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Bioactive Phenolics and Polyphenols 2018

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (31 January 2018) | Viewed by 199828

Special Issue Editors

Department of Horticultural Sciences, Texas A&M University, College Station, TX 77843-2133, USA
Interests: secondary metabolism of plants under stress conditions; functional foods and cell molecular targets; postharvest biology and technology
Special Issues, Collections and Topics in MDPI journals
Centro de Biotecnología-FEMSA, School of Engineering and Sciences. Tecnológico de Monterrey. E. Garza Sada 2501 Sur, C.P. 64849, Monterrey, N.L., Mexico
Interests: phenolics biosynthesis; methods of analysis; antioxidant activity; non-thermal processing technologies; extraction and purification techniques; postharvest physiology; postharvest stress responses
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue, Bioactive Phenolics and Polyphenols 2018, will cover a selection of recent research topics and current review articles in the field of bioactive phenolics and polyphenols. Experimental papers, up-to-date review articles, and commentaries are all welcome.

The scientific interest in plant phenolics as chemopreventive and therapeutic agents against chronic and degenerative diseases has been increasing since the late 1990s, when the French paradox was associated to the high intake of polyphenols present in red wine. Since then, research advances include their biosynthesis, biological activities, purification, and chemical characterization in different plant species. Furthermore, research on the stability of phenolics in food processing techniques and storage is an area of major interest.

Contributions to this Special Issue, may cover all aspects of phenolics and polyphenols including: not only their chemical characterization on different plant species; methods for their extraction, purification, and quantification; but also elucidation of their mechanism of action; development of innovative methods for the evaluation of their bioactivity in vitro and in vivo; evaluation of their stability to thermal and non-thermal food processing techniques; elicitation of plant phenolic biosynthesis pathway; and effect of postharvest handling on the phenolic profiles of plant foods. Papers regarding the development of food products and dietary supplements enriched with plant phenolics will be also taken into consideration.

Prof. Dr. Luis Cisneros-Zevallos
Prof. Dr. Daniel Jacobo-Velazquez
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • Phenolic metabolism

  • Biological activities

  • Stability to food processing

  • Elicitation

  • Methods of analysis

  • Dietary supplements

  • Nutraceutical ingredients

  • Non-thermal processing

  • Extraction and purification

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Published Papers (27 papers)

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Editorial

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4 pages, 226 KiB  
Editorial
Bioactive Phenolics and Polyphenols: Current Advances and Future Trends
by Daniel A. Jacobo-Velázquez and Luis Cisneros-Zevallos
Int. J. Mol. Sci. 2020, 21(17), 6142; https://doi.org/10.3390/ijms21176142 - 26 Aug 2020
Cited by 6 | Viewed by 2284
Abstract
Phenolic compounds are secondary plant metabolites with remarkable health-promoting properties [...] Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)

