Molecules

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20 pages, 2969 KiB

Open AccessArticle

Effects of the Seed Oil of Carica papaya Linn on Food Consumption, Adiposity, Metabolic and Inflammatory Profile of Mice Using Hyperlipidic Diet

by Lidiani Figueiredo Santana, Bruna Larissa Spontoni do Espirito Santo, Mariana Bento Tatara, Fábio Juliano Negrão, Júlio Croda, Flávio Macedo Alves, Wander Fernando de Oliveira Filiú, Leandro Fontoura Cavalheiro, Carlos Eduardo Domingues Nazário, Marcel Arakaki Asato, Bernardo Bacelar de Faria, Valter Aragão do Nascimento, Rita de Cássia Avellaneda Guimarães, Karine de Cássia Freitas and Priscila Aiko Hiane

Molecules 2022, 27(19), 6705; https://doi.org/10.3390/molecules27196705 - 8 Oct 2022

Cited by 6 | Viewed by 3091

Abstract

Background: Studies indicate that different parts of Carica papaya Linn have nutritional properties that mean it can be used as an adjuvant for the treatment of various pathologies. Methods: The fatty acid composition of the oil extracted from the seeds of Carica papaya [...] Read more.

Background: Studies indicate that different parts of Carica papaya Linn have nutritional properties that mean it can be used as an adjuvant for the treatment of various pathologies. Methods: The fatty acid composition of the oil extracted from the seeds of Carica papaya Linn was evaluated by gas chromatography, and an acute toxicity test was performed. For the experiment, Swiss mice were fed a balanced or high-fat diet and supplemented with saline, soybean oil, olive oil, or papaya seed oil. Oral glucose tolerance and insulin sensitivity tests were performed. After euthanasia, adiposity, glycemia, total cholesterol and fractions, insulin, resistin, leptin, MCP-1, TNF-α, and IL-6 and the histology of the liver, pancreas, and adipose tissue were evaluated. Results: Papaya seed oil showed predominance of monounsaturated fatty acids in its composition. No changes were observed in the acute toxicity test. Had lower food intake in grams, and caloric intake and in the area of adipocytes without minimizing weight gain or adiposity and impacting the liver or pancreas. Reductions in total and non-HDL-c, LDL-c, and VLDL-c were also observed. The treatment had a hypoglycemic and protective effect on insulin resistance. Supplementation also resulted in higher leptin and lower insulin and cytokine resistance. Conclusions: Under these experimental conditions, papaya seed oil led to higher amounts of monounsaturated fatty acids and had hypocholesterolemic, hypotriglyceridemic, and hypoglycemic effects. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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19 pages, 3786 KiB

Open AccessArticle

Exceptional Properties of Lepidium sativum L. Extract and Its Impact on Cell Viability, Ros Production, Steroidogenesis, and Intracellular Communication in Mice Leydig Cells In Vitro

by Tomas Jambor, Terezia Zajickova, Julius Arvay, Eva Ivanisova, Ivana Tirdilova, Nikola Knizatova, Hana Greifova, Anton Kovacik, Eliska Galova and Norbert Lukac

Molecules 2022, 27(16), 5127; https://doi.org/10.3390/molecules27165127 - 11 Aug 2022

Cited by 3 | Viewed by 2061

Abstract

The prevalence of reproductive dysfunction in males has risen in the last few years, and alternative therapies are gradually gaining in popularity. Our in vitro study aimed to evaluate the potential impact of Lepidium sativum L. on mice TM3 Leydig cells, concerning basal [...] Read more.

The prevalence of reproductive dysfunction in males has risen in the last few years, and alternative therapies are gradually gaining in popularity. Our in vitro study aimed to evaluate the potential impact of Lepidium sativum L. on mice TM3 Leydig cells, concerning basal parameters such as cell viability, cell membrane integrity, and lysosomal activity, after 24 h and 48 h exposure. Moreover, reactive oxygens species generation, sex-steroid hormone secretion, and intercellular communication were quantified. In the present study, the microgreen extract from Lepidium was rich in ferulic acid, 4-OH benzoic acid, and resveratrol, with a significant antioxidant activity. The results showed that lower experimental doses (62.5–250 µg/mL) could positively affect the observed parameters, with significant differences at 250 µg/mL after 24 h and 48 h, respectively. Potential risks could be associated with higher concentrations, starting at 500 µg/mL, 1000 µg/mL, and 2000 µg/mL of Lepidium. Nevertheless, biochemical quantification indicated a significant antioxidant potential and a rich content of biologically active molecules at the applied doses, and time determined the intracellular response of the cultured model. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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22 pages, 1221 KiB

Open AccessArticle

Antioxidant and Antimicrobial Activities of Erodium arborescens Aerial Part Extracts and Characterization by LC-HESI-MS² of Its Acetone Extract

by Sonda Samet, Amani Ayachi, Mariam Fourati, Lotfi Mallouli, Noureddine Allouche, Michel Treilhou, Nathan Téné and Raoudha Mezghani-Jarraya

Molecules 2022, 27(14), 4399; https://doi.org/10.3390/molecules27144399 - 8 Jul 2022

Cited by 7 | Viewed by 2139

Abstract

The phytochemical analysis of antioxidant and antibacterial activities of Erodium arborescens aerial part extracts constitute the focus of this research. The chemical composition of an acetone extract was investigated using LC-HESI-MS², which revealed the presence of 70 compounds. The major identified [...] Read more.

The phytochemical analysis of antioxidant and antibacterial activities of Erodium arborescens aerial part extracts constitute the focus of this research. The chemical composition of an acetone extract was investigated using LC-HESI-MS², which revealed the presence of 70 compounds. The major identified components were tannin derivatives. Total polyphenol and total flavonoid contents were assessed in plant extracts (hexane, ethyl acetate, acetone and methanol). The results showed that the acetone extract exhibited the highest contents of polyphenols and flavonoids, 895.54 and 36.39 mg QE/g DE, respectively. Furthermore, when compared to other extracts, Erodium arborescens acetone extract was endowed with the highest antioxidant activity with 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) tests. In addition, the four extracts of Erodium arborescens showed variable degrees of antimicrobial activity against the tested strains, and the interesting activity was obtained with acetone and methanol extracts. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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22 pages, 6021 KiB

Open AccessArticle

Purification and Characterization of Gum-Derived Polysaccharides of Moringa oleifera and Azadirachta indica and Their Applications as Plant Stimulants and Bio-Pesticidal Agents

by Nagarajan Shobana, Pandurangan Prakash, Antony V. Samrot, P. J. Jane Cypriyana, Purohit Kajal, Mahendran Sathiyasree, Subramanian Saigeetha, T. Stalin Dhas, D. Alex Anand, Gokul Shankar Sabesan, Bala Sundaram Muthuvenkatachalam, Basanta Kumar Mohanty and Sridevi Visvanathan

Molecules 2022, 27(12), 3720; https://doi.org/10.3390/molecules27123720 - 9 Jun 2022

Cited by 11 | Viewed by 3935

Abstract

Plant gums are bio-organic substances that are derived from the barks of trees. They are biodegradable and non-adverse complex polysaccharides that have been gaining usage in recent years due to a number of advantages they contribute to various applications. In this study, gum [...] Read more.

Plant gums are bio-organic substances that are derived from the barks of trees. They are biodegradable and non-adverse complex polysaccharides that have been gaining usage in recent years due to a number of advantages they contribute to various applications. In this study, gum was collected from Moringa oleifera and Azadirachta indica trees, then dried and powdered. Characterizations of gum polysaccharides were performed using TLC, GC-MS, NMR, etc., and sugar molecules such as glucose and xylose were found to be present. Effects of the gums on Abelmoschus esculentus growth were observed through root growth, shoot growth, and biomass content. The exposure of the seeds to the plant gums led to bio stimulation in the growth of the plants. Poor quality soil was exposed to the gum polysaccharide, where the polysaccharide was found to improve soil quality, which was observed through soil analysis and SEM analysis of soil porosity and structure. Furthermore, the plant gums were also found to have bio-pesticidal activity against mealybugs, which showed certain interstitial damage evident through histopathological analysis. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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21 pages, 3533 KiB

Open AccessArticle

Polymeric Forms of Plant Flavonoids Obtained by Enzymatic Reactions

by Malgorzata Latos-Brozio, Anna Masek and Małgorzata Piotrowska

Molecules 2022, 27(12), 3702; https://doi.org/10.3390/molecules27123702 - 9 Jun 2022

Cited by 8 | Viewed by 2449

Abstract

Naringenin is one of the flavonoids originating from citrus fruit. This polyphenol is mainly found in grapefruit, orange and lemon. The antioxidant and antimicrobial properties of flavonoids depend on their structure, including the polymeric form. The aim of this research was to achieve [...] Read more.

