390/molecules28031333 - 30 Jan 2023

Cited by 2 | Viewed by 2354

Abstract

Calendula officinalis is commonly known as marigold and its flowers are used in herbal medicines, cosmetics, perfumes, dyes, pharmaceutical preparations, and food products. However, the utility of its leaves has not been studied in depth. The purpose of the present study was to [...] Read more.

Calendula officinalis is commonly known as marigold and its flowers are used in herbal medicines, cosmetics, perfumes, dyes, pharmaceutical preparations, and food products. However, the utility of its leaves has not been studied in depth. The purpose of the present study was to identify the major compounds in C. officinalis leaves and to determine the inhibitory properties of the isolated compounds toward human catechol-O-methyltransferase (COMT), a key neurotransmitter involved in Parkinson’s disease and depression. We isolated and identified ten compounds, including two phenylpropanoids and seven flavonoids, from C. officinalis leaf extracts, of which four flavonoids were identified from C. officinalis leaves for the first time. Eight compounds exhibited COMT inhibitory activities with IC₅₀ values of less than 100 μM. Our results indicate that compounds in C. officinalis leaves are potentially effective for preventing Parkinson’s disease and depression. Thus, C. officinalis leaves may hold promise as dietary supplements. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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15 pages, 2277 KiB

Open AccessArticle

Curcumin and Andrographolide Co-Administration Safely Prevent Steatosis Induction and ROS Production in HepG2 Cell Line

by Rosaria Maria Pipitone, Rossella Zito, Giulia Lupo, Ayesha Javed, Claudia La Mantia, Gabriele Di Maria, Giovanni Pratelli, Francesca Di Salvo, Simona Fontana, Marzia Pucci, Daniela Carlisi and Stefania Grimaudo

Molecules 2023, 28(3), 1261; https://doi.org/10.3390/molecules28031261 - 27 Jan 2023

Cited by 5 | Viewed by 2837

Abstract

Non-alcoholic fatty liver disease (NAFLD) is an emerging chronic liver disease worldwide. Curcumin and andrographolide are famous for improving hepatic functions, being able to reverse oxidative stress and release pro-inflammatory cytokines, and they are implicated in hepatic stellate cell activation and in liver [...] Read more.

Non-alcoholic fatty liver disease (NAFLD) is an emerging chronic liver disease worldwide. Curcumin and andrographolide are famous for improving hepatic functions, being able to reverse oxidative stress and release pro-inflammatory cytokines, and they are implicated in hepatic stellate cell activation and in liver fibrosis development. Thus, we tested curcumin and andrographolide separately and in combination to determine their effect on triglyceride accumulation and ROS production, identifying the differential expression of genes involved in fatty liver and oxidative stress development. In vitro steatosis was induced in HepG2 cells and the protective effect of curcumin, andrographolide, and their combination was observed evaluating cell viability, lipid and triglyceride content, ROS levels, and microarray differential gene expression. Curcumin, andrographolide, and their association were effective in reducing steatosis, triglyceride content, and ROS stress, downregulating the genes involved in lipid accumulation. Moreover, the treatments were able to protect the cytotoxic effect of steatosis, promoting the expression of survival and anti-inflammatory genes. The present study showed that the association of curcumin and andrographolide could be used as a therapeutic approach to counter high lipid content and ROS levels in steatosis liver, avoiding the possible hepatotoxic effect of curcumin. Furthermore, this study improved our understanding of the antisteatosis and hepatoprotective properties of a curcumin and andrographolide combination. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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15 pages, 2950 KiB

Open AccessArticle

Strictinin, a Major Ingredient in Yunnan Kucha Tea Possessing Inhibitory Activity on the Infection of Mouse Hepatitis Virus to Mouse L Cells

by Erh-Chuang Tu, Wei-Li Hsu and Jason T. C. Tzen

Molecules 2023, 28(3), 1080; https://doi.org/10.3390/molecules28031080 - 21 Jan 2023

Cited by 6 | Viewed by 3126

Abstract

Theacrine and strictinin of Yunnan Kucha tea prepared from a mutant variety of wild Pu’er tea plants were two major ingredients responsible for the anti-influenza activity. As the COVID-19 outbreak is still lurking, developing safe and cost-effective therapeutics is an urgent need. This [...] Read more.