Research

Jump to: Editorial, Review

16 pages, 3324 KiB  
Article
Ellagic Acid and Urolithins A and B Differentially Regulate Fat Accumulation and Inflammation in 3T3-L1 Adipocytes While Not Affecting Adipogenesis and Insulin Sensitivity
by Luis Cisneros-Zevallos, Woo Young Bang and Claudia Delgadillo-Puga
Int. J. Mol. Sci. 2020, 21(6), 2086; https://doi.org/10.3390/ijms21062086 - 18 Mar 2020
Cited by 26 | Viewed by 4424
Abstract
Ellagic acid (EA) is a component of ellagitannins, present in crops such as pecans, walnuts, and many berries, which metabolized by the gut microbiota forms urolithins A, B, C, or D. In this study, ellagic acid, as well as urolithins A and B, [...] Read more.
Ellagic acid (EA) is a component of ellagitannins, present in crops such as pecans, walnuts, and many berries, which metabolized by the gut microbiota forms urolithins A, B, C, or D. In this study, ellagic acid, as well as urolithins A and B, were tested on 3T3-L1 preadipocytes for differentiation and lipid accumulation. In addition, inflammation was studied in mature adipocytes challenged with lipopolysaccharide (LPS). Results indicated that EA and urolithins A and B did not affect differentiation (adipogenesis) and only EA and urolithin A attenuated lipid accumulation (lipogenesis), which seemed to be through gene regulation of glucose transporter type 4 (GLUT4) and adiponectin. On the other hand, gene expression of cytokines and proteins associated with the inflammation process indicate that urolithins and EA differentially inhibit tumor necrosis factor alpha (TNFα), inducible nitric oxide synthase (iNOS), interleukin 6 (IL-6), and monocyte chemoattractant protein-1 (MCP-1). Urolithins A and B were found to reduce nuclear levels of phosphorylated nuclear factor κB (p-NF-κB), whereas all treatments showed expression of nuclear phosphorylated protein kinase B (p-AKT) in challenged LPS cells when treated with insulin, indicating the fact that adipocytes remained insulin sensitive. In general, urolithin A is a compound able to reduce lipid accumulation, without affecting the protein expression of peroxisome proliferator-activated receptor-γ (PPARγ), CCAAT/enhancer binding protein-α (c/EBPα), and PPARα, whereas EA and urolithin B were found to enhance PPARγ and c/EBPα protein expressions as well as fatty acid (FA) oxidation, and differentially affected lipid accumulation. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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26 pages, 3035 KiB  
Article
Wounding and UVB Light Synergistically Induce the Biosynthesis of Phenolic Compounds and Ascorbic Acid in Red Prickly Pears (Opuntia ficus-indica cv. Rojo Vigor)
by Erika Ortega-Hernández, Vimal Nair, Jorge Welti-Chanes, Luis Cisneros-Zevallos and Daniel A. Jacobo-Velázquez
Int. J. Mol. Sci. 2019, 20(21), 5327; https://doi.org/10.3390/ijms20215327 - 25 Oct 2019
Cited by 29 | Viewed by 3482
Abstract
The present study evaluated the effects of ultraviolet B (UVB) radiation and wounding stress, applied alone or combined, on the biosynthesis of phenolic compounds and ascorbic acid in the peel and pulp of red prickly pear (Opuntia ficus-indica cv. Rojo Vigor). Whole [...] Read more.
The present study evaluated the effects of ultraviolet B (UVB) radiation and wounding stress, applied alone or combined, on the biosynthesis of phenolic compounds and ascorbic acid in the peel and pulp of red prickly pear (Opuntia ficus-indica cv. Rojo Vigor). Whole and wounded-fruit samples were treated with UVB radiation (6.4 W·m−2) for 0 and 15 min, and stored for 24 h at 16 °C. Phytochemical analyses were performed separately in the peel and pulp. The highest phenolic accumulation occurred after storage of the whole tissue treated with UVB, where the main phenolic compounds accumulated in the peel and pulp were quercetin, sinapic acid, kaempferol, rosmarinic acid, and sinapoyl malate, showing increases of 709.8%, 570.2%, 442.8%, 439.9%, and 186.2%, respectively, as compared with the control before storage. Phenylalanine ammonia-lyase (PAL) activity was increased after storage of the whole and wounded tissue treated with UVB light, and this increase in PAL activity was associated to phenolic accumulation. On the other hand, l-galactono-γ-lactone dehydrogenase (GalLDH) activity and ascorbic acid biosynthesis was enhanced due to UVB radiation, and the effect was increased when UVB was applied in the wounded tissue showing 125.1% and 94.1% higher vitamin C content after storage when compared with the control. Respiration rate was increased due to wounding stress, whereas ethylene production was increased by wounding and UVB radiation in prickly pears. Results allowed the generation of a physiological model explaining the UVB and wound-induced accumulation of phenolic compounds and ascorbic acid in prickly pears, where wounding facilitates UVB to access the underlying tissue and enhances an apparent synergistic response. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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15 pages, 5054 KiB  
Article
Carnosol Increases Skeletal Muscle Cell Glucose Uptake via AMPK-Dependent GLUT4 Glucose Transporter Translocation
by Filip Vlavcheski, David Baron, Ioannis A. Vlachogiannis, Rebecca E. K. MacPherson and Evangelia Tsiani
Int. J. Mol. Sci. 2018, 19(5), 1321; https://doi.org/10.3390/ijms19051321 - 29 Apr 2018
Cited by 41 | Viewed by 5608
Abstract
Skeletal muscle is a major insulin-target tissue and plays an important role in glucose homeostasis. Insulin action in muscle activates the phosphatidylinositol-3 kinase (PI3K)/Akt signaling pathway causing the translocation of intracellularly stored GLUT4 glucose transporters to the plasma membrane and increased glucose uptake. [...] Read more.
Skeletal muscle is a major insulin-target tissue and plays an important role in glucose homeostasis. Insulin action in muscle activates the phosphatidylinositol-3 kinase (PI3K)/Akt signaling pathway causing the translocation of intracellularly stored GLUT4 glucose transporters to the plasma membrane and increased glucose uptake. Impaired insulin action in muscle results in insulin resistance and type 2 diabetes mellitus (T2DM). Activation of the energy sensor AMP-activated kinase (AMPK) increases muscle glucose uptake and the use of AMPK activators is viewed as an effective strategy to combat insulin resistance. Rosemary extract (RE) has been shown to stimulate muscle AMPK and glucose uptake, but the exact components responsible for these effects are unknown. In the current study, we investigated the effect of carnosol, a RE polyphenol, in L6 rat muscle cells. Carnosol stimulated glucose uptake in L6 myotubes in a dose- and time-dependent manner, did not affect Akt, increased AMPK phosphorylation and plasma membrane GLUT4 levels. The carnosol-stimulated glucose uptake and GLUT4 translocation was significantly reduced by the AMPK inhibitor compound C (CC). Our study is the first to show an AMPK-dependent increase in muscle glucose uptake by carnosol. Carnosol has potential as a glucose homeostasis regulating agent and deserves further study. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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13 pages, 7727 KiB  
Article
The Flavonoid Isoquercitrin Precludes Initiation of Zika Virus Infection in Human Cells
by Arnaud Gaudry, Sandra Bos, Wildriss Viranaicken, Marjolaine Roche, Pascale Krejbich-Trotot, Gilles Gadea, Philippe Desprès and Chaker El-Kalamouni