Naringenin is one of the flavonoids originating from citrus fruit. This polyphenol is mainly found in grapefruit, orange and lemon. The antioxidant and antimicrobial properties of flavonoids depend on their structure, including the polymeric form. The aim of this research was to achieve enzymatic polymerization of naringenin and to study the properties of poly(naringenin). The polymerization was performed by methods using two different enzymes, i.e., laccase and horseradish peroxidase (HRP). According to the literature data, naringenin had not been polymerized previously using the enzymatic polymerization method. Therefore, obtaining polymeric naringenin by reaction with enzymes is a scientific novelty. The research methodology included analysis of the structure of poly(naringenin) by NMR, GPC, FTIR and UV-Vis and its morphology by SEM, as well as analysis of its properties, i.e., thermal stability (DSC and TGA), antioxidant activity (ABTS, DPPH, FRAP and CUPRAC) and antimicrobial properties. Naringenin oligomers were obtained as a result of polymerization with two types of enzymes. The polymeric forms of naringenin were more resistant to thermo-oxidation; the final oxidation temperature T_o of naringenin catalyzed by laccase (poly(naringenin)-laccase) was 28.2 °C higher, and poly(naringenin)-HRP 23.6 °C higher than that of the basic flavonoid. Additionally, due to the higher molar mass and associated increase in OH groups in the structure, naringenin catalyzed by laccase (poly(naringenin)-laccase) showed better activity for scavenging ABTS^+• radicals than naringenin catalyzed by HRP (poly(naringenin)-HRP) and naringenin. In addition, poly(naringenin)-laccase at a concentration of 5 mg/mL exhibited better microbial activity against E. coli than monomeric naringenin. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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16 pages, 1598 KiB

Open AccessArticle

Ultrasound-Assisted Extraction of Phenolic Compounds from Psidium cattleianum Leaves: Optimization Using the Response Surface Methodology

by Napoleón González-Silva, Yolanda Nolasco-González, Gabriela Aguilar-Hernández, Sonia Guadalupe Sáyago-Ayerdi, Zuamí Villagrán, José Luis Acosta, Efigenia Montalvo-González and Luis Miguel Anaya-Esparza

Molecules 2022, 27(11), 3557; https://doi.org/10.3390/molecules27113557 - 31 May 2022

Cited by 21 | Viewed by 3719

Abstract

In this study, conditions for the ultrasound-assisted extraction (UAE) of soluble polyphenols from Psidium cattleianum (PC) leaves were optimized using response surface methodology (RSM) by assessing the effect of extraction time (X_ET = 2, 4, and 6 min), sonication amplitude (X_SA [...] Read more.

In this study, conditions for the ultrasound-assisted extraction (UAE) of soluble polyphenols from Psidium cattleianum (PC) leaves were optimized using response surface methodology (RSM) by assessing the effect of extraction time (X_ET = 2, 4, and 6 min), sonication amplitude (X_SA = 60, 80, and 100%), and pulse cycle (X_PC = 0.4, 0.7, and 1 s). Furthermore, the optimized UAE conditions were compared with a conventional aqueous–organic extraction (AOE) method for extracting total phenolics; moreover, a phenolic profile using HPLC and antioxidant activity (DPPH, ABTS, and FRAP) were also compared. According to the RSM, the best conditions for UAE to extract the highest soluble polyphenol content and yield (158.18 mg/g dry matter [DM] and 15.81%) include a 100% sonication amplitude for 4 min at 0.6 s of pulse cycle. The optimal UAE conditions exhibited an effectiveness of 1.71 times in comparison to the AOE method for extracting total phenolics, in 96.66% less time; moreover, PC leaf extracts by UAE showed higher antioxidant values than AOE. Additionally, gallic, protocateic, chlorogenic, caffeic, coumaric, trans-cinnamic, 4-hydroxybenzoic, and syringic acids, as well as kaempferol were identified in PC leaves under UAE. PC leaf extracts are widely used for therapeutic and other industrial purposes; thus, the UAE proves to be a useful technology with which to improve the yield extraction of PC leaf phytochemicals. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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27 pages, 9786 KiB

Open AccessArticle

Targeting Akt/NF-κB/p53 Pathway and Apoptosis Inducing Potential of 1,2-Benzenedicarboxylic Acid, Bis (2-Methyl Propyl) Ester Isolated from Onosma bracteata Wall. against Human Osteosarcoma (MG-63) Cells

by Ajay Kumar, Sandeep Kaur, Sukhvinder Dhiman, Prithvi Pal Singh, Gaurav Bhatia, Sharad Thakur, Hardeep Singh Tuli, Upendra Sharma, Subodh Kumar, Abdulmajeed G. Almutary, Abdullah M. Alnuqaydan, Arif Hussain, Shafiul Haque, Kuldeep Dhama and Satwinderjeet Kaur

Molecules 2022, 27(11), 3478; https://doi.org/10.3390/molecules27113478 - 28 May 2022

Cited by 12 | Viewed by 3683

Abstract

Onosma bracteata Wall. is an important medicinal and immunity-enhancing herbs. This plant is commonly used in the preparation of traditional Ayurvedic drugs to treat numerous diseases. Inspired by the medicinal properties of this plant, the present study aimed to investigate the antiproliferative potential [...] Read more.

Onosma bracteata Wall. is an important medicinal and immunity-enhancing herbs. This plant is commonly used in the preparation of traditional Ayurvedic drugs to treat numerous diseases. Inspired by the medicinal properties of this plant, the present study aimed to investigate the antiproliferative potential and the primary molecular mechanisms of the apoptotic induction against human osteosarcoma (MG-63) cells. Among all the fractions isolated from O. bracteata, ethyl acetate fraction (Obea) showed good antioxidant activity in superoxide radical scavenging assay and lipid peroxidation assay with an EC₅₀ value of 95.12 and 80.67 µg/mL, respectively. Silica gel column chromatography of ethyl acetate (Obea) fraction of O. bracteata yielded a pure compound, which was characterized by NMR, FTIR, and HR-MS analysis and was identified as 1,2-benzene dicarboxylic acid, bis (2-methyl propyl) ester (BDCe fraction). BDCe fraction was evaluated for the antiproliferative potential against human osteosarcoma MG-63, human neuroblastoma IMR-32, and human lung carcinoma A549 cell lines by MTT assay and exhibited GI₅₀ values of 37.53 μM, 56.05 μM, and 47.12 μM, respectively. In MG-63 cells, the BDCe fraction increased the level of ROS and simultaneously decreased the mitochondria membrane potential (MMP) potential by arresting cells at the G₀/G₁ phase, suggesting the initiation of apoptosis. Western blotting analysis revealed the upregulation of p53, caspase3, and caspase9 while the expressions of p-NF-κB, p-Akt and Bcl-xl were decreased. RT-qPCR studies also showed upregulation in the expression of p53 and caspase3 and downregulation in the expression of CDK2, Bcl-2 and Cyclin E genes. Molecular docking analysis displayed the interaction between BDCe fraction with p53 (−151.13 kcal/mol) and CDK1 (−133.96 kcal/mol). The results of the present work suggest that the BDCe fraction has chemopreventive properties against osteosarcoma (MG-63) cells through the induction of cell cycle arrest and apoptosis via Akt/NF-κB/p53 pathways. This study contributes to the understanding of the utilization of BDCe fraction in osteosarcoma treatment. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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31 pages, 3140 KiB

Open AccessArticle

Can Extracts from the Leaves and Fruits of the Cotoneaster Species Be Considered Promising Anti-Acne Agents?

by Barbara Krzemińska, Michał P. Dybowski, Katarzyna Klimek, Rafał Typek, Małgorzata Miazga-Karska, Grażyna Ginalska and Katarzyna Dos Santos Szewczyk

Molecules 2022, 27(9), 2907; https://doi.org/10.3390/molecules27092907 - 2 May 2022

Cited by 3 | Viewed by 2836

Abstract

This study aimed to evaluate the phenolic profile and biological activity of the extracts from the leaves and fruits of Cotoneaster nebrodensis and Cotoneaster roseus. Considering that miscellaneous species of Cotoneaster are thought to be healing in traditional Asian medicine, we assumed [...] Read more.

This study aimed to evaluate the phenolic profile and biological activity of the extracts from the leaves and fruits of Cotoneaster nebrodensis and Cotoneaster roseus. Considering that miscellaneous species of Cotoneaster are thought to be healing in traditional Asian medicine, we assumed that this uninvestigated species may reveal significant therapeutic properties. Here, we report the simultaneous assessment of chemical composition as well as biological activities (antioxidant, anti-inflammatory, antibacterial, and cytotoxic properties) of tested species. Complementary LC-MS analysis revealed that polyphenols (especially flavonoids and proanthocyanidins) are the overriding phytochemicals with the greatest significance in tested biological activities. In vitro chemical tests considering biological activities revealed that obtained results showed different values depending on concentration, extraction solvent as well as phenolic content. Biological assays demonstrated that the investigated extracts possessed antibacterial properties and were not cytotoxic toward normal skin fibroblasts. Given the obtained results, we concluded that knowledge of the chemical composition and biological activities of investigated species are important to achieve a better understanding of the utilization of these plants in traditional medicine and be useful for further research in their application to treat various diseases, such as skin disorders. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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13 pages, 2077 KiB

Open AccessArticle

Composition and Antifungal Activity of the Alkaloidal Fraction of Lupinus mirabilis Leaves: A Biochemometrics-Based Exploration

by Freddy A. Bernal and Ericsson Coy-Barrera

Molecules 2022, 27(9), 2832; https://doi.org/10.3390/molecules27092832 - 29 Apr 2022

Cited by 2 | Viewed by 1866

Abstract

Lupinus plants are well-recognized due to their significant alkaloid content, which has made them the subject of several studies. However, the lack of chemical and biological information on the Colombian Lupinus species remains a fact. Therefore, the alkaloidal fractions from the leaves of [...] Read more.