Theacrine and strictinin of Yunnan Kucha tea prepared from a mutant variety of wild Pu’er tea plants were two major ingredients responsible for the anti-influenza activity. As the COVID-19 outbreak is still lurking, developing safe and cost-effective therapeutics is an urgent need. This study aimed to evaluate the effects of these tea compounds on the infection of mouse hepatitis virus (MHV), a β-coronavirus serving as a surrogate for SARS-CoV. Treatment with strictinin (100 μM), but not theacrine, completely eliminated MHV infection, as indicated by a pronounced reduction in plaque formation, nucleocapsid protein expression, and progeny production of MHV. Subsequently, a time-of-drug addition protocol, including pre-, co-, or post-treatment, was exploited to further evaluate the possible mechanism of antiviral activity mediated by strictinin, and remdesivir, a potential drug for the treatment of SARS-CoV-2, was used as a positive control against MHV infection. The results showed that all three treatments of remdesivir (20 μM) completely blocked MHV infection. In contrast, no significant effect on MHV infection was observed when cells were pre-treated with strictinin (100 μM) prior to infection, while significant inhibition of MHV infection was observed when strictinin was introduced upon viral adsorption (co-treatment) and after viral entry (post-treatment). Of note, as compared with the co-treatment group, the inhibitory effect of strictinin was more striking in the post-treatment group. These results indicate that strictinin suppresses MHV infection by multiple mechanisms; it possibly interferes with viral entry and also critical step(s) of viral infection. Evidently, strictinin significantly inhibited MHV infection and might be a suitable ingredient for protection against coronavirus infection. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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15 pages, 6957 KiB

Open AccessArticle

Obtaining 2,3-Dihydrobenzofuran and 3-Epilupeol from Ageratina pichinchensis (Kunth) R.King & Ho.Rob. Cell Cultures Grown in Shake Flasks under Photoperiod and Darkness, and Its Scale-Up to an Airlift Bioreactor for Enhanced Production

by Mariana Sánchez-Ramos, Silvia Marquina-Bahena, Laura Alvarez, Antonio Bernabé-Antonio, Emmanuel Cabañas-García, Angélica Román-Guerrero and Francisco Cruz-Sosa

Molecules 2023, 28(2), 578; https://doi.org/10.3390/molecules28020578 - 6 Jan 2023

Cited by 6 | Viewed by 2536

Abstract

Ageratina pichinchensis (Kunth) R.King & Ho.Rob. is a plant used in traditional Mexican medicine, and some biotechnological studies have shown that its calluses and cell suspension cultures can produce important anti-inflammatory compounds. In this study, we established a cell culture of A. pichinchensis [...] Read more.

Ageratina pichinchensis (Kunth) R.King & Ho.Rob. is a plant used in traditional Mexican medicine, and some biotechnological studies have shown that its calluses and cell suspension cultures can produce important anti-inflammatory compounds. In this study, we established a cell culture of A. pichinchensis in a 2 L airlift bioreactor and evaluated the production of the anti-inflammatory compounds 2,3-dihydrobenzofuran (1) and 3-epilupeol (2). The maximum biomass production (11.90 ± 2.48 g/L) was reached at 11 days of culture and cell viability was between 80% and 90%. Among kinetic parameters, the specific growth rate (µ) was 0.2216 days⁻¹ and doubling time (td) was 3.13 days. Gas chromatography coupled with mass spectrometry (GC-MS) analysis of extracts showed the maximum production of compound 1 (903.02 ± 41.06 µg/g extract) and compound 2 (561.63 ± 10.63 µg/g extract) at 7 and 14 days, respectively. This study stands out for the significant production of 2,3-dihydrobenzofuran and 3-epilupeol and by the significant reduction in production time compared to callus and cell suspension cultures, previously reported. To date, these compounds have not been found in the wild plant, i.e., its production has only been reported in cell cultures of A. pichinchensis. Therefore, plant cell cultured in an airlift reactor can be an alternative for the improved production of these anti-inflammatory compounds. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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14 pages, 845 KiB

Open AccessArticle

Blackcurrant (Ribes nigrum L.) Seeds—A Valuable Byproduct for Further Processing

by Magdalena Wójciak, Barbara Mazurek, Katarzyna Tyśkiewicz, Małgorzata Kondracka, Grażyna Wójcicka, Tomasz Blicharski and Ireneusz Sowa

Molecules 2022, 27(24), 8679; https://doi.org/10.3390/molecules27248679 - 8 Dec 2022

Cited by 7 | Viewed by 2188

Abstract

The rational exploitation of byproducts is important from the point of view of their potential applicability in various fields. In this study, the possibility of further processing of blackcurrant seeds (BCs), which are a byproduct of fruit processing, was investigated. BCs were used [...] Read more.