Int. J. Mol. Sci. 2018, 19(4), 1093; https://doi.org/10.3390/ijms19041093 - 05 Apr 2018
Cited by 60 | Viewed by 5931
Abstract
The medical importance of Zika virus (ZIKV) was fully highlighted during the recent epidemics in South Pacific islands and Americas due to ZIKV association with severe damage to fetal brain development and neurological complications in adult patients. A worldwide research effort has been [...] Read more.
The medical importance of Zika virus (ZIKV) was fully highlighted during the recent epidemics in South Pacific islands and Americas due to ZIKV association with severe damage to fetal brain development and neurological complications in adult patients. A worldwide research effort has been undertaken to identify effective compounds to prevent or treat ZIKV infection. Fruits and vegetables may be sources of compounds with medicinal properties. Flavonoids are one class of plant compounds that emerge as promising antiviral molecules against ZIKV. In the present study, we demonstrated that flavonoid isoquercitrin exerts antiviral activity against African historical and Asian epidemic strains of ZIKV in human hepatoma, epithelial, and neuroblastoma cell lines. Time-of-drug addition assays showed that isoquercitrin acts on ZIKV entry by preventing the internalisation of virus particles into the host cell. Our data also suggest that the glycosylated moiety of isoquercitrin might play a role in the antiviral effect of the flavonoid against ZIKV. Our results highlight the importance of isoquercitrin as a promising natural antiviral compound to prevent ZIKV infection. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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18 pages, 8779 KiB  
Article
Investigation of Linum flavum (L.) Hairy Root Cultures for the Production of Anticancer Aryltetralin Lignans
by Sullivan Renouard, Cyrielle Corbin, Samantha Drouet, Barbara Medvedec, Joël Doussot, Cyril Colas, Benoit Maunit, Avninder S. Bhambra, Eric Gontier, Nathalie Jullian, François Mesnard, Michèle Boitel, Bilal Haider Abbasi, Randolph R. J. Arroo, Eric Lainé and Christophe Hano
Int. J. Mol. Sci. 2018, 19(4), 990; https://doi.org/10.3390/ijms19040990 - 26 Mar 2018
Cited by 30 | Viewed by 6423
Abstract
Linum flavum hairy root lines were established from hypocotyl pieces using Agrobacterium rhizogenes strains LBA 9402 and ATCC 15834. Both strains were effective for transformation but induction of hairy root phenotype was more stable with strain ATCC 15834. Whereas similar accumulation patterns were [...] Read more.
Linum flavum hairy root lines were established from hypocotyl pieces using Agrobacterium rhizogenes strains LBA 9402 and ATCC 15834. Both strains were effective for transformation but induction of hairy root phenotype was more stable with strain ATCC 15834. Whereas similar accumulation patterns were observed in podophyllotoxin-related compounds (6-methoxy-podophyllotoxin, podophyllotoxin and deoxypodophyllotoxin), significant quantitative variations were noted between root lines. The influence of culture medium and various treatments (hormone, elicitation and precursor feeding) were evaluated. The highest accumulation was obtained in Gamborg B5 medium. Treatment with methyl jasmonate, and feeding using ferulic acid increased the accumulation of aryltetralin lignans. These results point to the use of hairy root culture lines of Linum flavum as potential sources for these valuable metabolites as an alternative, or as a complement to Podophyllum collected from wild stands. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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13 pages, 1167 KiB  
Article
Chlorogenic Acid and Its Microbial Metabolites Exert Anti-Proliferative Effects, S-Phase Cell-Cycle Arrest and Apoptosis in Human Colon Cancer Caco-2 Cells
by Shima Sadeghi Ekbatan, Xiu-Qing Li, Mohammad Ghorbani, Behnam Azadi and Stan Kubow
Int. J. Mol. Sci. 2018, 19(3), 723; https://doi.org/10.3390/ijms19030723 - 03 Mar 2018
Cited by 105 | Viewed by 7127
Abstract
Chlorogenic acid (CGA) decreases colon cancer-cell proliferation but the combined anti-cancer effects of CGA with its major colonic microbial metabolites, caffeic acid (CA), 3-phenylpropionic acid (3-PPA) and benzoic acid (BA), needs elucidation as they occur together in colonic digesta. Caco-2 cancer cells were [...] Read more.
Chlorogenic acid (CGA) decreases colon cancer-cell proliferation but the combined anti-cancer effects of CGA with its major colonic microbial metabolites, caffeic acid (CA), 3-phenylpropionic acid (3-PPA) and benzoic acid (BA), needs elucidation as they occur together in colonic digesta. Caco-2 cancer cells were treated for 24 h with the four compounds individually (50–1000 µM) and as an equimolar ratio (1:1:1:1; MIX). The effective concentration to decrease cell proliferation by 50% (EC50) was lower for MIX (431 ± 51.84 µM) and CA (460 ± 21.88) versus CGA (758 ± 19.09 µM). The EC50 for cytotoxicity measured by lactate dehydrogenase release in MIX (527 ± 75.34 µM) showed more potency than CA (740 ± 38.68 µM). Cell proliferation was decreased by 3-PPA and BA at 1000 µM with no cytotoxicity. Cell-cycle arrest was induced at the S-phase by CA (100 µM), MIX (100 µM), CGA (250 µM) and 3-PPA (500 µM) with activation of caspase-3 by CGA, CA, MIX (500 and 1000 µM). Mitochondrial DNA content was reduced by 3-PPA (1000 µM). The anti-cancer effects occurred at markedly lower concentrations of each compound within MIX than when provided singly, indicating that they function together to enhance anti-colon cancer activities. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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11 pages, 1701 KiB  
Article
Anti-Hypertensive Effects of Acacia Polyphenol in Spontaneously Hypertensive Rats
by Nobutomo Ikarashi, Takahiro Toda, Yusuke Hatakeyama, Yoshiki Kusunoki, Risako Kon, Nanaho Mizukami, Miho Kaneko, Sosuke Ogawa and Kiyoshi Sugiyama
Int. J. Mol. Sci. 2018, 19(3), 700; https://doi.org/10.3390/ijms19030700 - 01 Mar 2018
Cited by 27 | Viewed by 4815
Abstract
We have previously demonstrated that acacia polyphenol (AP) exerts strong anti-obesity, anti-diabetic, and anti-atopic dermatitis effects. In the present study, we investigated the anti-hypertensive effects of AP. Spontaneously hypertensive rats (SHR) with hypertension and control Wistar Kyoto rats (WKY) were used. WKY and [...] Read more.
We have previously demonstrated that acacia polyphenol (AP) exerts strong anti-obesity, anti-diabetic, and anti-atopic dermatitis effects. In the present study, we investigated the anti-hypertensive effects of AP. Spontaneously hypertensive rats (SHR) with hypertension and control Wistar Kyoto rats (WKY) were used. WKY and SHR were fed AP-containing food or AP-free food (control group) ad libitum for 4 weeks, and their blood pressures were measured. After AP administration, both systolic and diastolic blood pressures were significantly lower in the SHR group than in the control group. There were no differences in the systolic or diastolic blood pressure of WKY between the AP group and the control group. Angiotensin-converting enzyme (ACE) activity, nicotinamide adenine dinucleotide phosphate (NADPH) oxidase expression, and superoxide dismutase (SOD) activity in SHR kidneys were not altered by AP administration. Blood SOD activity in SHR was significantly higher in the AP group than in the control group. AP exerts anti-hypertensive effects on hypertension but has almost no effect on normal blood pressure. The anti-hypertensive effects of AP may be related to the anti-oxidative effects of increased blood SOD activity. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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12 pages, 1812 KiB  
