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Special Issue "Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits"

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 (30 November 2018)

Special Issue Editors

Guest Editor
Dr. Gerard Aragonès

Universitat Rovira i Virgili, Department of Biochemistry and Biotechnology, Nutrigenomics Research Group, Tarragona, Spain
Website | E-Mail
Interests: bioactive compounds; chrono-nutrition; energy homeostasis; epigenetics; functional foods; gut microbiota; leptin signalling; metabolism nutrigenomics; obesity xenohormesis
Guest Editor
Dr. Letizia Bresciani

The Laboratory of Phytochemicals in Physiology, Human Nutrition Unit, Department of Food & Drugs, University of Parma, 43125 Parma, Italy
Website | E-Mail
Interests: bioactivity; bioavailability; colonic metabolites; gut microbiota; inter-individual variability; metabolism; pharmacokinetics; phytochemicals; plant based-foods and beverages; supplements; TMAO; urinary excretion

Special Issue Information

Dear Colleagues,

Most polyphenols cannot be absorbed as such, and need some structural modification prior absorption. The absorption of a minimal part of the ingested polyphenols occurs in the first gastro-intestinal tract, whereas the largest part reaches the colon, where polyphenolic compounds are metabolized by the host microbiota. In the large intestine, the unmetabolized polyphenols undergo ring fission, leading to the production of smaller molecules, which in turn can be subject to reduction, decarboxylation, demethylation and dehydroxylation reactions, prior to efficient absorption. Once absorbed, polyphenols and their derived microbial metabolites follow the common metabolic pathway of exogenous organic substances, undergoing cellular and/or hepatic phase II metabolism, resulting in the formation of conjugated metabolites, such as methyl-, sulfate- and/or glucuronide-derivatives. From the liver, potential bioactive metabolites enter systemic circulation prior urinary excretion. The understanding of the absorption efficacy, the polyphenol–gut microbiota interactions and the gut microbial bioconversion capability could provide more insight into the human metabolism and the bioavailability of bioactive polyphenols and represent a necessary step to further elucidate the potential health effects of polyphenols and their derived metabolites. Moreover, the inter-individual variability in the production of specific metabolites also highlights the need for more efforts in this research field. With the support of IJMS, this Special Issue welcomes manuscripts from human and animal studies on the absorption and metabolism of polyphenols, as well as in vitro studies aimed at evaluating the potential polyphenol bioactivity and their molecular mechanisms of action.

Dr. Gerard Aragonès
Dr. Letizia Bresciani
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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 monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Bioactivity
  • Bioavailability
  • Metabolism
  • Pharmacokinetics
  • Polyphenols

Published Papers (5 papers)