Lupinus plants are well-recognized due to their significant alkaloid content, which has made them the subject of several studies. However, the lack of chemical and biological information on the Colombian Lupinus species remains a fact. Therefore, the alkaloidal fractions from the leaves of L. mirabilis obtained by conventional solvent and ultrasound-assisted extraction (CSE and UAE, respectively) at different time frames were analyzed. Sparteine (2) was the main component in all cases; however, its relative abundance showed large variability, ranging from 64.7% to 80.6%. Minor constituents were also affected by the extraction conditions. In general, prolonged times gave a higher proportion of alkaloids under CSE, while only a slight decrease was observed under UAE. Both the method and extraction time appeared to equally affect the ratios of particular alkaloids, leading to variations in their effect on the mycelial growth of Fusarium oxysporum. Holistic analysis through multiple-covariate statistical methods as an approach to integrating chemical and bioactivity datasets allowed inferring the compounds most likely responsible for the changes in mycelial growth inhibition. 13α-Hydroxylupanine (12) might represent a promising compound to be included in further studies against this phytopathogen. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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17 pages, 13512 KiB

Open AccessArticle

Effects of Artemisia macrocephala Jacquem on Memory Deficits and Brain Oxidative Stress in Streptozotocin-Induced Diabetic Mice

by Atiqul Bari, Syed Muhammad Mukarram Shah, Fakhria A. Al-Joufi, Syed Wadood Ali Shah, Mohammad Shoaib, Ismail Shah, Muhammad Zahoor, Muhammad Naeem Ahmed, Mehreen Ghias, Syed Muhammad Hassan Shah and Atif Ali Khan Khalil

Molecules 2022, 27(8), 2399; https://doi.org/10.3390/molecules27082399 - 8 Apr 2022

Cited by 6 | Viewed by 2229

Abstract

Different species of Artemisia have been reported to have therapeutic potential in treating various health disorders, including diabetes and memory dysfunction. The present study was planned to evaluate the effects of Artemisia macrocephala Jacquem crude extract and its subfractions as antiamnesic agents in [...] Read more.

Different species of Artemisia have been reported to have therapeutic potential in treating various health disorders, including diabetes and memory dysfunction. The present study was planned to evaluate the effects of Artemisia macrocephala Jacquem crude extract and its subfractions as antiamnesic agents in streptozotocin-induced (STZ) diabetic mice. The in vivo behavioral studies were performed using the Y Maze test and novel object recognition test (NORT) test at doses of 100 and 200 mg/kg of crude extract and 75 and 150 mg/kg of fractions. The in vitro and ex vivo anticholinesterase activities, along with biochemical parameters (superoxide dismutase, catalase, glutathione and lipid peroxidation) in the brain, were evaluated. Blood glucose levels were monitored with a glucometer; crude extract and fractions reduced the glucose level considerably, with some differences in the extent of their efficacies. The crude extract and fractions demonstrated significant inhibitory activity against cholinesterases (AChE and BuChE) in vitro. Crude, chloroform and ethyl acetate extract were found to be more potent than the other fractions, with IC₅₀ of Crd-Am = 116.36 ± 1.48 and 240.52 ± 1.35 µg/mL, Chl-Am = 52.68 ± 1.09 and 57.45 ± 1.39 µg/mL and Et-Am = 75.19 ± 1.02 and 116.58 ± 1.09 µg/mL, respectively. Oxidative stress biomarkers like superoxide dismutase, catalase and glutathione levels were elevated, whereas MDA levels were reduced by crude extract and all fractions with little difference in their respective values. The Y-maze test and novel object recognition test demonstrated declines in memory impairment in groups (n = 6) treated with crude extract and fractions as compared to STZ diabetic (amnesic) group. The most active fraction, Chl-Am, was also subjected to isolation of bioactive compounds; three compounds were obtained in pure state and designated as AB-I, AB-II and AB-III. Overall, the results of the study showed that Artemisia macrocephala Jacquem enhanced the memory impairment associated with diabetes, elevated acetylcholine levels and ameliorated oxidative stress. Further studies are needed to explore the beneficial role of the secondary metabolites isolated in the present study as memory enhancers. Toxicological aspects of the extracts are also important and need to be evaluated in other animal models. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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13 pages, 905 KiB

Open AccessArticle

HESI-MS/MS Analysis of Phenolic Compounds from Calendula aegyptiaca Fruits Extracts and Evaluation of Their Antioxidant Activities

by Wafa Grati, Sonda Samet, Bouthaina Bouzayani, Amani Ayachi, Michel Treilhou, Nathan Téné and Raoudha Mezghani-Jarraya

Molecules 2022, 27(7), 2314; https://doi.org/10.3390/molecules27072314 - 2 Apr 2022

Cited by 21 | Viewed by 3516

Abstract

Considering medicinal plants as an inexhaustible source of active ingredients that may be easily isolated using simple and inexpensive techniques, phytotherapy is becoming increasingly popular. Various experimental approaches and analytical methods have been used to demonstrate that the genus Calendula (Asteraceae) has a [...] Read more.

Considering medicinal plants as an inexhaustible source of active ingredients that may be easily isolated using simple and inexpensive techniques, phytotherapy is becoming increasingly popular. Various experimental approaches and analytical methods have been used to demonstrate that the genus Calendula (Asteraceae) has a particular richness in active ingredients, especially phenolic compounds, which justifies the growing interest in scientific studies on this genus’ species. From a chemical and biological viewpoint, Calendula aegyptiaca is a little-studied plant. For the first time, high-performance liquid chromatography combined with negative electrospray ionization mass spectrometry (HPLC-HESI-MS) was used to analyze methanolic extracts of Calendula aegyptiaca (C. aegyptiaca) fruits. Thirty-five molecules were identified. Flavonoids (47.87%), phenolic acids (5.18%), and saponins (6.47%) formed the majority of these chemicals. Rutin, caffeic acid hexoside, and Soyasaponin βg’ were the most abundant molecules in the fruit methanolic extract, accounting for 17.49% of total flavonoids, 2.32 % of total phenolic acids, and 0.95% of total saponins, respectively. The antioxidant activity of the fruit extracts of C. aegyptiaca was investigated using FRAP, TAC, and DPPH as well as flavonoids and total phenols content. Because the phenolic components were more extractable using polar solvents, the antioxidant activity of the methanolic extract was found to be higher than that of the dichloromethane and hexane extracts. The IC50 value for DPPH of methanolic extract was found to be 0.041 mg·mL⁻¹. Our findings showed that C. aegyptiaca is an important source of physiologically active compounds. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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19 pages, 5922 KiB

Open AccessArticle

Structure-Based Molecular Networking for the Discovery of Anti-HBV Compounds from Saussurea lappa (Decne.) C.B Clarke

by Tao Wu, Xin-Jian Yan, Tian-Rong Yang, Yun-Fen Wang, Jing-Yi He, Yang Feng, Li-Hua Su, Hao Chen and Min Xu

Molecules 2022, 27(6), 2023; https://doi.org/10.3390/molecules27062023 - 21 Mar 2022

Cited by 5 | Viewed by 2742

Abstract

It is a crucial to find target compounds in natural product research. This study presents a concept of structure-guided isolation to find candidate active molecules from herbs. We establish a process of anti-viral sesquiterpene networking. An analysis of the networking suggested that new [...] Read more.

It is a crucial to find target compounds in natural product research. This study presents a concept of structure-guided isolation to find candidate active molecules from herbs. We establish a process of anti-viral sesquiterpene networking. An analysis of the networking suggested that new anti-HBV sesquiterpene may be attributable to eudesmane-, guaiane-, cadinane-, germacane- and bisabolane-type sesquiterpenes. In order to evaluate the efficiency of the structure-based molecular networking, ethanol extract of Saussurea lappa (Decne.) C.B Clarke was investigated, which led to the isolation of two guaiane-type (1 and 14), ten eudesmane-type (2–5 and 8–13), two chain (6 and 7) and one germacrane-type (15) sesquiterpenes, including seven new ones, lappaterpenes A–G (1–7), which are reported on herein. The absolute configurations of the new compounds were established by coupling constants, calculated ECD and ROESY correlations, as well as comparisons of optical rotation values with those of known compounds. The absolute configuration of compound 2 was further confirmed by X-ray diffraction. Compounds 1–15 were evaluated for their potency against hepatitis B virus. Compounds 4, 6, 7 and 9 showed effect on HBsAg with inhibition ratios of more than 40% at 30 μM concentrations. Compounds 14 and 15 inhibited HBsAg secretion with the values of IC₅₀ 0.73 ± 0.18 and 1.43 ± 0.54 μM, respectively. Structure-based molecular networking inspired the discovery of target compounds. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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16 pages, 5285 KiB

Open AccessArticle

Dihydrohomoplantagin and Homoplantaginin, Major Flavonoid Glycosides from Salvia plebeia R. Br. Inhibit oxLDL-Induced Endothelial Cell Injury and Restrict Atherosclerosis via Activating Nrf2 Anti-Oxidation Signal Pathway

by Ning Meng, Kai Chen, Yanhong Wang, Jiarong Hou, Wenhui Chu, Shan Xie, Fengying Yang and Chunhui Sun

Molecules 2022, 27(6), 1990; https://doi.org/10.3390/molecules27061990 - 19 Mar 2022

Cited by 22 | Viewed by 2575

Abstract

Oxidized low-density lipoprotein (oxLDL)-induced endothelium injury promotes the development of atherosclerosis. It has been reported that homoplantaginin, a flavonoid glycoside from the traditional Chinese medicine Salvia plebeia R. Br., protected vascular endothelial cells by inhibiting inflammation. However, it is undetermined whether homoplantaginin affects [...] Read more.