Article
3,5,6,7,8,3′,4′-Heptamethoxyflavone, a Citrus Flavonoid, Inhibits Collagenase Activity and Induces Type I Procollagen Synthesis in HDFn Cells
by Hong-Il Kim, Yong-Un Jeong, Jong-Hyeon Kim and Young-Jin Park
Int. J. Mol. Sci. 2018, 19(2), 620; https://doi.org/10.3390/ijms19020620 - 22 Feb 2018
Cited by 19 | Viewed by 5125
Abstract
Citrus fruits contain various types of flavonoids with powerful anti-aging and photoprotective effects on the skin, and have thus been attracting attention as potential, efficacious skincare agents. Here, we aimed to investigate the chemical composition of Citrus unshiu and its protective effects on [...] Read more.
Citrus fruits contain various types of flavonoids with powerful anti-aging and photoprotective effects on the skin, and have thus been attracting attention as potential, efficacious skincare agents. Here, we aimed to investigate the chemical composition of Citrus unshiu and its protective effects on photoaging. We isolated and identified a bioactive compound, 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF), from C. unshiu peels using ethanol extraction and hexane fractionation. HMF inhibited collagenase activity and increased type I procollagen content in UV-induced human dermal fibroblast neonatal (HDFn) cells. HMF also suppressed the expression of matrix metalloproteinases 1 (MMP-1) and induced the expression of type I procollagen protein in UV-induced HDFn cells. Additionally, HMF inhibited ultraviolet B (UVB)-induced phosphorylation of the mitogen-activated protein kinases (MAPK) cascade signaling components—ERK, JNK, and c-Jun—which are involved in the induction of MMP-1 expression. Furthermore, HMF affected the TGF-β/Smad signaling pathway, which is involved in the regulation of type I procollagen expression. In particular, HMF induced Smad3 protein expression and suppressed Smad7 protein expression in UV-induced HDFn cells in a dose-dependent manner. These findings suggest a role for Citrus unshiu in the preparation of skincare products in future. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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15 pages, 1231 KiB  
Article
Intestinal Permeability and Cellular Antioxidant Activity of Phenolic Compounds from Mango (Mangifera indica cv. Ataulfo) Peels
by Ramón Pacheco-Ordaz, Marilena Antunes-Ricardo, Janet A. Gutiérrez-Uribe and Gustavo A. González-Aguilar
Int. J. Mol. Sci. 2018, 19(2), 514; https://doi.org/10.3390/ijms19020514 - 08 Feb 2018
Cited by 49 | Viewed by 7002
Abstract
Mango (Mangifera indica cv. Ataulfo) peel contains bound phenolics that may be released by alkaline or acid hydrolysis and may be converted into less complex molecules. Free phenolics from mango cv. Ataulfo peel were obtained using a methanolic extraction, and their cellular [...] Read more.
Mango (Mangifera indica cv. Ataulfo) peel contains bound phenolics that may be released by alkaline or acid hydrolysis and may be converted into less complex molecules. Free phenolics from mango cv. Ataulfo peel were obtained using a methanolic extraction, and their cellular antioxidant activity (CAA) and permeability were compared to those obtained for bound phenolics released by alkaline or acid hydrolysis. Gallic acid was found as a simple phenolic acid after alkaline hydrolysis along with mangiferin isomers and quercetin as aglycone and glycosides. Only gallic acid, ethyl gallate, mangiferin, and quercetin were identified in the acid fraction. The acid and alkaline fractions showed the highest CAA (60.5% and 51.5%) when tested at 125 µg/mL. The value of the apparent permeability coefficient (Papp) across the Caco-2/HT-29 monolayer of gallic acid from the alkaline fraction was higher (2.61 × 10−6 cm/s) than in the other fractions and similar to that obtained when tested pure (2.48 × 10−6 cm/s). In conclusion, mango peels contain bound phenolic compounds that, after their release, have permeability similar to pure compounds and exert an important CAA. This finding can be applied in the development of nutraceuticals using this important by-product from the mango processing industry. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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19 pages, 3644 KiB  
Article
Evaluation of Polyphenol Anthocyanin-Enriched Extracts of Blackberry, Black Raspberry, Blueberry, Cranberry, Red Raspberry, and Strawberry for Free Radical Scavenging, Reactive Carbonyl Species Trapping, Anti-Glycation, Anti-β-Amyloid Aggregation, and Microglial Neuroprotective Effects
by Hang Ma, Shelby L. Johnson, Weixi Liu, Nicholas A. DaSilva, Susan Meschwitz, Joel A. Dain and Navindra P. Seeram
Int. J. Mol. Sci. 2018, 19(2), 461; https://doi.org/10.3390/ijms19020461 - 03 Feb 2018
Cited by 126 | Viewed by 11514
Abstract
Glycation is associated with several neurodegenerative disorders, including Alzheimer’s disease (AD), where it potentiates the aggregation and toxicity of proteins such as β-amyloid (Aβ). Published studies support the anti-glycation and neuroprotective effects of several polyphenol-rich fruits, including berries, which are rich in anthocyanins. [...] Read more.
Glycation is associated with several neurodegenerative disorders, including Alzheimer’s disease (AD), where it potentiates the aggregation and toxicity of proteins such as β-amyloid (Aβ). Published studies support the anti-glycation and neuroprotective effects of several polyphenol-rich fruits, including berries, which are rich in anthocyanins. Herein, blackberry, black raspberry, blueberry, cranberry, red raspberry, and strawberry extracts were evaluated for: (1) total phenolic and anthocyanins contents, (2) free radical (DPPH) scavenging and reactive carbonyl species (methylglyoxal; MGO) trapping, (3) anti-glycation (using BSA-fructose and BSA-MGO models), (4) anti-Aβ aggregation (using thermal- and MGO-induced fibrillation models), and, (5) murine microglia (BV-2) neuroprotective properties. Berry crude extracts (CE) were fractionated to yield anthocyanins-free (ACF) and anthocyanins-enriched (ACE) extracts. The berry ACEs (at 100 μg/mL) showed superior free radical scavenging, reactive carbonyl species trapping, and anti-glycation effects compared to their respective ACFs. The berry ACEs (at 100 μg/mL) inhibited both thermal- and MGO-induced Aβ fibrillation. In addition, the berry ACEs (at 20 μg/mL) reduced H2O2-induced reactive oxygen species production, and lipopolysaccharide-induced nitric oxide species in BV-2 microglia as well as decreased H2O2-induced cytotoxicity and caspase-3/7 activity in BV-2 microglia. The free radical scavenging, reactive carbonyl trapping, anti-glycation, anti-Aβ fibrillation, and microglial neuroprotective effects of these berry extracts warrant further in vivo studies to evaluate their potential neuroprotective effects against AD. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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16 pages, 12559 KiB  
Article
Pharmacokinetic Study of Bioactive Flavonoids in the Traditional Japanese Medicine Keigairengyoto Exerting Antibacterial Effects against Staphylococcus aureus