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Research

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Open AccessArticle Inhibitory and Inductive Effects of Opuntia ficus indica Extract and Its Flavonoid Constituents on Cytochrome P450s and UDP-Glucuronosyltransferases
Int. J. Mol. Sci. 2018, 19(11), 3400; https://doi.org/10.3390/ijms19113400
Received: 8 September 2018 / Revised: 18 October 2018 / Accepted: 26 October 2018 / Published: 30 October 2018
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Abstract
Opuntia ficus indica (OFI) is grown abundantly in arid areas and its fruits are regarded as an important food and nutrient source owing to the presence of flavonoids, minerals, and proteins. The previous report that OFI exerts phytoestrogenic activity makes it plausible for
[...] Read more.
Opuntia ficus indica (OFI) is grown abundantly in arid areas and its fruits are regarded as an important food and nutrient source owing to the presence of flavonoids, minerals, and proteins. The previous report that OFI exerts phytoestrogenic activity makes it plausible for OFI-containing supplements to be used as alternative estrogen replacement therapy. In the case of polypharmacy with the consumption of OFI-containing botanicals in post- or peri-menopausal women, it is critical to determine the potential drug-OFI interaction due to the modulation of drug metabolism. In the present study, the modulating effects on the hepatic drug metabolizing enzymes (DMEs) by OFI and its flavonoid constituents (kaempferol, quercetin, isorhamnetin, and their glycosidic forms) were investigated using the liver microsomal fractions prepared from ovariectomized (OVX) rats, human liver microsomes, and human hepatocarcinoma cell line (HepG2). As a result, the oral administration of extracts of OFI (OFIE) in OVX rats induced hepatic CYP2B1, CYP3A1, and UGT2B1. OFIE, hydrolyzed (hdl) OFIE, and several flavonols induced the transcriptional activities of both CYP2B6 and CYP3A4 genes in HepG2 cells. Finally, OFIE did not inhibit activities of cytochrome P450 (CYPs) or uridine diphosphate (UDP)-glucuronosyltransferases (UGTs), whereas hdl OFIE or flavonol treatment inhibited CYP1A2 and CYP3A1/3A4 in rat and human liver microsomes. Our data demonstrate that OFIE may induce or inhibit certain types of DMEs and indicate that drug-OFI interaction may occur when the substrate or inhibitor drugs of specific CYPs or UGTs are taken concomitantly with OFI-containing products. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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Open AccessArticle The Beneficial Effect of Proanthocyanidins and Icariin on Biochemical Markers of Bone Turnover in Rats
Int. J. Mol. Sci. 2018, 19(9), 2746; https://doi.org/10.3390/ijms19092746
Received: 27 July 2018 / Revised: 10 September 2018 / Accepted: 10 September 2018 / Published: 13 September 2018
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Abstract
Nutrition is an important factor that influences bone metabolism, the endocrine and/or paracrine system, and bone-active mineral elements homeostasis. We studied antiosteoporotic effects of grape seed proanthocyanidins extract, icariin or alendronate (ALN) in retinoic acid-induced (13cRA) bone loss in rats. Proanthocyanidins and icariin
[...] Read more.
Nutrition is an important factor that influences bone metabolism, the endocrine and/or paracrine system, and bone-active mineral elements homeostasis. We studied antiosteoporotic effects of grape seed proanthocyanidins extract, icariin or alendronate (ALN) in retinoic acid-induced (13cRA) bone loss in rats. Proanthocyanidins and icariin have beneficial effects on bone health; they have improved the bone weight reduction, the length and the diameter of the bone, calcium, and phosphorus content in bone ash, bone mineral density (BMD), the biochemical markers of bone turnover and uterus atrophy induced by 13cRA. All results suggest that proanthocyanidins and icariin reverse osteoporosis in 13cRA rats by stimulating bone formation or regulating bone resorption by their antioxidative and estrogenic-like activity without toxic side-effects observed in ALN treatment. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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Open AccessArticle Gomisin N Alleviates Ethanol-Induced Liver Injury through Ameliorating Lipid Metabolism and Oxidative Stress
Int. J. Mol. Sci. 2018, 19(9), 2601; https://doi.org/10.3390/ijms19092601
Received: 10 July 2018 / Revised: 21 August 2018 / Accepted: 28 August 2018 / Published: 1 September 2018
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Abstract
Gomisin N (GN), a lignan derived from Schisandra chinensis, has been shown to possess antioxidant, anti-inflammatory, and anticancer properties. In the present study, we investigated the protective effect of GN against ethanol-induced liver injury using in vivo and in vitro experiments. Histopathological
[...] Read more.