Oxidized low-density lipoprotein (oxLDL)-induced endothelium injury promotes the development of atherosclerosis. It has been reported that homoplantaginin, a flavonoid glycoside from the traditional Chinese medicine Salvia plebeia R. Br., protected vascular endothelial cells by inhibiting inflammation. However, it is undetermined whether homoplantaginin affects atherosclerosis. In this study, we evaluated the effect of homoplantaginin and its derivative dihydrohomoplantagin on oxLDL-induced endothelial cell injury and atherosclerosis in apoE-/- mice. Our results showedthat both dihydrohomoplantagin and homoplantaginin inhibited apoptosis and the increased level of ICAM-1 and VCAM-1 in oxLDL-stimulated HUVECs and the plaque endothelium of apoE-/- mice. Additionally, both of them restricted atherosclerosis development of apoE-/- mice. Mechanistic studies showed that oxLDL-induced the increase in ROS production, phosphorylation of ERK and nuclear translocation of NF-κB in HUVECs was significantly inhibited by the compounds. Meanwhile, these two compounds promoted Nrf2 nuclear translocation and increased the anti-oxidation downstream HO-1 protein level in HUVECs and plaque endothelium. Notably, knockdown of Nrf2 by siRNA abolished the cell protective effects of compounds and antagonized the inhibition effects of them on ROS production and NF-κB activation in oxLDL-stimulated HUVECs. Collectively, dihydrohomoplantagin and homoplantaginin protected VECs by activating Nrf2 and thus inhibited atherosclerosis in apoE-/- mice. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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12 pages, 17192 KiB

Open AccessArticle

Chemical Composition of Leaves, Stem, and Roots of Peperomia pellucida (L.) Kunth

by Paulo Wender P. Gomes, Hugo Barretto, José Diogo E. Reis, Abraão Muribeca, Alice Veloso, Carlos Albuquerque, Andrew Teixeira, Wandson Braamcamp, Sônia Pamplona, Consuelo Silva and Milton Silva

Molecules 2022, 27(6), 1847; https://doi.org/10.3390/molecules27061847 - 11 Mar 2022

Cited by 13 | Viewed by 6257

Abstract

Peperomia pellucida is a species known in the Amazon as “erva-de-jabuti” that has been used in several therapeutic applications based on folk medicine. Herein, we describe the classes, subclasses, and the main compounds of the leaves, stems, and roots from P. pellucida by [...] Read more.

Peperomia pellucida is a species known in the Amazon as “erva-de-jabuti” that has been used in several therapeutic applications based on folk medicine. Herein, we describe the classes, subclasses, and the main compounds of the leaves, stems, and roots from P. pellucida by ultra-high performance liquid chromatography coupled to high-resolution mass spectrometry associated with molecular networks, mirror plot on the GNPS library, and machine learning. These data show compounds that were annotated for the first time in the Peperomia genus, such as 2′,4′,5′-trihydroxybutyrophenonevelutin, dehydroretrofractamide C, and retrofractamide B. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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14 pages, 2008 KiB

Open AccessArticle

Curcumin-Injected Musca domestica Larval Hemolymph: Cecropin Upregulation and Potential Anticancer Effect

by Shaymaa Mahmoud, Sobhy Hassab El-Nabi, Asmaa Hawash, Hesham R. El-Seedi, Shaden A. M. Khalifa, Sami Ullah, Abdullah G. Al-Sehemi and Islam M. El-Garawani

Molecules 2022, 27(5), 1570; https://doi.org/10.3390/molecules27051570 - 27 Feb 2022

Cited by 4 | Viewed by 2771

Abstract

Over recent decades, much attention has been given to imply the natural products in cancer therapy alone or in combination with other established procedures. Insects have a rich history in traditional medicine across the globe, which holds promise for the future of natural [...] Read more.

Over recent decades, much attention has been given to imply the natural products in cancer therapy alone or in combination with other established procedures. Insects have a rich history in traditional medicine across the globe, which holds promise for the future of natural product drug discovery. Cecropins, peptides produced by insects, are components of a defense system against infections and are well known to exert antimicrobial and antitumor capabilities. The present study aimed to investigate, for the first time, the role of curcumin in enhancing the anticancer effect of Musca domestica larval hemolymph. Third larval instars of M. domestica were injected with curcumin and the hemolymph was picked at 4, 8, and 24 h post-curcumin injection. M. domestica cecropin A (MdCecA) was evaluated in control and injected larval hemolymphs. The cytotoxicity on breast cancer cell lines (MCF-7) and normal Vero cells was assessed to be comparable to control larval hemolymph. Curcumin-injected larval hemolymphs exhibited significant cytotoxicity with respect to the uninjected ones against MCF-7; however, Vero cells showed no cytotoxicity. The IC₅₀ was 106 ± 2.9 and 388 ± 9.2 μg/mL for the hemolymphs of injected larvae at 4 and 8 h, respectively, while the control larval hemolymph revealed the IC₅₀ of >500 μg/mL. For mechanistic anticancer evaluation, concentrations of 30, 60, and 100 μg/mL of curcumin-injected larval hemolymphs were examined. A significant G₂/M cell cycle arrest was observed, confirming the anti-proliferative properties of hemolymphs over the tested concentrations. The MdCecA transcripts were significantly (p < 0.05) upregulated at 4 and 8 h post-injection, while a significant downregulation was observed after 24 h. Cecropin quantification by LC–MS revealed that MdCecA peptides have the highest expression in the hemolymph of the treated larvae at 8 h relative to the control group. The upregulation of cecropin expression at mRNA and protein levels may be attributed to the curcumin stimulation and linked to the increased cytotoxicity toward the cancer cell line. In conclusion, the results suggest that the apoptotic and anti-proliferative effects of M. domestica hemolymph on MCF-7 cells following the curcumin injection can be used as a natural candidate in future pharmaceutical industries. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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10 pages, 885 KiB

Open AccessArticle

Isolation and Characterization of Two Chalcone Derivatives with Anti-Hepatitis B Virus Activity from the Endemic Socotraen Dracaena cinnabari (Dragon’s Blood Tree)

by Ramzi A. Mothana, Ahmed H. Arbab, Ali A. ElGamal, Mohammad K. Parvez and Mohammed S. Al-Dosari

Molecules 2022, 27(3), 952; https://doi.org/10.3390/molecules27030952 - 30 Jan 2022

Cited by 8 | Viewed by 3374

Abstract

Hepatitis B virus (HBV) infection is prevalent and continues to be a global health concern. In this study, we determined the anti-hepatitis B virus (HBV) potential of the Socotra-endemic medicinal plant Dracaena cinnabari and isolated and characterized the responsible constituents. A bioassay-guided fractionation [...] Read more.

Hepatitis B virus (HBV) infection is prevalent and continues to be a global health concern. In this study, we determined the anti-hepatitis B virus (HBV) potential of the Socotra-endemic medicinal plant Dracaena cinnabari and isolated and characterized the responsible constituents. A bioassay-guided fractionation using different chromatographic techniques of the methanolic extract of D. cinnabari led to the isolation of two chalcone derivatives. Using a variety of spectroscopic techniques, including ¹H-, ¹³C-, and 2D-NMR, these derivatives were identified as 2,4’-dihydroxy-4-methoxydihydrochalcone (compound 1) and 2,4’-dihydroxy-4-methoxyhydrochalcone (compound 2). Both compounds were isolated for the first time from the red resin (dragon’s blood) of D. cinnabari. The compounds were first evaluated for cytotoxicity on HepG2.2.15 cells and 50% cytotoxicity concentration (CC50) values were determined. They were then evaluated for anti-HBV activity against HepG2.2.15 cells by assessing the suppression of HBsAg and HBeAg production in the culture supernatants and their half maximum inhibitory concentration (IC₅₀) and therapeutic index (TI) values were determined. Compounds 1 and 2 indicated inhibition of HBsAg production in a dose- and time-dependent manner with IC₅₀ values of 20.56 and 6.36 μg/mL, respectively. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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14 pages, 1985 KiB

Open AccessArticle

Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall.

by Oraphan Sakulkeo, Chatchai Wattanapiromsakul, Thanet Pitakbut and Sukanya Dej-adisai

Molecules 2022, 27(3), 639; https://doi.org/10.3390/molecules27030639 - 19 Jan 2022

Cited by 25 | Viewed by 3369

Abstract

Neuropeltis racemosa Wall. (Convolvulaceae) is wildly distributed in Asia. Its stem is used as the component in traditional Thai recipes for treatments of muscle rigidity, skin disorder, dysentery, and hypoglycemia. However, the chemical constituents and biological activities of N. racemosa have not been [...] Read more.

Neuropeltis racemosa Wall. (Convolvulaceae) is wildly distributed in Asia. Its stem is used as the component in traditional Thai recipes for treatments of muscle rigidity, skin disorder, dysentery, and hypoglycemia. However, the chemical constituents and biological activities of N. racemosa have not been reported. From a screening assay, N. racemosa stem crude extract showed the potent effect on alpha-glucosidase inhibition at 2 mg/mL as 96.09%. The bioassay-guiding isolation led to 5 compounds that were identified by spectroscopic techniques as scopoletin (1), syringic acid (2), methyl 3-methyl-2-butenoate (3), N-trans-feruloyltyramine (4), and N-trans- coumaroyltyramine (5). Compounds 1, 4, and 5 exhibited an IC₅₀ of 110.97, 29.87, and 0.92 µg/mL, respectively, while the IC₅₀ of positive standard, acarbose was 272.72 µg/mL. Kinetic study showed that compound 1 performed as the mixed-type inhibition mechanism, whereas compounds 4 and 5 displayed the uncompetitive inhibition mechanism. The docking study provided the molecular understanding of isolated aromatic compounds (1, 2, 4 and 5) to alpha-glucosidase. Hence, this study would be the first report of isolated compounds and their anti-alpha-glucosidase activity with the mechanism of action from N. racemosa. Thus, these active compounds will be further studied to be the lead compounds among natural antidiabetic drugs. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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18 pages, 4516 KiB

Open AccessArticle

The In Vitro Anti-Cancer Activities and Mechanisms of Action of 9-Methoxycanthin-6-one from Eurycoma longifolia in Selected Cancer Cell Lines

by Nurhanan Murni Yunos, Nor Datiakma Mat Amin, Muhammad Haffiz Jauri, Sui Kiong Ling, Nor Hasnida Hassan and Nor Jannah Sallehudin

Molecules 2022, 27(3), 585; https://doi.org/10.3390/molecules27030585 - 18 Jan 2022

Cited by 10 | Viewed by 3545

Abstract

An alkaloid compound from the hairy root culture of Eurycoma longifolia has been isolated and characterised as 9-methoxycanthin-6-one. The aims of these studies were to investigate the in vitro anti-cancer activities of 9-methoxycanthin-6-one against ovarian cancer (A2780, SKOV-3), breast cancer (MCF-7), colorectal cancer [...] Read more.