by Takashi Matsumoto, Atsushi Kaneko, Junichi Koseki, Yosuke Matsubara, Setsuya Aiba and Kenshi Yamasaki
Int. J. Mol. Sci. 2018, 19(2), 328; https://doi.org/10.3390/ijms19020328 - 23 Jan 2018
Cited by 22 | Viewed by 5623
Abstract
Recent studies have demonstrated that flavonoid glucuronides can be deconjugated to the active form aglycone by β-glucuronidase-expressing macrophages. Keigairengyoto (KRT) is a flavonoid-rich traditional Japanese medicine reported to enhance bacterial clearance through immune modulation. Our aims are to examine the pharmacokinetics of KRT [...] Read more.
Recent studies have demonstrated that flavonoid glucuronides can be deconjugated to the active form aglycone by β-glucuronidase-expressing macrophages. Keigairengyoto (KRT) is a flavonoid-rich traditional Japanese medicine reported to enhance bacterial clearance through immune modulation. Our aims are to examine the pharmacokinetics of KRT flavonoids and to identify active flavonoids contributing to the adjuvant effects of KRT. KRT was evaluated at pharmacokinetic analysis to quantify absorbed flavonoids, and cutaneous infection assay induced in mice by inoculation of Staphylococcus aureus. Preventive or therapeutic KRT administration reduced the number of bacteria in the infection site as well as macroscopic and microscopic lesion scores with efficacies similar to antibiotics. Pharmacokinetic study revealed low plasma levels of flavonoid aglycones after KRT administration; however, plasma concentrations were enhanced markedly by β-glucuronidase treatment, with baicalein the most abundant (Cmax, 1.32 µg/mL). In random screening assays, flavonoids such as bacalein, genistein, and apigenin enhanced bacteria phagocytosis by macrophages. Glucuronide bacalin was converted to aglycone baicalein by incubation with living macrophages, macrophage lysate, or skin homogenate. Taken together, the adjuvant effect of KRT may be due to some blood-absorbed flavonoids which enhance macrophage functions in host defense. Flavonoid-rich KRT may be a beneficial treatment for infectious skin inflammation. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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5295 KiB  
Article
Extracts of Crataegus oxyacantha and Rosmarinus officinalis Attenuate Ischemic Myocardial Damage by Decreasing Oxidative Stress and Regulating the Production of Cardiac Vasoactive Agents
by Raúl Enrique Cuevas-Durán, Juan Carlos Medrano-Rodríguez, María Sánchez-Aguilar, Elizabeth Soria-Castro, María Esther Rubio-Ruíz, Leonardo Del Valle-Mondragón, Alicia Sánchez-Mendoza, Juan Carlos Torres-Narvaéz, Gustavo Pastelín-Hernández and Luz Ibarra-Lara
Int. J. Mol. Sci. 2017, 18(11), 2412; https://doi.org/10.3390/ijms18112412 - 14 Nov 2017
Cited by 17 | Viewed by 4144
Abstract
Numerous studies have supported a role for oxidative stress in the development of ischemic damage and endothelial dysfunction. Crataegus oxyacantha (Co) and Rosmarinus officinalis (Ro) extracts are polyphenolic-rich compounds that have proven to be efficient in the treatment of [...] Read more.
Numerous studies have supported a role for oxidative stress in the development of ischemic damage and endothelial dysfunction. Crataegus oxyacantha (Co) and Rosmarinus officinalis (Ro) extracts are polyphenolic-rich compounds that have proven to be efficient in the treatment of cardiovascular diseases. We studied the effect of extracts from Co and Ro on the myocardial damage associated with the oxidative status and to the production of different vasoactive agents. Rats were assigned to the following groups: (a) sham; (b) vehicle-treated myocardial infarction (MI) (MI-V); (c) Ro extract-treated myocardial infarction (MI-Ro); (d) Co extract-treated myocardial infarction (MI-Co); or (e) Ro+Co-treated myocardial infarction (MI-Ro+Co). Ro and Co treatments increased total antioxidant capacity, the expression of superoxide dismutase (SOD)-Cu2+/Zn2+, SOD-Mn2+, and catalase, with the subsequent decline of malondialdehyde and 8-hydroxy-2′-deoxyguanosine levels. The extracts diminished vasoconstrictor peptide levels (angiotensin II and endothelin-1), increased vasodilators agents (angiotensin 1–7 and bradikinin) and improved nitric oxide metabolism. Polyphenol treatment restored the left intraventricular pressure and cardiac mechanical work. We conclude that Ro and Co treatment attenuate morphological and functional ischemic-related changes by both an oxidant load reduction and improvement of the balance between vasoconstrictors and vasodilators. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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2466 KiB  
Article
Aspidosperma pyrifolium Has Anti-Inflammatory Properties: An Experimental Study in Mice with Peritonitis Induced by Tityus serrulatus Venom or Carrageenan
by Maíra Conceição Jerônimo de Souza Lima, Mariana Angélica Oliveira Bitencourt, Allanny Alves Furtado, Manoela Torres-Rêgo, Emerson Michell da Silva Siqueira, Ruth Medeiros Oliveira, Hugo Alexandre Oliveira Rocha, Keyla Borges Ferreira Rocha, Arnóbio Antônio da Silva-Júnior, Silvana Maria Zucolotto and Matheus De Freitas Fernandes-Pedrosa
Int. J. Mol. Sci. 2017, 18(11), 2248; https://doi.org/10.3390/ijms18112248 - 11 Nov 2017
Cited by 13 | Viewed by 4448
Abstract
Scorpions of the genus Tityus are responsible for the majority of envenomation in Brazil, the Tityus serrulatus species being the most common and dangerous in South America. In this approach, we have investigated the ability of the aqueous extract from the leaves of [...] Read more.
Scorpions of the genus Tityus are responsible for the majority of envenomation in Brazil, the Tityus serrulatus species being the most common and dangerous in South America. In this approach, we have investigated the ability of the aqueous extract from the leaves of Aspidosperma pyrifolium in reducing carrageenan-induced inflammation and the inflammation induced by T. serrulatus envenomation in mice. We also evaluated the cytotoxic effects of this extract, using the 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl-2H-tetrazolium (MTT) assay and the results revealed that the extract is safe. Analysis by High Performance Liquid Chromatography coupled with Diode Array Detector (HPLC-DAD) and Liquid Chromatography Coupled with Mass Spectrometry with Diode Array Detection (LC-DAD-MS) showed one major chemical component, the flavonoid rutin and phenolics compounds. For in vivo studies in carrageenan-induced peritonitis model, mice received extracts, dexamethasone, rutin or saline, before administration of carrageenan. For venom-induced inflammation model, animals received T. serrulatus venom and were, simultaneously, treated with extracts, antivenom, rutin or saline. The extract and rutin showed a reduction in the cell migration into the peritoneal cavity, and in the same way the envenomated animals also showed reduction of edema, inflammatory cell infiltration and vasodilation in lungs. This is an original study revealing the potential action of A. pyrifolium against inflammation caused by Tityus serrulatus venom and carrageenan, revealing that this extract and its bioactive molecules, specifically rutin, may present potential anti-inflammatory application. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
UVA, UVB Light, and Methyl Jasmonate, Alone or Combined, Redirect the Biosynthesis of Glucosinolates, Phenolics, Carotenoids, and Chlorophylls in Broccoli Sprouts