Gomisin N (GN), a lignan derived from Schisandra chinensis, has been shown to possess antioxidant, anti-inflammatory, and anticancer properties. In the present study, we investigated the protective effect of GN against ethanol-induced liver injury using in vivo and in vitro experiments. Histopathological examination revealed that GN administration to chronic-binge ethanol exposure mice significantly reduced ethanol-induced hepatic steatosis through reducing lipogenesis gene expression and increasing fatty acid oxidation gene expression, and prevented liver injury by lowering the serum levels of aspartate transaminase and alanine transaminase. Further, it significantly inhibited cytochrome P450 2E1 (CYP2E1) gene expression and enzyme activity, and enhanced antioxidant genes and glutathione level in hepatic tissues, which led to decreased hepatic malondialdehyde levels. It also lowered inflammation gene expression. Finally, GN administration promoted hepatic sirtuin1 (SIRT1)-AMP-activated protein kinase (AMPK) signaling in ethanol-fed mice. Consistent with in vivo data, treatment with GN decreased lipogenesis gene expression and increased fatty acid oxidation gene expression in ethanol-treated HepG2 cells, thereby preventing ethanol-induced triglyceride accumulation. Furthermore, it inhibited reactive oxygen species generation by downregulating CYP2E1 and upregulating antioxidant gene expression, and suppressed inflammatory gene expression. Moreover, GN prevented ethanol-mediated reduction in SIRT1 and phosphorylated AMPK. These findings indicate that GN has therapeutic potential against alcoholic liver disease through inhibiting hepatic steatosis, oxidative stress and inflammation. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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Open AccessArticle Sulfated Metabolites of Flavonolignans and 2,3-Dehydroflavonolignans: Preparation and Properties
Int. J. Mol. Sci. 2018, 19(8), 2349; https://doi.org/10.3390/ijms19082349
Received: 7 July 2018 / Revised: 31 July 2018 / Accepted: 6 August 2018 / Published: 9 August 2018
Cited by 1 | PDF Full-text (2199 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Silymarin, an extract from milk thistle (Silybum marianum) fruits, is consumed in various food supplements. The metabolism of silymarin flavonolignans in mammals is complex, the exact structure of their metabolites still remains partly unclear and standards are not commercially available. This
[...] Read more.
Silymarin, an extract from milk thistle (Silybum marianum) fruits, is consumed in various food supplements. The metabolism of silymarin flavonolignans in mammals is complex, the exact structure of their metabolites still remains partly unclear and standards are not commercially available. This work is focused on the preparation of sulfated metabolites of silymarin flavonolignans. Sulfated flavonolignans were prepared using aryl sulfotransferase from Desulfitobacterium hafniense and p-nitrophenyl sulfate as a sulfate donor and characterized by high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). 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; ferric (FRAP) and Folin–Ciocalteu reagent (FCR) reducing activity; anti-lipoperoxidant potential; and effect on the nuclear erythroid 2-related factor 2 (Nrf2) signaling pathway were examined. Pure silybin A 20-O-sulfate, silybin B 20-O-sulfate, 2,3-dehydrosilybin-20-O-sulfate, 2,3-dehydrosilybin-7,20-di-O-sulfate, silychristin-19-O-sulfate, 2,3-dehydrosilychristin-19-O-sulfate, and silydianin-19-O-sulfate were prepared and fully characterized. Sulfated 2,3-dehydroderivatives were more active in FCR and FRAP assays than the parent compounds, and remaining sulfates were less active chemoprotectants. The sulfated flavonolignans obtained can be now used as authentic standards for in vivo metabolic experiments and for further research on their biological activity. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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Review

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Open AccessReview Current Disease-Targets for Oleocanthal as Promising Natural Therapeutic Agent
Int. J. Mol. Sci. 2018, 19(10), 2899; https://doi.org/10.3390/ijms19102899
Received: 5 September 2018 / Revised: 19 September 2018 / Accepted: 20 September 2018 / Published: 24 September 2018
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Abstract
The broad number of health benefits which can be obtained from the long-term consumption of olive oil are attributed mainly to its phenolic fraction. Many olive oil phenolics have been studied deeply since their discovery due to their bioactivity properties, such as Hydroxytyrosol.
[...] Read more.
The broad number of health benefits which can be obtained from the long-term consumption of olive oil are attributed mainly to its phenolic fraction. Many olive oil phenolics have been studied deeply since their discovery due to their bioactivity properties, such as Hydroxytyrosol. Similarly, in the last decade, the special attention of researchers has been addressed to Oleocanthal (OC). This olive oil phenolic compound has recently emerged as a potential therapeutic agent against a variety of diseases, including cancer, inflammation, and neurodegenerative and cardiovascular diseases. Recently, different underlying mechanisms of OC against these diseases have been explored. This review summarizes the current literature on OC to date, and focuses on its promising bioactivities against different disease-targets. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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