The rational exploitation of byproducts is important from the point of view of their potential applicability in various fields. In this study, the possibility of further processing of blackcurrant seeds (BCs), which are a byproduct of fruit processing, was investigated. BCs were used as a material for the extraction of oil on a semi-industrial scale, and the residues were assessed in terms of their potential application in skin care products. Supercritical fluid extraction (SFE) using CO₂ at pressures of 230 and 330 bar and extraction temperature of 40 °C was exploited for isolation of oil, and the products were characterised taking into account lipophilic constituents. After 120 min, the oil yields were 19.67% and 20.94% using CO₂ at 230 and 330 bar, respectively, which showed that SFE was an effective method on a semi-industrial scale, taking into account the extraction yield. The oils had similar fatty acid compositions with a high percentage of linoleic acid (ca. 43%); however, tocopherols and carotenoids were most abundant in the oil obtained at 230 bar. It was also found that the composition of the SFE oils was comparable with that of cold-pressed oil, which shows that supercritical fluid extraction provides a high-quality product; therefore, it can be an alternative to cold pressing. Furthermore, the chemical compositions of the extracts from the oil isolation residues were established using UPLC-MS, and the impact of the extracts on human skin fibroblasts was assessed using the MTT and NR assays. The quantitative analysis revealed that the residues contained high amounts of polyphenolic acids, including gallic, protocatechuic, and hydroxybenzoic acid derivatives, as well as flavonoids, especially quercetin and kaempferol glucoside. Moreover, it was found that the extracts were nontoxic and exerted a stimulatory effect on cell metabolism. Therefore, they can be a valuable additive to natural plant-based cosmetics. Our results showed that blackcurrant seeds, regarded as a byproduct, can be a valuable material for further use. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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19 pages, 3302 KiB

Open AccessArticle

Phytochemical Characterization of Chamomile (Matricaria recutita L.) Roots and Evaluation of Their Antioxidant and Antibacterial Potential

by Lilo K. Mailänder, Peter Lorenz, Hannes Bitterling, Florian C. Stintzing, Rolf Daniels and Dietmar R. Kammerer

Molecules 2022, 27(23), 8508; https://doi.org/10.3390/molecules27238508 - 3 Dec 2022

Cited by 17 | Viewed by 4538

Abstract

Matricaria recutita L., German chamomile, is one of the most widely used medicinal plants, whose efficacy has been proven in numerous studies. However, its roots have attracted only little interest so far, since mainly above-ground plant parts are used for medicinal purposes. To [...] Read more.

Matricaria recutita L., German chamomile, is one of the most widely used medicinal plants, whose efficacy has been proven in numerous studies. However, its roots have attracted only little interest so far, since mainly above-ground plant parts are used for medicinal purposes. To broaden the knowledge of chamomile roots, a profound phytochemical characterization was performed along with a bioactivity screening of corresponding root extracts. While volatile constituents such as chamomillol and polyynes were detected using GC-MS, HPLC-MSⁿ analyses revealed the occurrence of four coumarin glycosides, more than ten phenolic acid esters and five glyceroglycolipids. Furthermore, the antioxidant activity of the extracts was evaluated. Polar extracts revealed IC₅₀ values ranging from 13 to 57 µg/mL in the DPPH radical scavenging assay, which is in the same range as reported for chamomile flower extracts. In addition, superoxide radical scavenging potential and mild antibacterial effects against S. aureus und B. subtilis were demonstrated. Moreover, to assess interspecies variation in chamomile roots, extracts of M. recutita were compared to those of M. discoidea DC. Interestingly, the latter revealed stronger antioxidant activity. The presented results aim at the valorization of chamomile roots, previously discarded as by-product of chamomile flower production, as a sustainable source of bioactive phytochemicals. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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13 pages, 1378 KiB