by Melissa Moreira-Rodríguez, Vimal Nair, Jorge Benavides, Luis Cisneros-Zevallos and Daniel A. Jacobo-Velázquez
Int. J. Mol. Sci. 2017, 18(11), 2330; https://doi.org/10.3390/ijms18112330 - 04 Nov 2017
Cited by 118 | Viewed by 6304
Abstract
Broccoli sprouts contain health-promoting phytochemicals that can be enhanced by applying ultraviolet light (UV) or phytohormones. The separate and combined effects of methyl jasmonate (MJ), UVA, or UVB lights on glucosinolate, phenolic, carotenoid, and chlorophyll profiles were assessed in broccoli sprouts. Seven-day-old broccoli [...] Read more.
Broccoli sprouts contain health-promoting phytochemicals that can be enhanced by applying ultraviolet light (UV) or phytohormones. The separate and combined effects of methyl jasmonate (MJ), UVA, or UVB lights on glucosinolate, phenolic, carotenoid, and chlorophyll profiles were assessed in broccoli sprouts. Seven-day-old broccoli sprouts were exposed to UVA (9.47 W/m2) or UVB (7.16 W/m2) radiation for 120 min alone or in combination with a 25 µM MJ solution, also applied to sprouts without UV supplementation. UVA + MJ and UVB + MJ treatments increased the total glucosinolate content by ~154% and ~148%, respectively. MJ induced the biosynthesis of indole glucosinolates, especially neoglucobrassicin (~538%), showing a synergistic effect with UVA stress. UVB increased the content of aliphatic and indole glucosinolates, such as glucoraphanin (~78%) and 4-methoxy-glucobrassicin (~177%). UVA increased several phenolics such as gallic acid (~57%) and a kaempferol glucoside (~25.4%). MJ treatment decreased most phenolic levels but greatly induced accumulation of 5-sinapoylquinic acid (~239%). MJ treatments also reduced carotenoid and chlorophyll content, while UVA increased lutein (~23%), chlorophyll b (~31%), neoxanthin (~34%), and chlorophyll a (~67%). Results indicated that UV- and/or MJ-treated broccoli sprouts redirect the carbon flux to the biosynthesis of specific glucosinolates, phenolics, carotenoids, and chlorophylls depending on the type of stress applied. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
Involvement of Opioid System, TRPM8, and ASIC Receptors in Antinociceptive Effect of Arrabidaea brachypoda (DC) Bureau
by Vinícius Peixoto Rodrigues, Cláudia Quintino da Rocha, Larissa Lucena Périco, Raquel De Cássia dos Santos, Rie Ohara, Catarine Massucato Nishijima, Emerson Ferreira Queiroz, Jean-Luc Wolfender, Lúcia Regina Machado da Rocha, Adair Roberto Soares Santos, Wagner Vilegas and Clélia Akiko Hiruma-Lima
Int. J. Mol. Sci. 2017, 18(11), 2304; https://doi.org/10.3390/ijms18112304 - 02 Nov 2017
Cited by 12 | Viewed by 4821
Abstract
Arrabidaea brachypoda (DC) Bureau is a medicinal plant found in Brazil. Known as “cipó-una”, it is popularly used as a natural therapeutic agent against pain and inflammation. This study evaluated the chemical composition and antinociceptive activity of the dichloromethane fraction from the roots [...] Read more.
Arrabidaea brachypoda (DC) Bureau is a medicinal plant found in Brazil. Known as “cipó-una”, it is popularly used as a natural therapeutic agent against pain and inflammation. This study evaluated the chemical composition and antinociceptive activity of the dichloromethane fraction from the roots of A. brachypoda (DEAB) and its mechanism of action. The chemical composition was characterized by high-performance liquid chromatography, and this fraction is composed only of dimeric flavonoids. The antinociceptive effect was evaluated in formalin and hot plate tests after oral administration (10–100 mg/kg) in male Swiss mice. We also investigated the involvement of TRPV1 (transient receptor potential vanilloid 1), TRPA1 (transient receptor potential ankyrin 1), TRPM8 (transient receptor potential melastatin 8), and ASIC (acid-sensing ion channel), as well as the opioidergic, glutamatergic, and supraspinal pathways. Moreover, the nociceptive response was reduced (30 mg/kg) in the early and late phase of the formalin test. DEAB activity appears to involve the opioid system, TRPM8, and ASIC receptors, clearly showing that the DEAB alleviates acute pain in mice and suggesting the involvement of the TRPM8 and ASIC receptors and the opioid system in acute pain relief. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
Chemoenzymatic Preparation and Biophysical Properties of Sulfated Quercetin Metabolites
by Kateřina Valentová, Kristýna Káňová, Florent Di Meo, Helena Pelantová, Christopher Steven Chambers, Lenka Rydlová, Lucie Petrásková, Alena Křenková, Josef Cvačka, Patrick Trouillas and Vladimír Křen
Int. J. Mol. Sci. 2017, 18(11), 2231; https://doi.org/10.3390/ijms18112231 - 25 Oct 2017
Cited by 21 | Viewed by 4872
Abstract
Sulfated quercetin derivatives are important authentic standards for metabolic studies. Quercetin-3′-O-sulfate, quercetin-4′-O-sulfate, and quercetin-3-O-sulfate as well as quercetin-di-O-sulfate mixture (quercetin-7,3′-di-O-sulfate, quercetin-7,4′-di-O-sulfate, and quercetin-3′,4′-di-O-sulfate) were synthetized by arylsulfotransferase from Desulfitobacterium [...] Read more.
Sulfated quercetin derivatives are important authentic standards for metabolic studies. Quercetin-3′-O-sulfate, quercetin-4′-O-sulfate, and quercetin-3-O-sulfate as well as quercetin-di-O-sulfate mixture (quercetin-7,3′-di-O-sulfate, quercetin-7,4′-di-O-sulfate, and quercetin-3′,4′-di-O-sulfate) were synthetized by arylsulfotransferase from Desulfitobacterium hafniense. Purified monosulfates and disulfates were fully characterized using MS and NMR and tested for their 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) and N,N-dimethyl-p-phenylenediamine (DMPD) radical scavenging, Folin-Ciocalteau reduction (FCR), ferric reducing antioxidant power (FRAP), and anti-lipoperoxidant activities in rat liver microsomes damaged by tert-butylhydroperoxide. Although, as expected, the sulfated metabolites were usually less active than quercetin, they remained still effective antiradical and reducing agents. Quercetin-3′-O-sulfate was more efficient than quercetin-4′-O-sulfate in DPPH and FCR assays. In contrast, quercetin-4′-O-sulfate was the best ferric reductant and lipoperoxidation inhibitor. The capacity to scavenge ABTS+• and DMPD was comparable for all substances, except for disulfates, which were the most efficient. Quantum calculations and molecular dynamics simulations on membrane models supported rationalization of free radical scavenging and lipid peroxidation inhibition. These results clearly showed that individual metabolites of food bioactives can markedly differ in their biological activity. Therefore, a systematic and thorough investigation of all bioavailable metabolites with respect to native compounds is needed when evaluating food health benefits. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
Quercetin Attenuates Manganese-Induced Neuroinflammation by Alleviating Oxidative Stress through Regulation of Apoptosis, iNOS/NF-κB and HO-1/Nrf2 Pathways
by Entaz Bahar, Ji-Ye Kim and Hyonok Yoon
Int. J. Mol. Sci. 2017, 18(9), 1989; https://doi.org/10.3390/ijms18091989 - 15 Sep 2017
Cited by 119 | Viewed by 8794
Abstract
Manganese (Mn) is an essential trace element required for the development of human body and acts as an enzyme co-factor or activator for various reactions of metabolism. While essential in trace amounts, excessive Mn exposure can result in toxic accumulations in human brain [...] Read more.