An alkaloid compound from the hairy root culture of Eurycoma longifolia has been isolated and characterised as 9-methoxycanthin-6-one. The aims of these studies were to investigate the in vitro anti-cancer activities of 9-methoxycanthin-6-one against ovarian cancer (A2780, SKOV-3), breast cancer (MCF-7), colorectal cancer (HT29), skin cancer (A375) and cervical cancer (HeLa) cell lines by using a Sulphorhodamine B assay, and to evaluate the mechanisms of action of 9-methoxycanthin-6-one via the Hoechst 33342 assay and proteomics approach. The results had shown that 9-methoxycanthin-6-one gave IC₅₀ values of 4.04 ± 0.36 µM, 5.80 ± 0.40 µM, 15.09 ± 0.99 µM, 3.79 ± 0.069 µM, 5.71 ± 0.20 µM and 4.30 ± 0.27 µM when tested in A2780, SKOV-3, MCF-7, HT-29, A375 and HeLa cell lines, respectively. It was found that 9-methoxycanthin-6-one induced apoptosis in a concentration dependent manner when analysed via the Hoechst 33342 assay. 9-methoxycanthine-6-one were found to affect the expressions of apoptotic-related proteins, that were proteins pyruvate kinase (PKM), annexin A2 (ANXA2), galectin 3 (LGAL3), heterogeneous nuclear ribonucleoprotein A1 (HNRNP1A1), peroxiredoxin 3 (PRDX3), and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) from the differential analysis of 2-DE profiles between treated and non-treated 9-methoxycanthine-6-one. Proteins such as acetyl-CoA acyltransferase 2 (ACAA2), aldehyde dehydrogenase 1 (ALDH1A1), capping protein (CAPG), eukaryotic translation elongation factor 1 (EEF1A1), malate dehydrogenase 2 (MDH2), purine nucleoside phosphorylase (PNP), and triosephosphate isomerase 1 (TPI1) were also identified to be associated with A2780 cell death induced by 9-methoxycanthine-6-one. These findings may provide a new insight on the mechanisms of action of 9-methoxycanthin-6-one in exerting its anti-cancer effects in vitro. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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22 pages, 7203 KiB

Open AccessArticle

Beneficial Effects of Laurel (Laurus nobilis L.) and Myrtle (Myrtus communis L.) Extract on Rat Health

by Marija Berendika, Sandra Domjanić Drozdek, Dyana Odeh, Nada Oršolić, Petar Dragičević, Marijana Sokolović, Ivona Elez Garofulić, Domagoj Đikić and Irena Landeka Jurčević

Molecules 2022, 27(2), 581; https://doi.org/10.3390/molecules27020581 - 17 Jan 2022

Cited by 12 | Viewed by 4032

Abstract

Polyphenols of Laurel and Myrtle exhibit structural diversity, which affects bioavailability, metabolism, and bioactivity. The gut microbiota plays a key role in modulating the production, bioavailability and, thus the biological activities of phenolic metabolites, particularly after the intake of food containing high-molecular-weight polyphenols. [...] Read more.

Polyphenols of Laurel and Myrtle exhibit structural diversity, which affects bioavailability, metabolism, and bioactivity. The gut microbiota plays a key role in modulating the production, bioavailability and, thus the biological activities of phenolic metabolites, particularly after the intake of food containing high-molecular-weight polyphenols. The aim of this study was to investigate whether the polyphenolic components of Laurel and Myrtle aqueous extract have beneficial effects on rat health. The growth of lactic acid bacteria (LAB), β-glucuronidase, β-glucosidase, β-galactosidase activity, pH value, body weight change and food efficacy ratio after intragastric treatment of rats with Laurel and Myrtle extract at doses of 50 and 100 mg/kg for two weeks were investigated. The endogenous populations of colonic probiotic bacteria (Lactobacilli and Bifidobacteria) were counted on selective media. According to the obtained data, Laurel extract in the applied dose of 50 and 100 and Myrtle extract (100 mg/kg) positively affects the rats health by increasing the number of colonies of Lactobacilli and Bifidobacteria compared to the control group, causes changes in glycolytic enzymatic activity and minor change in antioxidative tissue activity. In addition, high doses of Laurel increase food efficiency ratio, while Myrtle has the same effect at a lower dose. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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18 pages, 2837 KiB

Open AccessArticle

Antioxidant Activity and Mechanism of Resveratrol and Polydatin Isolated from Mulberry (Morus alba L.)

by Ziwei Li, Xiaoman Chen, Guo Liu, Jun Li, Jinglin Zhang, Yong Cao and Jianyin Miao

Molecules 2021, 26(24), 7574; https://doi.org/10.3390/molecules26247574 - 14 Dec 2021

Cited by 39 | Viewed by 3985

Abstract

Natural stilbenes have unique physiological effects, such as anti-senile dementia, anti-cancer, anti-bacterial, lowering blood lipid, and other important biological functions, which have attracted great attention from scholars in recent years. In this study, two stilbene compounds, resveratrol (RES) and polydatin (PD), were isolated [...] Read more.

Natural stilbenes have unique physiological effects, such as anti-senile dementia, anti-cancer, anti-bacterial, lowering blood lipid, and other important biological functions, which have attracted great attention from scholars in recent years. In this study, two stilbene compounds, resveratrol (RES) and polydatin (PD), were isolated from Mulberry (Morus alba L.), and their antioxidant activity and mechanism were investigated. The results showed that the contents of RES and PD in mulberry roots were 32.45 and 3.15 μg/g, respectively, significantly higher than those in mulberry fruits (0.48 and 0.0020 μg/g) and mulberry branches (5.70 and 0.33 μg/g). Both RES and PD showed high antioxidant potential by DPPH, ABTS free-scavenging methods, and ORAC assay, and provided protection against oxidative damage in HepG2 cells by increased catalase (CAT) activity, superoxide dismutase (SOD) activity, and Glutathione (GSH) content, and decreasing generation of reactive oxygen species (ROS), lactate dehydrogenase (LDH) level, and malondialdehyde (MDA) content. Therefore, RES and PD treatment could be effective for attenuating AAPH-induced oxidative stress in HepG2 cells. This study will promote the development and application of stilbene compounds. Furthermore, the RES and PD could be used as antioxidant supplements in functional foods, cosmetics, or pharmaceuticals, contributing to health improvement. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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22 pages, 20208 KiB

Open AccessArticle

Polyphenolic QTOF-ESI MS Characterization and the Antioxidant and Cytotoxic Activities of Prunus domestica Commercial Cultivars from Costa Rica

by Mirtha Navarro-Hoyos, Elizabeth Arnáez-Serrano, Silvia Quesada-Mora, Gabriela Azofeifa-Cordero, Krissia Wilhelm-Romero, María Isabel Quirós-Fallas, Diego Alvarado-Corella, Felipe Vargas-Huertas and Andrés Sánchez-Kopper

Molecules 2021, 26(21), 6493; https://doi.org/10.3390/molecules26216493 - 27 Oct 2021

Cited by 13 | Viewed by 2842

Abstract

There is an increased interest in plum research because of their metabolites’ potential bioactivities. In this study, the phenolic profiles of Prunus domestica commercial cultivars (Methley, Pisardii and Satsuma) in Costa Rica were determined by Ultra Performance Liquid Chromatography coupled with High Resolution [...] Read more.

There is an increased interest in plum research because of their metabolites’ potential bioactivities. In this study, the phenolic profiles of Prunus domestica commercial cultivars (Methley, Pisardii and Satsuma) in Costa Rica were determined by Ultra Performance Liquid Chromatography coupled with High Resolution Mass Spectrometry using a quadrupole-time-of-flight analyzer (UPLC-ESI-QTOF MS) on enriched phenolic extracts obtained through Pressurized Liquid Extraction (PLE) under acidic and neutral extraction conditions. In total, 41 different phenolic compounds were identified in the skin and flesh extracts, comprising 11 flavan-3-ols, 14 flavonoids and 16 hydroxycinnamic acids and derivatives. Neutral extractions for the skins and flesh from all of the cultivars yielded a larger number of compounds, and were particularly rich in the number of procyanidin trimers and tetramers when compared to the acid extractions. The total phenolic content (TPC) and antioxidant potential using the DPPH and ORAC methods exhibited better results for neutral extracts with Satsuma skins and Methley flesh, which showed the best values (685.0 and 801.6 mg GAE/g extract; IC₅₀ = 4.85 and 4.39 µg/mL; and 12.55 and 12.22 mmol TE/g extract, respectively). A Two-Way ANOVA for cytotoxicity towards AGS gastric adenocarcinoma and SW620 colon adenocarcinoma indicated a significant difference (p < 0.05) for PLE conditions, with better results for neutral extractions, with Satsuma skin delivering the best results (IC₅₀ = 60.7 and 46.7 µg/mL respectively) along with Methley flesh (IC₅₀ = 76.3 and 60.9 µg/mL, respectively). In addition, a significant positive correlation was found between TPC and ORAC (r = 0.929, p < 0.05), as well as a significant negative correlation (p < 0.05) between TPC and cytotoxicity towards AGS and SW620 cell lines (r = −0.776, and −0.751, respectively). A particularly high, significant, negative correlation (p < 0.05) was found between the number of procyanidins and cytotoxicity against the AGS (r = −0.868) and SW620 (r = −0.855) cell lines. Finally, the PCA clearly corroborated that neutral extracts are a more homogenous group exhibiting higher antioxidant and cytotoxic results regardless of the part or cultivar; therefore, our findings suggest that PLE extracts under neutral conditions would be of interest for further studies on their potential health benefits. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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10 pages, 2264 KiB