Open AccessArticle

Mass Spectrometry-Based Identification of Bioactive Bee Pollen Proteins: Evaluation of Allergy Risk after Bee Pollen Supplementation

by Eliza Matuszewska, Szymon Plewa, Dagmara Pietkiewicz, Kacper Kossakowski, Joanna Matysiak, Grzegorz Rosiński and Jan Matysiak

Molecules 2022, 27(22), 7733; https://doi.org/10.3390/molecules27227733 - 10 Nov 2022

Cited by 11 | Viewed by 2683

Abstract

Bee pollen, because of its high content of nutrients, is a very valuable medicinal and nutritional product. However, since its composition is not completely studied, the consumption of this product may cause adverse effects, including allergic reactions. Therefore, this study aimed to discover [...] Read more.

Bee pollen, because of its high content of nutrients, is a very valuable medicinal and nutritional product. However, since its composition is not completely studied, the consumption of this product may cause adverse effects, including allergic reactions. Therefore, this study aimed to discover and characterize the bioactive proteins of bee pollen collected in Poland, focusing mainly on the allergens. For this purpose, the purified and concentrated pollen aqueous solutions were analyzed using the nanoLC-MALDI-TOF/TOF MS analytical platform. As a result of the experiments, 197 unique proteins derived from green plants (Viridiplantae) and 10 unique proteins derived from bees (Apis spp.) were identified. Among them, potential plant allergens were discovered. Moreover, proteins belonging to the group of hypothetical proteins, whose expression had not been confirmed experimentally before, were detected. Because of the content of bioactive compounds—both beneficial and harmful—there is a critical need to develop guidelines for standardizing bee pollen, especially intended for consumption or therapeutic purposes. This is of particular importance because awareness of the allergen content of bee pollen and other bee products can prevent health- or life-threatening incidents following the ingestion of these increasingly popular “superfoods”. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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19 pages, 3974 KiB

Open AccessArticle

Anthocyanins Formulated with Carboxymethyl Starch for Gastric and Intestinal Delivery

by Luiz Bruno De Sousa Sabino, Francesco Copes, Solène Saulais, Edy Sousa De Brito, Ivanildo José Da Silva Júnior, Tien Canh Le, Mircea Alexandru Mateescu and Diego Mantovani

Molecules 2022, 27(21), 7271; https://doi.org/10.3390/molecules27217271 - 26 Oct 2022

Cited by 3 | Viewed by 1983

Abstract

Anthocyanins obtained from jambolan have been used as active agents in different carboxymethyl starch-based tablet formulations and their release profiles evaluated in simulated gastric fluids (SGF) and simulated intestinal (SIF) fluids. Structural analysis highlighted a strong interaction between anthocyanins and carboxymethyl starch, evidenced [...] Read more.

Anthocyanins obtained from jambolan have been used as active agents in different carboxymethyl starch-based tablet formulations and their release profiles evaluated in simulated gastric fluids (SGF) and simulated intestinal (SIF) fluids. Structural analysis highlighted a strong interaction between anthocyanins and carboxymethyl starch, evidenced by scanning electron microscopy and infrared analysis. Tablet dissolution behavior varied according to the pH of the media, being controlled by the swelling and/or erosion of the polymeric matrix. Various formulations for immediate, fast, and sustained release of anthocyanins for 30 min, 2 h and 12 h of dissolution have been developed. It was found that monolithic carboxymethyl starch tablets loaded with powdered jambolan extract efficiently afforded the complete delivery (100% of anthocyanins) to different sites of the simulated gastrointestinal tract and ensured the stability of these pigments, which maintained their antioxidant activity. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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10 pages, 1059 KiB

Open AccessArticle

Cinnamomum verum J. Presl Bark Contains High Contents of Nicotinamide Mononucleotide

by Jing Yan, Takumi Sakamoto, Ariful Islam, Yashuang Ping, Soho Oyama, Hiroyuki Fuchino, Hitomi Kawakami, Kayo Yoshimatsu, Tomoaki Kahyo and Mitsutoshi Setou

Molecules 2022, 27(20), 7054; https://doi.org/10.3390/molecules27207054 - 19 Oct 2022

Cited by 1 | Viewed by 3139

Abstract

The global population is aging, and intervention strategies for anti-aging and the prevention of aging-related diseases have become a topic actively explored today. Nicotinamide adenine dinucleotide (NAD⁺) is an important molecule in the metabolic process, and its content in tissues and [...] Read more.