Manganese (Mn) is an essential trace element required for the development of human body and acts as an enzyme co-factor or activator for various reactions of metabolism. While essential in trace amounts, excessive Mn exposure can result in toxic accumulations in human brain tissue and resulting extrapyramidal symptoms called manganism similar to idiopathic Parkinson’s disease (PD). Quercetin (QCT) has been demonstrated to play an important role in altering the progression of neurodegenerative diseases by protecting against oxidative stress. This study aimed to investigate the protective effect of QCT on Mn-induced neurotoxicity and the underlying mechanism in SK-N-MC human neuroblastoma cell line and Sprague-Dawley (SD) male rat brain. The results showed that Mn treatment significantly decreased the cell viability of SK-N-MC cell and increased the release of lactate dehydrogenase (LDH), which was attenuated by QCT pretreatment at 10 and 20 µg/mL. Compared to the Mn alone group, QCT pretreatment significantly attenuated Mn-induced oxidative stress, mitochondrial dysfunction and apoptosis. Meanwhile, QCT pretreatment markedly downregulated the NF-κB but upregulated the heme oxygenase-1 (HO-1) and Nrf2 proteins, compared to the Mn alone group. Our result showed the beneficial effect of QCT on hematological parameters against Mn in rat brain. QCT decrease reactive oxygen species (ROS) and protein carbonyl levels and increased Cu/Zn-superoxide dismutase (SOD) activity induced in Mn-treated rats. QCT administration caused a significant reduction in the Mn-induced neuroinflammation by inhibiting the expression of inflammatory markers such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6) cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). QCT lowered the Mn elevated levels of various downstream apoptotic markers, including Bax, cytochrome c, cleaved caspase-3 and polymerase-1 (PARP-1), while QCT treatment upregulated anti-apoptotic Bcl-2 proteins and prevented Mn-induced neurodegeneration. Furthermore, administration of QCT (25 and 50 mg/kg) to Mn-exposed rats showed improvement of histopathological alteration in comparison to Mn-treated rats. Moreover, administration of QCT to Mn-exposed rats showed significant reduction of 8-hydroxy-2’-deoxyguanosine (8-OHdG), Bax, activated caspase-3 and PARP-1 immunoreactivity. These results indicate that QCT could effectively inhibit Mn induced apoptosis and inflammatory response in SK-N-MC cells and SD rats, which may involve the activation of HO-1/Nrf2 and inhibition of NF-κB pathway. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
Bioaccessibility, Intestinal Permeability and Plasma Stability of Isorhamnetin Glycosides from Opuntia ficus-indica (L.)
by Marilena Antunes-Ricardo, César Rodríguez-Rodríguez, Janet A. Gutiérrez-Uribe, Eduardo Cepeda-Cañedo and Sergio O. Serna-Saldívar
Int. J. Mol. Sci. 2017, 18(8), 1816; https://doi.org/10.3390/ijms18081816 - 22 Aug 2017
Cited by 40 | Viewed by 5212
Abstract
Isorhamnetin glycosides are representative compounds of Opuntia ficus-indica that possess different biological activities. There is slight information about the changes in bioaccessibility induced by the glycosylation pattern of flavonoids, particularly for isorhamnetin. In this study, the bioaccessibility and permeability of isorhamnetin glycosides extracted [...] Read more.
Isorhamnetin glycosides are representative compounds of Opuntia ficus-indica that possess different biological activities. There is slight information about the changes in bioaccessibility induced by the glycosylation pattern of flavonoids, particularly for isorhamnetin. In this study, the bioaccessibility and permeability of isorhamnetin glycosides extracted from O. ficus-indica were contrasted with an isorhamnetin standard. Also, the plasma stability of these isorhamnetin glycosides after intravenous administration in rats was evaluated. Recoveries of isorhamnetin after oral and gastric digestion were lower than that observed for its glycosides. After intestinal digestion, isorhamnetin glycosides recoveries were reduced to less than 81.0%. The apparent permeability coefficient from apical (AP) to basolateral (BL) direction (Papp(AP-BL)) of isorhamnetin was 2.6 to 4.6-fold higher than those obtained for its glycosides. Isorhamnetin diglycosides showed higher Papp(AP-BL) values than triglycosides. Sugar substituents affected the Papp(AP-BL) of the triglycosides. Isorhamnetin glycosides were better retained in the circulatory system than the aglycone. After intravenous dose of the isorhamnetin standard, the elimination half-life was 0.64 h but increased to 1.08 h when the O. ficus-indica extract was administered. These results suggest that isorhamnetin glycosides naturally found in O. ficus-indica could be a controlled delivery system to maintain a constant plasmatic concentration of this important flavonoid to exert its biological effects in vivo. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Article
Isorhamnetin and Quercetin Derivatives as Anti-Acetylcholinesterase Principles of Marigold (Calendula officinalis) Flowers and Preparations
by Daniil N. Olennikov, Nina I. Kashchenko, Nadezhda K. Chirikova, Anzurat Akobirshoeva, Ifrat N. Zilfikarov and Cecile Vennos
Int. J. Mol. Sci. 2017, 18(8), 1685; https://doi.org/10.3390/ijms18081685 - 02 Aug 2017
Cited by 62 | Viewed by 8011
Abstract
Marigold (Calendula officinalis L.) is one of the most common and widespread plants used medicinally all over the world. The present study aimed to evaluate the anti-acetylcholinesterase activity of marigold flowers, detect the compounds responsible and perform chemical analysis of marigold commercial [...] Read more.
Marigold (Calendula officinalis L.) is one of the most common and widespread plants used medicinally all over the world. The present study aimed to evaluate the anti-acetylcholinesterase activity of marigold flowers, detect the compounds responsible and perform chemical analysis of marigold commercial products. Analysis of 23 varieties of C. officinalis flowers introduced into Siberia allowed us to select the Greenheart Orange variety due to the superior content of flavonoids (46.87 mg/g) and the highest inhibitory activity against acetylcholinesterase (IC50 63.52 µg/mL). Flavonoids, isorhamnetin and quercetin derivatives were revealed as potential inhibitors with the application of high-performance liquid chromatography (HPLC) activity-based profiling. Investigation of the inhibitory activity of isorhamnetin glycosides demonstrated the maximal potency for isorhamnetin-3-О-(2′′,6′′-di-acetyl)-glucoside (IC50 51.26 μM) and minimal potency for typhaneoside (isorhamnetin-3-O-(2′′,6′′-di-rhamnosyl)-glucoside; IC50 94.92 µM). Among quercetin derivatives, the most active compound was quercetin-3-О-(2′′,6′′-di-acetyl)-glucoside (IC50 36.47 µM), and the least active component was manghaslin (quercetin-3-O-(2′′,6′′-di-rhamnosyl)-glucoside; IC50 94.92 µM). Some structure-activity relationships were discussed. Analysis of commercial marigold formulations revealed a reduced flavonoid content (from 7.18–19.85 mg/g) compared with introduced varieties. Liquid extract was the most enriched preparation, characterized by 3.10 mg/mL of total flavonoid content, and infusion was the least enriched formulation (0.41 mg/mL). The presented results suggest that isorhamnetin and quercetin and its glycosides can be considered as potential anti-acetylcholinesterase agents. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Review

