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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) | Viewed by 68935

Special Issue Editors

Nutrigenomics Research Group, Department of Biochemistry and Biotechnology, Universitat Rovira i Virgili, 43007 Tarragona, Spain
Interests: adipose expandability; bioactive compounds; biological rhythms; chrononutrition; energy metabolism; epigenetics; functional foods; gut microbiota; hypothalamic dysfunction; leptin; nutrigenomics; obesity; polyphenols; xenohormesis
Special Issues, Collections and Topics in MDPI journals
The Laboratory of Phytochemicals in Physiology, Human Nutrition Unit, Department of Veterinary Science, University of Parma, 43125 Parma, Italy
Interests: nutrition; polyphenol; bioactive compounds; metabolism; bioavailability; beneficial effects; prevention; mass spectometry
Special Issues, Collections and Topics in MDPI journals

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

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Keywords

  • Bioactivity
  • Bioavailability
  • Metabolism
  • Pharmacokinetics
  • Polyphenols

Published Papers (13 papers)

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Research

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12 pages, 1727 KiB  
Article
The Effect of Green and Black Tea Polyphenols on BRCA2 Deficient Chinese Hamster Cells by Synthetic Lethality through PARP Inhibition
by Shaherah Alqahtani, Kelly Welton, Jeffrey P. Gius, Suad Elmegerhi and Takamitsu A. Kato
Int. J. Mol. Sci. 2019, 20(6), 1274; https://doi.org/10.3390/ijms20061274 - 14 Mar 2019
Cited by 4 | Viewed by 3674
Abstract
Tea polyphenols are known antioxidants presenting health benefits due to their observed cellular activities. In this study, two tea polyphenols, epigallocatechin gallate, which is common in green tea, and theaflavin, which is common in black tea, were investigated for their PARP inhibitory activity [...] Read more.
Tea polyphenols are known antioxidants presenting health benefits due to their observed cellular activities. In this study, two tea polyphenols, epigallocatechin gallate, which is common in green tea, and theaflavin, which is common in black tea, were investigated for their PARP inhibitory activity and selective cytotoxicity to BRCA2 mutated cells. The observed cytotoxicity of these polyphenols to BRCA2 deficient cells is believed to be a result of PARP inhibition induced synthetic lethality. Chinese hamster V79 cells and their BRCA2 deficient mutant V-C8, and V-C8 with gene complemented cells were tested against epigallocatechin gallate and theaflavin. In addition, Chinese hamster ovary (CHO) wild-type cells and rad51D mutant 51D1 cells were used to further investigate the synthetic lethality of these molecules. The suspected PARP inhibitory activity of epigallocatechin and theaflavin was confirmed through in vitro and in vivo experiments. Epigallocatechin gallate showed a two-fold increase of cytotoxicity to V-C8 cells compared to V79 and gene complimented cells. Compared to CHO wild type cells, 51D1 cells also showed elevated cytotoxicity following treatment with epigallocatechin gallate. Theaflavin, however, showed a similar increase of cytotoxicity to VC8 compared to V79 and gene corrected cells, but did not show elevation of cytotoxicity towards rad51D mutant cells compared to CHO cells. Elevation of sister chromatid exchange formation was observed in both tea polyphenol treatments. Polyphenol treatment induced more micronuclei formation in BRCA2 deficient cells and rad51D deficient cells when compared against the respective wild type cells. In conclusion, tea polyphenols, epigallocatechin gallate, and theaflavin may present selective cytotoxicity to BRCA2 deficient cells through synthetic lethality induced by PARP inhibition. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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13 pages, 1651 KiB  
Article
Effects of Quercetin Metabolites on Triglyceride Metabolism of 3T3-L1 Preadipocytes and Mature Adipocytes
by Itziar Eseberri, Jonatan Miranda, Arrate Lasa, Andrea Mosqueda-Solís, Susana González-Manzano, Celestino Santos-Buelga and Maria P. Portillo
Int. J. Mol. Sci. 2019, 20(2), 264; https://doi.org/10.3390/ijms20020264 - 11 Jan 2019
Cited by 25 | Viewed by 5747
Abstract
Quercetin (Q) has rapid metabolism, which may make it worthwhile to focus on the potential activity of its metabolites. Our aim was to evaluate the triglyceride-lowering effects of Q metabolites in mature and pre-adipocytes, and to compare them to those induced by Q. [...] Read more.