The global population is aging, and intervention strategies for anti-aging and the prevention of aging-related diseases have become a topic actively explored today. Nicotinamide adenine dinucleotide (NAD⁺) is an important molecule in the metabolic process, and its content in tissues and cells decreases with age. The supplementation of nicotinamide mononucleotide (NMN), an important intermediate and precursor of NAD⁺, has increased NAD⁺ levels, and its safety has been demonstrated in rodents and human studies. However, the high content of NMN in natural plants has not been fully explored as herbal medicines for drug development. Here, we identified that the leaf of Cinnamomum verum J. Presl (C. verum) was the highest NMN content among the Plant Extract Library (PEL) with food experience, using ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS). To validate this result, the extraction and quantitative analysis of bark, leaf, root, and stem of fresh C. verum was conducted. The results revealed that the bark had the highest NMN content in C. verum (0.471 mg/100 g). Our study shed light on the prospects of developing natural plants in the context of NMN as drugs for anti-aging and prevention of aging-related diseases. The future should focus on the development and application of C. verum pharmaceutical formulations. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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15 pages, 2092 KiB

Open AccessArticle

Design, Synthesis and Biological Evaluation of Lophanic Acid Derivatives as Antifungal and Antibacterial Agents

by Xiang Yu, Xun Song, Yi Zhang, Yemeng Yang, Jianghai Ye, Yahua Liu, Lutai Pan and Hongjie Zhang

Molecules 2022, 27(20), 6836; https://doi.org/10.3390/molecules27206836 - 12 Oct 2022

Cited by 1 | Viewed by 1935

Abstract

In order to discover more promising antifungal and antibacterial agents, a series of new derivatives were designed and synthesized by structure modification based on the naturally occurring antimicrobial compound lophanic acid. The structures of all the target compounds were well characterized by spectroscopic [...] Read more.

In order to discover more promising antifungal and antibacterial agents, a series of new derivatives were designed and synthesized by structure modification based on the naturally occurring antimicrobial compound lophanic acid. The structures of all the target compounds were well characterized by spectroscopic data. The stereochemistry of these compounds was further determined through the X-ray diffraction analysis of 6a. The synthetic compounds were evaluated for their antimicrobial activities against filamentous fungi (T. rubrum, T. mentagrophytes), yeasts (C. neoformans, C. albicans) and Gram-positive and Gram-negative bacteria (MRSA, S. mutans, S. sobrinus, and E. coli). Among them, 3d and 3i are found as the most promising leads that showed potent inhibitory effects against all the tested fungal and bacterial strains except for E. coli. The presence of the C-20 carboxylic ester groups and the free hydroxy group at C-13 was found to be essential for the antifungal and antibacterial activities of the lophanic acid derivatives. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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20 pages, 4891 KiB

Open AccessArticle

Mulberry Leaf Extract Improves Metabolic Syndrome by Alleviating Lipid Accumulation In Vitro and In Vivo

by Liangyu He, Yan Xing, Xinxiu Ren, Mengjiao Zheng, Shiqiang Yu, Yinbo Wang, Zhilong Xiu and Yuesheng Dong

Molecules 2022, 27(16), 5111; https://doi.org/10.3390/molecules27165111 - 11 Aug 2022

Cited by 14 | Viewed by 2794

Abstract

Metabolic syndrome (MS) is a metabolic disease with multiple complications. Mulberry leaf extract (MLE) is rich in flavonoids and has great potential in alleviating glucose and lipid metabolism disorders. This study evaluated the effect and mechanism of MLE on the alleviation of MS. [...] Read more.