Open AccessArticle

Antispasmodic Effect of Asperidine B, a Pyrrolidine Derivative, through Inhibition of L-Type Ca²⁺ Channel in Rat Ileal Smooth Muscle

by Acharaporn Duangjai, Vatcharin Rukachaisirikul, Yaowapa Sukpondma, Chutima Srimaroeng and Chatchai Muanprasat

Molecules 2021, 26(18), 5492; https://doi.org/10.3390/molecules26185492 - 9 Sep 2021

Cited by 2 | Viewed by 2576

Abstract

Antispasmodic agents are used for modulating gastrointestinal motility. Several compounds isolated from terrestrial plants have antispasmodic properties. This study aimed to explore the inhibitory effect of the pyrrolidine derivative, asperidine B, isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, on spasmodic activity. Isolated [...] Read more.

Antispasmodic agents are used for modulating gastrointestinal motility. Several compounds isolated from terrestrial plants have antispasmodic properties. This study aimed to explore the inhibitory effect of the pyrrolidine derivative, asperidine B, isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, on spasmodic activity. Isolated rat ileum was set up in an organ bath. The contractile responses of asperidine B (0.3 to 30 µM) on potassium chloride and acetylcholine-induced contractions were recorded. To investigate its antispasmodic mechanism, CaCl₂, acetylcholine, Nω-nitro-l-arginine methyl ester (l-NAME), nifedipine, methylene blue and tetraethylammonium chloride (TEA) were tested in the absence or in the presence of asperidine B. Cumulative concentrations of asperidine B reduced the ileal contraction by ~37%. The calcium chloride and acetylcholine-induced ileal contraction was suppressed by asperidine B. The effects of asperidine B combined with nifedipine, atropine or TEA were similar to those treated with nifedipine, atropine or TEA, respectively. In contrast, in the presence of l-NAME and methylene blue, the antispasmodic effect of asperidine B was unaltered. These results suggest that the antispasmodic property of asperidine B is probably due to the blockage of the L-type Ca²⁺ channel and is associated with K⁺ channels and muscarinic receptor, possibly by affecting non-selective cation channels and/or releasing intracellular calcium. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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12 pages, 4795 KiB

Open AccessArticle

Dried Destoned Virgin Olive Pomace: A Promising New By-Product from Pomace Extraction Process

by Cinzia Benincasa, Massimiliano Pellegrino, Lucia Veltri, Salvatore Claps, Carmelo Fallara and Enzo Perri

Molecules 2021, 26(14), 4337; https://doi.org/10.3390/molecules26144337 - 17 Jul 2021

Cited by 6 | Viewed by 3622

Abstract

At present the olive oil industry produces large amounts of secondary products once considered waste or by-products. In this paper, we present, for the first time, a new interesting olive by-product named “dried destoned virgin olive pomace” (DDVOP), produced by the pomace oil [...] Read more.

At present the olive oil industry produces large amounts of secondary products once considered waste or by-products. In this paper, we present, for the first time, a new interesting olive by-product named “dried destoned virgin olive pomace” (DDVOP), produced by the pomace oil industry. The production of DDVOP is possible thanks to the use of a new system that differs from the traditional ones by having the dryer set at a lower temperature value, 350 °C instead of 550 °C, and by avoiding the solvent extraction phase. In order to evaluate if DDVOP may be suitable as a new innovative feeding integrator for animal feed, its chemical characteristics were investigated. Results demonstrated that DDVOP is a good source of raw protein and precious fiber; that it is consistent in total phenols (6156 mg/kg); rich in oleic (72.29%), linoleic (8.37%) acids and tocopherols (8.80 mg/kg). A feeding trial was, therefore, carried out on sheep with the scope of investigating the influence of the diet on the quality of milk obtained from sheep fed with DDVOP-enriched feed. The resulting milk was enriched in polyunsaturated (0.21%) and unsaturated (2.42%) fatty acids; and had increased levels of phenols (10.35 mg/kg) and tocopherols (1.03 mg/kg). Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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9 pages, 1131 KiB

Open AccessCommunication

A Standardized Extract Prepared from Red Orange and Lemon Wastes Blocks High-Fat Diet-Induced Hyperglycemia and Hyperlipidemia in Mice

by Santina Chiechio, Magda Zammataro, Massimo Barresi, Margherita Amenta, Gabriele Ballistreri, Simona Fabroni and Paolo Rapisarda

Molecules 2021, 26(14), 4291; https://doi.org/10.3390/molecules26144291 - 15 Jul 2021

Cited by 15 | Viewed by 3024

Abstract

Citrus fruits are a rich source of high-value bioactive compounds and their consumption has been associated with beneficial effects on human health. Red (blood) oranges (Citrus sinensis L. Osbeck) are particularly rich in anthocyanins (95% of which are represented by cyanidin-3-glucoside and [...] Read more.

Citrus fruits are a rich source of high-value bioactive compounds and their consumption has been associated with beneficial effects on human health. Red (blood) oranges (Citrus sinensis L. Osbeck) are particularly rich in anthocyanins (95% of which are represented by cyanidin-3-glucoside and cyanidin-3-6″-malonyl-glucoside), flavanones (hesperidin, narirutin, and didymin), and hydroxycinnamic acids (caffeic acid, coumaric acid, sinapic, and ferulic acid). Lemon fruit (Citrus limon) is also rich in flavanones (eriocitrin, hesperidin, and diosmin) and other polyphenols. All of these compounds are believed to play a very important role as dietary antioxidants due to their ability to scavenge free radicals. A standardized powder extract, red orange and lemon extract (RLE), was obtained by properly mixing anthocyanins and other polyphenols recovered from red orange processing waste with eriocitrin and other flavanones recovered from lemon peel by a patented extraction process. RLE was used for in vivo assays aimed at testing a potential beneficial effect on glucose and lipid metabolism. In vivo experiments performed on male CD1 mice fed with a high-fat diet showed that an 8-week treatment with RLE was able to induce a significant reduction in glucose, cholesterol and triglycerides levels in the blood, with positive effects on regulation of hyperglycemia and lipid metabolism, thus suggesting a potential use of this new phytoextract for nutraceutical purposes. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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13 pages, 1587 KiB

Open AccessArticle

Benzylated Dihydroflavones and Isoquinoline-Derived Alkaloids from the Bark of Diclinanona calycina (Annonaceae) and Their Cytotoxicities

by Emmanoel V. Costa, Liviane do N. Soares, Jamal da Silva Chaar, Valdenizia R. Silva, Luciano de S. Santos, Hector H. F. Koolen, Felipe M. A. da Silva, Josean F. Tavares, Gokhan Zengin, Milena B. P. Soares and Daniel P. Bezerra

Molecules 2021, 26(12), 3714; https://doi.org/10.3390/molecules26123714 - 18 Jun 2021

Cited by 12 | Viewed by 4627

Abstract

Diclinanona calycina R. E. Fries popularly known as “envira”, is a species of the Annonaceae family endemic to Brazil. In our ongoing search for bioactive compounds from Annonaceae Amazon plants, the bark of D. calycina was investigated by classical chromatography techniques that yielded [...] Read more.

Diclinanona calycina R. E. Fries popularly known as “envira”, is a species of the Annonaceae family endemic to Brazil. In our ongoing search for bioactive compounds from Annonaceae Amazon plants, the bark of D. calycina was investigated by classical chromatography techniques that yielded thirteen compounds (alkaloids and flavonoids) described for the first time in D. calycina as well as in the genus Diclinanona. The structure of these isolated compounds were established by extensive analysis using 1D/2D-NMR spectroscopy in combination with MS. The isolated alkaloids were identified as belonging to the subclasses: simple isoquinoline, thalifoline (1); aporphine, anonaine (2); oxoaporphine, liriodenine (3); benzyltetrahydroisoquinolines, (S)-(+)-reticuline (4); dehydro-oxonorreticuline (3,4-dihydro-7-hydroxy-6-methoxy-1-isoquinolinyl)(3-hydroxy-4-methoxyphenyl)-methanone) (5); (+)-1S,2R-reticuline N_β-oxide (6); and (+)-1S,2S-reticuline N_α-oxide (7); tetrahydroprotoberberine, coreximine (8); and pavine, bisnorargemonine (9). While the flavonoids belong to the benzylated dihydroflavones, isochamanetin (10), dichamanetin (11), and a mixture of uvarinol (12) and isouvarinol (13). Compound 5 is described for the first time in the literature as a natural product. The cytotoxic activity of the main isolated compounds was evaluated against cancer and non-cancerous cell lines. Among the tested compounds, the most promising results were found for the benzylated dihydroflavones dichamanetin (10), and the mixture of uvarinol (12) and isouvarinol (13), which presented moderate cytotoxic activity against the tested cancer cell lines (<20.0 µg·mL⁻¹) and low cytotoxicity against the non-cancerous cell line MRC-5 (>25.0 µg·mL⁻¹). Dichamanetin (11) showed cytotoxic activity against HL-60 and HCT116 with IC₅₀ values of 15.78 µg·mL⁻¹ (33.70 µmol·L⁻¹) and 18.99 µg·mL⁻¹ (40.56 µmol·L⁻¹), respectively while the mixture of uvarinol (12) and isouvarinol (13) demonstrated cytotoxic activity against HL-60, with an IC₅₀ value of 9.74 µg·mL⁻¹, and HCT116, with an IC₅₀ value of 17.31 µg·mL⁻¹. These cytotoxic activities can be attributed to the presence of one or more hydroxybenzyl groups present in these molecules as well as the position in which these groups are linked. The cytotoxic activities of reticuline, anonaine and liriodenine have been previously established, with liriodenine being the most potent compound. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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Review