Quercetin (Q) has rapid metabolism, which may make it worthwhile to focus on the potential activity of its metabolites. Our aim was to evaluate the triglyceride-lowering effects of Q metabolites in mature and pre-adipocytes, and to compare them to those induced by Q. 3T3-L1 mature and pre-adipocytes were treated with 0.1, 1 and 10 µM of Q, tamarixetin (TAM), isorhamnetin (ISO), quercetin-3-O-glucuronide (3G), quercetin-3-O-sulfate (3S), as well as with 3S and quercetin-4-O-sulfate (4S) mixture (3S+4S). Triglyceride (TG) content in both cell types, as well as free fatty acid (FFA) and glycerol in the incubation medium of mature adipocytes were measured spectrophotometrically. Gene expression was assessed by RT-PCR. In mature adipocytes, Q decreased TG at 1 and 10 µM, 3S metabolite at 1 and 10 µM, and 3S+4S mixture at 10 µM. 3S treatment modified the glucose uptake, and TG assembling, but not lipolysis or apoptosis. During differentiation, only 10 µM of ISO reduced TG content, as did Q at physiological doses. In conclusion, 3S metabolite but not ISO, 3G, 4S and TAM metabolites can contribute to the in vivo delipidating effect of Q. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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15 pages, 1962 KiB  
Article
Oxyresveratrol Increases Energy Expenditure through Foxo3a-Mediated Ucp1 Induction in High-Fat-Diet-Induced Obese Mice
by Jin Hee Choi, No-Joon Song, A Reum Lee, Dong Ho Lee, Min-Ju Seo, Suji Kim, Seo-Hyuk Chang, Dong Kwon Yang, Yu-Jin Hwang, Kyung-A Hwang, Tal Soo Ha, Ui Jeong Yun and Kye Won Park
Int. J. Mol. Sci. 2019, 20(1), 26; https://doi.org/10.3390/ijms20010026 - 21 Dec 2018
Cited by 14 | Viewed by 4466
Abstract
The phytochemical oxyresveratrol has been shown to exert diverse biological activities including prevention of obesity. However, the exact reason underlying the anti-obese effects of oxyresveratrol is not fully understood. Here, we investigated the effects and mechanism of oxyresveratrol in adipocytes and high-fat diet [...] Read more.
The phytochemical oxyresveratrol has been shown to exert diverse biological activities including prevention of obesity. However, the exact reason underlying the anti-obese effects of oxyresveratrol is not fully understood. Here, we investigated the effects and mechanism of oxyresveratrol in adipocytes and high-fat diet (HFD)-fed obese mice. Oxyresveratrol suppressed lipid accumulation and expression of adipocyte markers during the adipocyte differentiation of 3T3-L1 and C3H10T1/2 cells. Administration of oxyresveratrol in HFD-fed obese mice prevented body-weight gains, lowered adipose tissue weights, improved lipid profiles, and increased glucose tolerance. The anti-obese effects were linked to increases in energy expenditure and higher rectal temperatures without affecting food intake, fecal lipid content, and physical activity. The increased energy expenditure by oxyresveratrol was concordant with the induction of thermogenic genes including Ucp1, and the reduction of white adipocyte selective genes in adipose tissue. Furthermore, Foxo3a was identified as an oxyresveratrol-induced gene and it mimicked the effects of oxyresveratrol for induction of thermogenic genes and suppression of white adipocyte selective genes, suggesting the role of Foxo3a in oxyresveratrol-mediated anti-obese effects. Taken together, these data show that oxyresveratrol increases energy expenditure through the induction of thermogenic genes in adipose tissue and further implicates oxyresveratrol as an ingredient and Foxo3a as a molecular target for the development of functional foods in obesity and metabolic diseases. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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13 pages, 3120 KiB  
Article
Inhibitory Effect of Synthetic Flavone Derivatives on Pan-Aurora Kinases: Induction of G2/M Cell-Cycle Arrest and Apoptosis in HCT116 Human Colon Cancer Cells
by Soon Young Shin, Youngshim Lee, Beom Soo Kim, Junho Lee, Seunghyun Ahn, Dongsoo Koh, Yoongho Lim and Young Han Lee
Int. J. Mol. Sci. 2018, 19(12), 4086; https://doi.org/10.3390/ijms19124086 - 17 Dec 2018
Cited by 10 | Viewed by 3135
Abstract
Members of the aurora kinase family are Ser/Thr kinases involved in regulating mitosis. Multiple promising clinical trials to target aurora kinases are in development. To discover flavones showing growth inhibitory effects on cancer cells, 36 flavone derivatives were prepared, and their cytotoxicity was [...] Read more.