Metabolic syndrome (MS) is a metabolic disease with multiple complications. Mulberry leaf extract (MLE) is rich in flavonoids and has great potential in alleviating glucose and lipid metabolism disorders. This study evaluated the effect and mechanism of MLE on the alleviation of MS. The components of the MLE were analyzed, and then the regulation of lipid metabolism by MLE in vitro and in vivo was determined. In a hepatocyte model of oleic acid-induced lipid accumulation, it was found that MLE alleviated lipid accumulation and decreased the expression of genes involved in lipogenesis. Furthermore, MLE improved obesity, insulin resistance, plasma lipid profile, and liver function in MS mice after a 15-week intervention. MLE decreased the expression of SREBP1, ACC, and FAS through the AMPK signaling pathway to inhibit lipid synthesis and increase the level of CPT1A to promote lipid decomposition to achieve its hypolipidemic effect. Meanwhile, MLE was also shown to affect the composition of the gut microbiota and the production of short-chain fatty acids, which contributed to the alleviation of lipid accumulation. Our results suggest that MLE can improve MS by improving lipid metabolism through multiple mechanisms and can be developed into dietary supplements for the improvement of MS. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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Review

Jump to: Research

32 pages, 1724 KiB

Open AccessReview

Bio-Actives from Natural Products with Potential Cardioprotective Properties: Isolation, Identification, and Pharmacological Actions of Apigenin, Quercetin, and Silibinin

by Ekaterina-Michaela Tomou, Paraskevi Papakyriakopoulou, Helen Skaltsa, Georgia Valsami and Nikolaos P. E. Kadoglou

Molecules 2023, 28(5), 2387; https://doi.org/10.3390/molecules28052387 - 5 Mar 2023

Cited by 15 | Viewed by 3536

Abstract

Cardiovascular diseases (CVDs) are the leading cause of morbidity and mortality worldwide. As a result, pharmaceutical and non-pharmaceutical interventions modifying risk factors for CVDs are a top priority of scientific research. Non-pharmaceutical therapeutical approaches, including herbal supplements, have gained growing interest from researchers [...] Read more.

Cardiovascular diseases (CVDs) are the leading cause of morbidity and mortality worldwide. As a result, pharmaceutical and non-pharmaceutical interventions modifying risk factors for CVDs are a top priority of scientific research. Non-pharmaceutical therapeutical approaches, including herbal supplements, have gained growing interest from researchers as part of the therapeutic strategies for primary or secondary prevention of CVDs. Several experimental studies have supported the potential effects of apigenin, quercetin, and silibinin as beneficial supplements in cohorts at risk of CVDs. Accordingly, this comprehensive review focused critically on the cardioprotective effects/mechanisms of the abovementioned three bio-active compounds from natural products. For this purpose, we have included in vitro, preclinical, and clinical studies associated with atherosclerosis and a wide variety of cardiovascular risk factors (hypertension, diabetes, dyslipidemia, obesity, cardiac injury, and metabolic syndrome). In addition, we attempted to summarize and categorize the laboratory methods for their isolation and identification from plant extracts. This review unveiled many uncertainties which are still unexplored, such as the extrapolation of experimental results to clinical practice, mainly due to the small clinical studies, heterogeneous doses, divergent constituents, and the absence of pharmacodynamic/pharmacokinetic analyses. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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16 pages, 1195 KiB

Open AccessReview

Spondias sp: Shedding Light on Its Vast Pharmaceutical Potential

by Érica Mendes dos Santos, Janaína Artem Ataide, Julia Cedran Coco, Ana Laura Masquetti Fava, Luiza Aparecida Luna Silvério, Ana Claudia Sueiro, Jéssica Ribeiro Alves Silva, André Moreni Lopes, Ana Cláudia Paiva-Santos and Priscila Gava Mazzola

Molecules 2023, 28(4), 1862; https://doi.org/10.3390/molecules28041862 - 16 Feb 2023

Cited by 5 | Viewed by 3448

Abstract

Many plants are used by the population through popular knowledge passed from generation to generation for the treatment of various diseases. However, there is not always any scientific content supporting these uses, which is very important for safety. One of these plants is [...] Read more.

Many plants are used by the population through popular knowledge passed from generation to generation for the treatment of various diseases. However, there is not always any scientific content supporting these uses, which is very important for safety. One of these plants is the fruit of the Spondias genus, which during its processing generates various residues that are discarded, but which also have pharmacological properties. The focus of this review is to survey the pharmacological activities that Spondias genus shows, as well as which part of the plant is used, since there is a lot of richness in its by-products, such as leaf, bark, resin, seed, and peel, which are discarded and could be reused. The main activities of this genus are antioxidant, anti-inflammatory, antidiabetic, antifungal, and antiviral, among others. These properties indicate that this genus could be used in the treatment of several diseases, but there are still not many products available on the market that use this genus as an active ingredient. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 3rd Edition)

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