Jump to: Research, Other

18 pages, 1440 KiB

Open AccessReview

Natural Dietary Compounds in the Treatment of Arsenic Toxicity

by Geir Bjørklund, Md. Shiblur Rahaman, Mariia Shanaida, Roman Lysiuk, Petro Oliynyk, Larysa Lenchyk, Salvatore Chirumbolo, Christos T. Chasapis and Massimiliano Peana

Molecules 2022, 27(15), 4871; https://doi.org/10.3390/molecules27154871 - 29 Jul 2022

Cited by 27 | Viewed by 4104

Abstract

Chronic exposure to arsenic (As) compounds leads to its accumulation in the body, with skin lesions and cancer being the most typical outcomes. Treating As-induced diseases continues to be challenging as there is no specific, safe, and efficacious therapeutic management. Therapeutic and preventive [...] Read more.

Chronic exposure to arsenic (As) compounds leads to its accumulation in the body, with skin lesions and cancer being the most typical outcomes. Treating As-induced diseases continues to be challenging as there is no specific, safe, and efficacious therapeutic management. Therapeutic and preventive measures available to combat As toxicity refer to chelation therapy, antioxidant therapy, and the intake of natural dietary compounds. Although chelation therapy is the most commonly used method for detoxifying As, it has several side effects resulting in various toxicities such as hepatotoxicity, neurotoxicity, and other adverse consequences. Drugs of plant origin and natural dietary compounds show efficient and progressive relief from As-mediated toxicity without any particular side effects. These natural compounds have also been found to aid the elimination of As from the body and, therefore, can be more effective than conventional therapeutic agents in ameliorating As toxicity. This review provides an overview of the recently updated knowledge on treating As poisoning through natural dietary compounds. This updated information may serve as a basis for defining novel prophylactic and therapeutic formulations. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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41 pages, 22468 KiB

Open AccessReview

Polyphenols for the Treatment of Ischemic Stroke: New Applications and Insights

by Shuhan Liu, Feng Lin, Jian Wang, Xiaoqiang Pan, Liguang Sun and Wei Wu

Molecules 2022, 27(13), 4181; https://doi.org/10.3390/molecules27134181 - 29 Jun 2022

Cited by 7 | Viewed by 4243

Abstract

Ischemic stroke (IS) is a leading cause of death and disability worldwide. Currently, the main therapeutic strategy involves the use of intravenous thrombolysis to restore cerebral blood flow to prevent the transition of the penumbra to the infarct core. However, due to various [...] Read more.

Ischemic stroke (IS) is a leading cause of death and disability worldwide. Currently, the main therapeutic strategy involves the use of intravenous thrombolysis to restore cerebral blood flow to prevent the transition of the penumbra to the infarct core. However, due to various limitations and complications, including the narrow time window in which this approach is effective, less than 10% of patients benefit from such therapy. Thus, there is an urgent need for alternative therapeutic strategies, with neuroprotection against the ischemic cascade response after IS being one of the most promising options. In the past few decades, polyphenolic compounds have shown great potential in animal models of IS because of their high biocompatibility and ability to target multiple ischemic cascade signaling pathways, although low bioavailability is an issue that limits the applications of several polyphenols. Here, we review the pathophysiological changes following cerebral ischemia and summarize the research progress regarding the applications of polyphenolic compounds in the treatment of IS over the past 5 years. Furthermore, we discuss several potential strategies for improving the bioavailability of polyphenolic compounds as well as some essential issues that remain to be addressed for the translation of the related therapies to the clinic. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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19 pages, 1750 KiB

Open AccessReview

Effects of Frankincense Compounds on Infection, Inflammation, and Oral Health

by Cássio Luiz Coutinho Almeida-da-Silva, Nallusamy Sivakumar, Homer Asadi, Anna Chang-Chien, M. Walid Qoronfleh, David M. Ojcius and Musthafa Mohamed Essa

Molecules 2022, 27(13), 4174; https://doi.org/10.3390/molecules27134174 - 29 Jun 2022

Cited by 16 | Viewed by 15445

Abstract

Boswellia trees, found throughout the Middle East and parts of Africa and Asia, are the source of frankincense oil. Since antiquity, frankincense has been traded as a precious commodity, but it has also been used for the treatment of chronic disease, inflammation, oral [...] Read more.

Boswellia trees, found throughout the Middle East and parts of Africa and Asia, are the source of frankincense oil. Since antiquity, frankincense has been traded as a precious commodity, but it has also been used for the treatment of chronic disease, inflammation, oral health, and microbial infection. More recently, the bioactive components of Boswellia trees have been identified and characterized for their effects on cancer, microbial infection (especially infection by oral pathogens), and inflammation. Most studies have focused on cell lines, but more recent research has also investigated effects in animal models of disease. As natural products are considered to be safer than synthetic drugs, there is growing interest in further developing the use of substances such as frankincense oil for therapeutic treatment. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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27 pages, 3586 KiB

Open AccessReview

Involvement of Phytochemical-Encapsulated Nanoparticles’ Interaction with Cellular Signalling in the Amelioration of Benign and Malignant Brain Tumours

by Sidharth Mehan, Navneet Arora, Sonalika Bhalla, Andleeb Khan, Muneeb U Rehman, Badrah S. Alghamdi, Torki Al Zughaibi and Ghulam Md Ashraf

Molecules 2022, 27(11), 3561; https://doi.org/10.3390/molecules27113561 - 1 Jun 2022

Cited by 7 | Viewed by 3759

Abstract

Brain tumours have unresolved challenges that include delay prognosis and lower patient survival rate. The increased understanding of the molecular pathways underlying cancer progression has aided in developing various anticancer medications. Brain cancer is the most malignant and invasive type of cancer, with [...] Read more.

Brain tumours have unresolved challenges that include delay prognosis and lower patient survival rate. The increased understanding of the molecular pathways underlying cancer progression has aided in developing various anticancer medications. Brain cancer is the most malignant and invasive type of cancer, with several subtypes. According to the WHO, they are classified as ependymal tumours, chordomas, gangliocytomas, medulloblastomas, oligodendroglial tumours, diffuse astrocytomas, and other astrocytic tumours on the basis of their heterogeneity and molecular mechanisms. The present study is based on the most recent research trends, emphasising glioblastoma cells classified as astrocytoma. Brain cancer treatment is hindered by the failure of drugs to cross the blood–brain barrier (BBB), which is highly impregnableto foreign molecule entry. Moreover, currently available medications frequently fail to cross the BBB, whereas chemotherapy and radiotherapy are too expensive to be afforded by an average incomeperson and have many associated side effects. When compared to our current understanding of molecularly targeted chemotherapeutic agents, it appears that investigating the efficacy of specific phytochemicals in cancer treatment may be beneficial. Plants and their derivatives are game changers because they are efficacious, affordable, environmentally friendly, faster, and less toxic for the treatment of benign and malignant tumours. Over the past few years, nanotechnology has made a steady progress in diagnosing and treating cancers, particularly brain tumours. This article discusses the effects of phytochemicals encapsulated in nanoparticles on molecular targets in brain tumours, along with their limitations and potential challenges. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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25 pages, 2386 KiB

Open AccessReview

Phytotherapy in Integrative Oncology—An Update of Promising Treatment Options

by Amy M. Zimmermann-Klemd, Jakob K. Reinhardt, Moritz Winker and Carsten Gründemann

Molecules 2022, 27(10), 3209; https://doi.org/10.3390/molecules27103209 - 17 May 2022

Cited by 14 | Viewed by 5881

Abstract

Modern phytotherapy is part of today’s conventional evidence-based medicine and the use of phytopharmaceuticals in integrative oncology is becoming increasingly popular. Approximately 40% of users of such phytopharmaceuticals are tumour patients. The present review provides an overview of the most important plants and [...] Read more.

Modern phytotherapy is part of today’s conventional evidence-based medicine and the use of phytopharmaceuticals in integrative oncology is becoming increasingly popular. Approximately 40% of users of such phytopharmaceuticals are tumour patients. The present review provides an overview of the most important plants and nature-based compounds used in integrative oncology and illustrates their pharmacological potential in preclinical and clinical settings. A selection of promising anti-tumour plants and ingredients was made on the basis of scientific evidence and therapeutic practical relevance and included Boswellia, gingko, ginseng, ginger, and curcumin. In addition to these nominees, there is a large number of other interesting plants and plant ingredients that can be considered for the treatment of cancer diseases or for the treatment of tumour or tumour therapy-associated symptoms. Side effects and interactions are included in the discussion. However, with the regular and intended use of phytopharmaceuticals, the occurrence of adverse side effects is rather rare. Overall, the use of defined phytopharmaceuticals is recommended in the context of a rational integrative oncology approach. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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19 pages, 1775 KiB

Open AccessReview

Nutraceutic Potential of Bioactive Compounds of Eugenia dysenterica DC in Metabolic Alterations

by Lidiani Figueiredo Santana, Sandramara Sasso, Diana Figueiredo Santana Aquino, Karine de Cássia Freitas, Rita de Cássia Avellaneda Guimarães, Arnildo Pott, Valter Aragão do Nascimento, Danielle Bogo, Patrícia de Oliveira Figueiredo and Priscila Aiko Hiane

Molecules 2022, 27(8), 2477; https://doi.org/10.3390/molecules27082477 - 12 Apr 2022

Cited by 4 | Viewed by 2661

Abstract

The fruit and leaves of Eugenia dysenterica DC., locally known as cagaita, are rich in antioxidant glycosylated quercetin derivatives and phenolic compounds that have beneficial effects on diabetes mellitus, hypertension and general inflammation. We conducted a literature search to investigate the nutraceutical [...] Read more.