Members of the aurora kinase family are Ser/Thr kinases involved in regulating mitosis. Multiple promising clinical trials to target aurora kinases are in development. To discover flavones showing growth inhibitory effects on cancer cells, 36 flavone derivatives were prepared, and their cytotoxicity was measured using a long-term clonogenic survival assay. Their half-maximal growth inhibitory effects against HCT116 human colon cancer cells were observed at the sub-micromolar level. Pharmacophores were derived based on three-dimensional quantitative structure–activity calculations. Because plant-derived flavones inhibit aurora kinase B, we selected 5-methoxy-2-(2-methoxynaphthalen-1-yl)-4H-chromen-4-one (derivative 31), which showed the best half-maximal cell growth inhibitory effect, and tested whether it can inhibit aurora kinases in HCT116 colon cancer cells. We found that derivative 31 inhibited the phosphorylation of aurora kinases A, aurora kinases B and aurora kinases C, suggesting that derivative 31 is a potential pan-aurora kinase inhibitor. The results of our analysis of the binding modes between derivative 31 and aurora A and aurora B kinases using in-silico docking were consistent with the pharmacophores proposed in this study. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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15 pages, 2919 KiB  
Article
Interaction of Chrysin and Its Main Conjugated Metabolites Chrysin-7-Sulfate and Chrysin-7-Glucuronide with Serum Albumin
by Violetta Mohos, Eszter Fliszár-Nyúl, Gabriella Schilli, Csaba Hetényi, Beáta Lemli, Sándor Kunsági-Máté, Balázs Bognár and Miklós Poór
Int. J. Mol. Sci. 2018, 19(12), 4073; https://doi.org/10.3390/ijms19124073 - 17 Dec 2018
Cited by 26 | Viewed by 4591
Abstract
Chrysin (5,7-dihydroxyflavone) is a flavonoid aglycone, which is found in nature and in several dietary supplements. During the biotransformation of chrysin, its conjugated metabolites chrysin-7-sulfate (C7S) and chrysin-7-glucuronide (C7G) are formed. Despite the fact that these conjugates appear in the circulation at much [...] Read more.