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16 pages, 1086 KiB  
Review
Bioactivities of Phenolics by Focusing on Suppression of Chronic Diseases: A Review
by Fereidoon Shahidi and JuDong Yeo
Int. J. Mol. Sci. 2018, 19(6), 1573; https://doi.org/10.3390/ijms19061573 - 25 May 2018
Cited by 272 | Viewed by 9959
Abstract
Phenolics, which are secondary metabolites of plants, exhibit remarkable bioactivities. In this contribution, we have focused on their protective effect against chronic diseases rather than their antioxidant activities, which have been widely discussed in the literature. A large body of epidemiological studies has [...] Read more.
Phenolics, which are secondary metabolites of plants, exhibit remarkable bioactivities. In this contribution, we have focused on their protective effect against chronic diseases rather than their antioxidant activities, which have been widely discussed in the literature. A large body of epidemiological studies has proven the bioactivities of phenolics in both standard compounds and natural extracts: namely, anticancer, anti-inflammatory, and antibacterial activities as well as reducing diabetes, cardiovascular disease, and neurodegenerative disease. Phenolics also display anti-analgesic, anti-allergic, and anti-Alzheimer’s properties. Thus, this review provides crucial information for better understanding the bioactivities of phenolics in foods and fills a gap in the existing collective and overall knowledge in the field. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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25 pages, 4994 KiB  
Review
Biological Activities of Stilbenoids
by Bolanle C. Akinwumi, Kimberly-Ann M. Bordun and Hope D. Anderson
Int. J. Mol. Sci. 2018, 19(3), 792; https://doi.org/10.3390/ijms19030792 - 09 Mar 2018
Cited by 228 | Viewed by 10835
Abstract
Stilbenoids are a group of naturally occurring phenolic compounds found in various plant species. They share a common backbone structure known as stilbene, but differ in the nature and position of substituents. Stilbenoids are classified as phytoalexins, which are antimicrobial compounds produced de [...] Read more.
Stilbenoids are a group of naturally occurring phenolic compounds found in various plant species. They share a common backbone structure known as stilbene, but differ in the nature and position of substituents. Stilbenoids are classified as phytoalexins, which are antimicrobial compounds produced de novo in plants to protect against fungal infection and toxins. In this review, the biological effects of stilbenoids such as resveratrol, pterostilbene, gnetol and piceatannol are discussed. Stilbenoids exert various biological activities ranging from cardioprotection, neuroprotection, anti-diabetic properties, depigmentation, anti-inflammation, cancer prevention and treatment. The results presented cover a myriad of models, from cell culture to animal studies as well as clinical human trials. Although positive results were obtained in most cell culture and animal studies, further human studies are needed to substantiate beneficial effects of stilbenoids. Resveratrol remains the most widely studied stilbenoid. However, there is limited information regarding the potential of less common stilbenoids. Therefore, further research is warranted to evaluate the salutary effects of various stilbenoids. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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33 pages, 710 KiB  
Review
Meta-Analysis of the Effects of Foods and Derived Products Containing Ellagitannins and Anthocyanins on Cardiometabolic Biomarkers: Analysis of Factors Influencing Variability of the Individual Responses
by María-Teresa García-Conesa, Karen Chambers, Emilie Combet, Paula Pinto, Mar Garcia-Aloy, Cristina Andrés-Lacueva, Sonia De Pascual-Teresa, Pedro Mena, Aleksandra Konic Ristic, Wendy J. Hollands, Paul A. Kroon, Ana Rodríguez-Mateos, Geoffrey Istas, Christos A. Kontogiorgis, Dilip K. Rai, Eileen R. Gibney, Christine Morand, Juan Carlos Espín and Antonio González-Sarrías
Int. J. Mol. Sci. 2018, 19(3), 694; https://doi.org/10.3390/ijms19030694 - 28 Feb 2018
Cited by 101 | Viewed by 9089
Abstract
Understanding interindividual variability in response to dietary polyphenols remains essential to elucidate their effects on cardiometabolic disease development. A meta-analysis of 128 randomized clinical trials was conducted to investigate the effects of berries and red grapes/wine as sources of anthocyanins and of nuts [...] Read more.
Understanding interindividual variability in response to dietary polyphenols remains essential to elucidate their effects on cardiometabolic disease development. A meta-analysis of 128 randomized clinical trials was conducted to investigate the effects of berries and red grapes/wine as sources of anthocyanins and of nuts and pomegranate as sources of ellagitannins on a range of cardiometabolic risk biomarkers. The potential influence of various demographic and lifestyle factors on the variability in the response to these products were explored. Both anthocyanin- and ellagitannin-containing products reduced total-cholesterol with nuts and berries yielding more significant effects than pomegranate and grapes. Blood pressure was significantly reduced by the two main sources of anthocyanins, berries and red grapes/wine, whereas waist circumference, LDL-cholesterol, triglycerides, and glucose were most significantly lowered by the ellagitannin-products, particularly nuts. Additionally, we found an indication of a small increase in HDL-cholesterol most significant with nuts and, in flow-mediated dilation by nuts and berries. Most of these effects were detected in obese/overweight people but we found limited or non-evidence in normoweight individuals or of the influence of sex or smoking status. The effects of other factors, i.e., habitual diet, health status or country where the study was conducted, were inconsistent and require further investigation. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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14 pages, 2099 KiB  
Review
Regulation of Cell Signaling Pathways and miRNAs by Resveratrol in Different Cancers
by Ammad Ahmad Farooqi, Sumbul Khalid and Aamir Ahmad
Int. J. Mol. Sci. 2018, 19(3), 652; https://doi.org/10.3390/ijms19030652 - 26 Feb 2018
Cited by 49 | Viewed by 8743
Abstract
Genomic and proteomic studies have helped improve our understanding of the underlying mechanism(s) of cancer development and progression. Mutations, overexpressed oncogenes, inactivated/downregulated tumor suppressors, loss of apoptosis, and dysregulated signal transduction cascades are some of the well-studied areas of research. Resveratrol has gained [...] Read more.
Genomic and proteomic studies have helped improve our understanding of the underlying mechanism(s) of cancer development and progression. Mutations, overexpressed oncogenes, inactivated/downregulated tumor suppressors, loss of apoptosis, and dysregulated signal transduction cascades are some of the well-studied areas of research. Resveratrol has gained considerable attention in the last two decades because of its pleiotropic anticancer activities. In this review, we have summarized the regulation of WNT, SHH (sonic hedgehog)/GLI (glioma-associated oncogene homolog), TGFβ1 (transforming growth factor beta 1)/SMAD, NOTCH, TRAIL (tumor necrosis factor-related apoptosis-inducing ligand), STAT (signal transducer and activator of transcription), and microRNAs by resveratrol in different cancers. The importance of these signaling pathways in cancer progression, along with their modulation by resveratrol, is discussed. Further, we also evaluate the mechanisms and implications of the downregulation of oncogenic miRNAs and the upregulation of tumor suppressor miRNAs by resveratrol, both of which also define its ability to inhibit tumor growth and metastasis. It is envisioned that designing effective clinical trials will be helpful for the identification of resveratrol responders and non-responders and the elucidation of how this phytochemical can be combined with current therapeutic options to improve their clinical efficacy and reduce off-target effects. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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21 pages, 1896 KiB  
Review
Nanofiltration and Tight Ultrafiltration Membranes for the Recovery of Polyphenols from Agro-Food By-Products
by Alfredo Cassano, Carmela Conidi, René Ruby-Figueroa and Roberto Castro-Muñoz
Int. J. Mol. Sci. 2018, 19(2), 351; https://doi.org/10.3390/ijms19020351 - 24 Jan 2018
Cited by 157 | Viewed by 10538
Abstract
Pressure-driven membrane-based technologies represent a valid approach to reduce the environmental pollution of several agro-food by-products. Recently, in relation to the major interest for natural compounds with biological activities, their use has been also addressed to the recovery, separation and fractionation of phenolic [...] Read more.
Pressure-driven membrane-based technologies represent a valid approach to reduce the environmental pollution of several agro-food by-products. Recently, in relation to the major interest for natural compounds with biological activities, their use has been also addressed to the recovery, separation and fractionation of phenolic compounds from such by-products. In particular, tight ultrafiltration (UF) and nanolfiltration (NF) membranes have been recognized for their capability to recover phenolic compounds from several types of agro-food by-products. The separation capability of these membranes, as well as their productivity, depends on multiple factors such as membrane material, molecular weight cut-off (MWCO) and operating conditions (e.g., pressure, temperature, feed flow rate, volume reduction factor, etc.). This paper aims at providing a critical overview of the influence of these parameters on the recovery of phenolic compounds from agro-food by-products by using tight UF and NF membranes. The literature data are analyzed and discussed in relation to separation processes, molecule properties, membrane characteristics and other phenomena occurring in the process. Current extraction methodologies of phenolic compounds from raw materials are also introduced in order to drive the implementation of integrated systems for the production of actractive phenolic formulations of potential interest as food antioxidants. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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9622 KiB  
Review
Polyphenol-Rich Lentils and Their Health Promoting Effects
by Kumar Ganesan and Baojun Xu
Int. J. Mol. Sci. 2017, 18(11), 2390; https://doi.org/10.3390/ijms18112390 - 10 Nov 2017
Cited by 139 | Viewed by 16646
Abstract
Lentil (Lens culinaris; Family: Fabaceae) is a potential functional dietary ingredient which has polyphenol-rich content. Several studies have demonstrated that the consumption of lentil is immensely connected to the reduction in the incidence of diseases such as diabetes, obesity, cancers and cardiovascular diseases [...] Read more.
Lentil (Lens culinaris; Family: Fabaceae) is a potential functional dietary ingredient which has polyphenol-rich content. Several studies have demonstrated that the consumption of lentil is immensely connected to the reduction in the incidence of diseases such as diabetes, obesity, cancers and cardiovascular diseases due to its bioactive compounds. There has been increasing scientific interest in the study area of lentils as the functional food due to its high nutritive value, polyphenols, and other bioactive compounds. These polyphenols and the bioactive compounds found in lentil play an important role in the prevention of those degenerative diseases in humans. Besides that, it has health-promoting effects. Based on the in vitro, in-vivo and clinical studies, the present review focuses to provide more information on the nutritional compositions, bioactive compounds including polyphenols and health-promoting effects of lentils. Health-promoting information was gathered and orchestrated at a suitable place in the review. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
672 KiB  
Review
Polyphenol-Rich Dry Common Beans (Phaseolus vulgaris L.) and Their Health Benefits
by Kumar Ganesan and Baojun Xu
Int. J. Mol. Sci. 2017, 18(11), 2331; https://doi.org/10.3390/ijms18112331 - 04 Nov 2017
Cited by 164 | Viewed by 16898
Abstract
Polyphenols are plant metabolites with potent anti-oxidant properties, which help to reduce the effects of oxidative stress-induced dreaded diseases. The evidence demonstrated that dietary polyphenols are of emerging increasing scientific interest due to their role in the prevention of degenerative diseases in humans. [...] Read more.
Polyphenols are plant metabolites with potent anti-oxidant properties, which help to reduce the effects of oxidative stress-induced dreaded diseases. The evidence demonstrated that dietary polyphenols are of emerging increasing scientific interest due to their role in the prevention of degenerative diseases in humans. Possible health beneficial effects of polyphenols are based on the human consumption and their bioavailability. Common beans (Phaseolus vulgaris L.) are a greater source of polyphenolic compounds with numerous health promoting properties. Polyphenol-rich dry common beans have potential effects on human health, and possess anti-oxidant, anti-diabetic, anti-obesity, anti-inflammatory and anti-mutagenic and anti-carcinogenic properties. Based on the studies, the current comprehensive review aims to provide up-to-date information on the nutritional compositions and health-promoting effect of polyphenol-rich common beans, which help to explore their therapeutic values for future clinical studies. Investigation of common beans and their impacts on human health were obtained from various library databases and electronic searches (Science Direct PubMed, and Google Scholar). Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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