The fruit and leaves of Eugenia dysenterica DC., locally known as cagaita, are rich in antioxidant glycosylated quercetin derivatives and phenolic compounds that have beneficial effects on diabetes mellitus, hypertension and general inflammation. We conducted a literature search to investigate the nutraceutical potentials of these phenolic compounds for treating obesity, diabetes mellitus and intestinal inflammatory disease. The phenolic compounds in E. dysenterica have demonstrated effects on carbohydrate metabolism, which can prevent the development of these chronic diseases and reduce LDL (low-density lipoprotein) cholesterol and hypertension. E. dysenterica also improves intestinal motility and microbiota and protects gastric mucosa, thereby preventing inflammation. However, studies are necessary to identify the mechanism by which E. dysenterica nutraceutical compounds act on such pathological processes to support future research. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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17 pages, 1788 KiB

Open AccessReview

Plants Used in Mexican Traditional Medicine for the Management of Urolithiasis: A Review of Preclinical Evidence, Bioactive Compounds, and Molecular Mechanisms

by Delia Sansores-España, Alfredo Geovanny Pech-Aguilar, Karol Guadalupe Cua-Pech, Isabel Medina-Vera, Martha Guevara-Cruz, Ana Ligia Gutiérrez-Solis, Juan G. Reyes-García and Azalia Avila-Nava

Molecules 2022, 27(6), 2008; https://doi.org/10.3390/molecules27062008 - 21 Mar 2022

Cited by 15 | Viewed by 5938

Abstract

Urolithiasis (UL) involves the formation of stones in different parts of the urinary tract. UL is a health problem, and its prevalence has increased considerably in developing countries. Several regions use plants in traditional medicine as an alternative in the treatment or prevention [...] Read more.

Urolithiasis (UL) involves the formation of stones in different parts of the urinary tract. UL is a health problem, and its prevalence has increased considerably in developing countries. Several regions use plants in traditional medicine as an alternative in the treatment or prevention of UL. Mexico has known about the role of traditional medicine in the management of urinary stones. Mexican traditional medicine uses plants such as Argemone mexicana L., Berberis trifoliata Hartw. ex Lindl., Costus mexicanus Liebm, Chenopodium album L., Ammi visnaga (L.) Lam., Eysenhardtia polystachya (Ortega) Sarg., Selaginella lepidophylla (Hook. & Grev.) Spring, and Taraxacum officinale L. These plants contain different bioactive compounds, including polyphenols, flavonoids, phytosterols, saponins, furanochromones, alkaloids, and terpenoids, which could be effective in preventing the process of stone formation. Evidence suggests that their beneficial effects might be associated with litholytic, antispasmodic, and diuretic activities, as well as an inhibitory effect on crystallization, nucleation, and aggregation of crystals. The molecular mechanisms involving these effects could be related to antioxidant, anti-inflammatory, and antimicrobial properties. Thus, the review aims to summarize the preclinical evidence, bioactive compounds, and molecular mechanisms of the plants used in Mexican traditional medicine for the management of UL. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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11 pages, 2142 KiB

Open AccessReview

Antiviral Plants from Marajó Island, Brazilian Amazon: A Narrative Review

by Paulo Wender P. Gomes, Luiza Martins, Emilli Gomes, Abraão Muribeca, Sônia Pamplona, Andrea Komesu, Carissa Bichara, Mahendra Rai, Consuelo Silva and Milton Silva

Molecules 2022, 27(5), 1542; https://doi.org/10.3390/molecules27051542 - 24 Feb 2022

Cited by 9 | Viewed by 3171

Abstract

Diseases caused by viruses are a global threat, resulting in serious medical and social problems for humanity. They are the main contributors to many minor and major outbreaks, epidemics, and pandemics worldwide. Over the years, medicinal plants have been used as a complementary [...] Read more.

Diseases caused by viruses are a global threat, resulting in serious medical and social problems for humanity. They are the main contributors to many minor and major outbreaks, epidemics, and pandemics worldwide. Over the years, medicinal plants have been used as a complementary treatment in a range of diseases. In this sense, this review addresses promising antiviral plants from Marajó island, a part of the Amazon region, which is known to present a very wide biodiversity of medicinal plants. The present review has been limited to articles and abstracts available in Scopus, Web of Science, Science Direct, Scielo, PubMed, and Google Scholar, as well as the patent offices in Brazil (INPI), United States (USPTO), Europe (EPO) and World Intellectual Property Organization (WIPO). As a result, some plants from Marajó island were reported to have actions against HIV-1,2, HSV-1,2, SARS-CoV-2, HAV and HBV, Poliovirus, and influenza. Our major conclusion is that plants of the Marajó region show promising perspectives regarding pharmacological potential in combatting future viral diseases. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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15 pages, 9340 KiB

Open AccessReview

The Bioavailability and Biological Activities of Phytosterols as Modulators of Cholesterol Metabolism

by Xiang Li, Yan Xin, Yuqian Mo, Pavel Marozik, Taiping He and Honghui Guo

Molecules 2022, 27(2), 523; https://doi.org/10.3390/molecules27020523 - 14 Jan 2022

Cited by 82 | Viewed by 8882

Abstract

Phytosterols are natural sterols widely found in plants that have a variety of physiological functions, and their role in reducing cholesterol absorption has garnered much attention. Although the bioavailability of phytosterols is only 0.5–2%, they can still promote cholesterol balance in the body. [...] Read more.

Phytosterols are natural sterols widely found in plants that have a variety of physiological functions, and their role in reducing cholesterol absorption has garnered much attention. Although the bioavailability of phytosterols is only 0.5–2%, they can still promote cholesterol balance in the body. A mechanism of phytosterols for lowering cholesterol has now been proposed. They not only reduce the uptake of cholesterol in the intestinal lumen and affect its transport, but also regulate the metabolism of cholesterol in the liver. In addition, phytosterols can significantly reduce the plasma concentration of total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C), with a dose-response relationship. Ingestion of 3 g of phytosterols per day can reach the platform period, and this dose can reduce LDL-C by about 10.7%. On the other hand, phytosterols can also activate the liver X receptor α-CPY7A1 mediated bile acids excretion pathway and accelerate the transformation and metabolism of cholesterol. This article reviews the research progress of phytosterols as a molecular regulator of cholesterol and the mechanism of action for this pharmacological effect. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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12 pages, 1400 KiB

Open AccessReview

The Analgesic Properties of Corydalis yanhusuo

by Lamees Alhassen, Travis Dabbous, Allyssa Ha, Leon Hoang Lam Dang and Olivier Civelli

Molecules 2021, 26(24), 7498; https://doi.org/10.3390/molecules26247498 - 10 Dec 2021

Cited by 19 | Viewed by 5407

Abstract

Corydalis yanhusuo extract (YHS) has been used for centuries across Asia for pain relief. The extract is made up of more than 160 compounds and has been identified as alkaloids, organic acids, volatile oils, amino acids, alcohols, and sugars. However, the most crucial [...] Read more.

Corydalis yanhusuo extract (YHS) has been used for centuries across Asia for pain relief. The extract is made up of more than 160 compounds and has been identified as alkaloids, organic acids, volatile oils, amino acids, alcohols, and sugars. However, the most crucial biological active constituents of YHS are alkaloids; more than 80 have been isolated and identified. This review paper aims to provide a comprehensive review of the phytochemical and pharmacological effects of these alkaloids that have significant ties to analgesia. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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5 pages, 459 KiB

Open AccessBrief Report

Bioactive Compounds from Lemon (Citrus limon) Extract Overcome TNF-α-Induced Insulin Resistance in Cultured Adipocytes

by Valeria Sorrenti, Valeria Consoli, Salvo Grosso, Marco Raffaele, Margherita Amenta, Gabriele Ballistreri, Simona Fabroni, Paolo Rapisarda and Luca Vanella

Molecules 2021, 26(15), 4411; https://doi.org/10.3390/molecules26154411 - 21 Jul 2021

Cited by 5 | Viewed by 3494

Abstract

The consumption of plant-based food is important for health promotion, especially regarding the prevention and management of chronic diseases such as diabetes. We investigated the effects of a lemon extract (LE), containing ≥20.0% total flavanones and ≥1.0% total hydroxycinnamic acids, on insulin signaling [...] Read more.

The consumption of plant-based food is important for health promotion, especially regarding the prevention and management of chronic diseases such as diabetes. We investigated the effects of a lemon extract (LE), containing ≥20.0% total flavanones and ≥1.0% total hydroxycinnamic acids, on insulin signaling in murine 3T3-L1 adipocytes treated with TNF-α, which was used to mimic in vitro the insulin resistance condition that characterizes diabetes mellitus. Our results showed LE increased PPARγ, GLUT4 and DGAT-1 levels, demonstrating the potential of this lemon extract in the management of insulin resistance conditions associated with TNF-α pathway activation. LE treatment further decreased the release of interleukin 6 (IL-6) and restored triglyceride synthesis, which is the main feature of a healthy adipocyte. Full article

(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 2nd Edition)

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