Chrysin (5,7-dihydroxyflavone) is a flavonoid aglycone, which is found in nature and in several dietary supplements. During the biotransformation of chrysin, its conjugated metabolites chrysin-7-sulfate (C7S) and chrysin-7-glucuronide (C7G) are formed. Despite the fact that these conjugates appear in the circulation at much higher concentrations than chrysin, their interactions with serum albumin have not been reported. In this study, the complex formation of chrysin, C7S, and C7G with human (HSA) and bovine (BSA) serum albumins was investigated employing fluorescence spectroscopic, ultrafiltration, and modeling studies. Our major observations/conclusions are as follows: (1) Compared to chrysin, C7S binds with a threefold higher affinity to HSA, while C7G binds with a threefold lower affinity; (2) the albumin-binding of chrysin, C7S, and C7G did not show any large species differences regarding HSA and BSA; (3) tested flavonoids likely occupy Sudlow’s Site I in HSA; (4) C7S causes significant displacement of Sudlow’s Site I ligands, exerting an even stronger displacing ability than the parent compound chrysin. Considering the above-listed observations, the high intake of chrysin (e.g., through the consumption of dietary supplements with high chrysin contents) may interfere with the albumin-binding of several drugs, mainly due to the strong interaction of C7S with HSA. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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15 pages, 2360 KiB  
Article
Inhibitory and Inductive Effects of Opuntia ficus indica Extract and Its Flavonoid Constituents on Cytochrome P450s and UDP-Glucuronosyltransferases
by Hyesoo Jeong, Soolin Kim, Mi-yeon Kim, Jimin Lee, Byoung Ha An, Hee-Doo Kim, Hyunyoung Jeong, Yun Seon Song and Minsun Chang
Int. J. Mol. Sci. 2018, 19(11), 3400; https://doi.org/10.3390/ijms19113400 - 30 Oct 2018
Cited by 6 | Viewed by 3316
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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19 pages, 1732 KiB  
Article
The Beneficial Effect of Proanthocyanidins and Icariin on Biochemical Markers of Bone Turnover in Rats
by Nada Oršolić, Johann Nemrava, Željko Jeleč, Marina Kukolj, Dyana Odeh, Svjetlana Terzić, Rajko Fureš, Tomica Bagatin and Dinko Bagatin
Int. J. Mol. Sci. 2018, 19(9), 2746; https://doi.org/10.3390/ijms19092746 - 13 Sep 2018
Cited by 18 | Viewed by 3840
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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17 pages, 4966 KiB  
Article
Gomisin N Alleviates Ethanol-Induced Liver Injury through Ameliorating Lipid Metabolism and Oxidative Stress
by Arulkumar Nagappan, Dae Young Jung, Ji-Hyun Kim, Hoyoung Lee and Myeong Ho Jung
Int. J. Mol. Sci. 2018, 19(9), 2601; https://doi.org/10.3390/ijms19092601 - 01 Sep 2018
Cited by 37 | Viewed by 5081
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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16 pages, 2199 KiB  
Article
Sulfated Metabolites of Flavonolignans and 2,3-Dehydroflavonolignans: Preparation and Properties
by Kateřina Valentová, Kateřina Purchartová, Lenka Rydlová, Lenka Roubalová, David Biedermann, Lucie Petrásková, Alena Křenková, Helena Pelantová, Veronika Holečková-Moravcová, Eva Tesařová, Josef Cvačka, Jiří Vrba, Jitka Ulrichová and Vladimír Křen
Int. J. Mol. Sci. 2018, 19(8), 2349; https://doi.org/10.3390/ijms19082349 - 09 Aug 2018
Cited by 21 | Viewed by 3694
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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39 pages, 3853 KiB  
Review
Molecular Mechanisms and Bioavailability of Polyphenols in Prostate Cancer
by Teodora Costea, Péter Nagy, Constanța Ganea, János Szöllősi and Maria-Magdalena Mocanu
Int. J. Mol. Sci. 2019, 20(5), 1062; https://doi.org/10.3390/ijms20051062 - 01 Mar 2019
Cited by 44 | Viewed by 5992
Abstract
Prostate cancer is the one of the most frequently diagnosed cancers among men over the age of 50. Several lines of evidence support the observation that polyphenols have preventive and therapeutic effects in prostate cancer. Moreover, prostate cancer is ideal for chemoprevention due [...] Read more.
Prostate cancer is the one of the most frequently diagnosed cancers among men over the age of 50. Several lines of evidence support the observation that polyphenols have preventive and therapeutic effects in prostate cancer. Moreover, prostate cancer is ideal for chemoprevention due to its long latency. We propose here an equilibrated lifestyle with a diet rich in polyphenols as prophylactic attempts to slow down the progression of localized prostate cancer or prevent the occurrence of the disease. In this review, we will first summarize the molecular mechanisms of polyphenols in prostate cancer with a focus on the antioxidant and pro-oxidant effects, androgen receptors (AR), key molecules involved in AR signaling and their transactivation pathways, cell cycle, apoptosis, angiogenesis, metastasis, genetic aspects, and epigenetic mechanisms. The relevance of the molecular mechanisms is discussed in light of current bioavailability data regarding the activity of polyphenols in prostate cancer. We also highlight strategies for improving the bioavailability of polyphenols. We hope that this review will lead to further research regarding the bioavailability and the role of polyphenols in prostate cancer prevention and treatment. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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16 pages, 947 KiB  
Review
Epigallocatechin Gallate Modulates Muscle Homeostasis in Type 2 Diabetes and Obesity by Targeting Energetic and Redox Pathways: A Narrative Review
by Ester Casanova, Josepa Salvadó, Anna Crescenti and Albert Gibert-Ramos
Int. J. Mol. Sci. 2019, 20(3), 532; https://doi.org/10.3390/ijms20030532 - 27 Jan 2019
Cited by 62 | Viewed by 7139
Abstract
Obesity is associated with the hypertrophy and hyperplasia of adipose tissue, affecting the healthy secretion profile of pro- and anti-inflammatory adipokines. Increased influx of fatty acids and inflammatory adipokines from adipose tissue can induce muscle oxidative stress and inflammation and negatively regulate myocyte [...] Read more.
Obesity is associated with the hypertrophy and hyperplasia of adipose tissue, affecting the healthy secretion profile of pro- and anti-inflammatory adipokines. Increased influx of fatty acids and inflammatory adipokines from adipose tissue can induce muscle oxidative stress and inflammation and negatively regulate myocyte metabolism. Muscle has emerged as an important mediator of homeostatic control through the consumption of energy substrates, as well as governing systemic signaling networks. In muscle, obesity is related to decreased glucose uptake, deregulation of lipid metabolism, and mitochondrial dysfunction. This review focuses on the effect of epigallocatechin-gallate (EGCG) on oxidative stress and inflammation, linked to the metabolic dysfunction of skeletal muscle in obesity and their underlying mechanisms. EGCG works by increasing the expression of antioxidant enzymes, by reversing the increase of reactive oxygen species (ROS) production in skeletal muscle and regulating mitochondria-involved autophagy. Moreover, EGCG increases muscle lipid oxidation and stimulates glucose uptake in insulin-resistant skeletal muscle. EGCG acts by modulating cell signaling including the NF-κB, AMP-activated protein kinase (AMPK), and mitogen-activated protein kinase (MAPK) signaling pathways, and through epigenetic mechanisms such as DNA methylation and histone acetylation. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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26 pages, 2466 KiB  
Review
Polyphenol Health Effects on Cardiovascular and Neurodegenerative Disorders: A Review and Meta-Analysis
by Francesco Potì, Daniele Santi, Giorgia Spaggiari, Francesca Zimetti and Ilaria Zanotti
Int. J. Mol. Sci. 2019, 20(2), 351; https://doi.org/10.3390/ijms20020351 - 16 Jan 2019
Cited by 175 | Viewed by 9936
Abstract
Several studies have demonstrated that polyphenol-enriched diets may have beneficial effects against the development of degenerative diseases, including atherosclerosis and disorders affecting the central nervous system. This activity has been associated not only with antioxidant and anti-inflammatory properties, but also with additional mechanisms, [...] Read more.
Several studies have demonstrated that polyphenol-enriched diets may have beneficial effects against the development of degenerative diseases, including atherosclerosis and disorders affecting the central nervous system. This activity has been associated not only with antioxidant and anti-inflammatory properties, but also with additional mechanisms, such as the modulation of lipid metabolism and gut microbiota function. However, long-term studies on humans provided controversial results, making the prediction of polyphenol impact on health uncertain. The aim of this review is to provide an overview and critical analysis of the literature related to the effects of the principal dietary polyphenols on cardiovascular and neurodegenerative disorders. We critically considered and meta-analyzed randomized controlled clinical trials involving subjects taking polyphenol-based supplements. Although some polyphenols might improve specific markers of cardiovascular risk and cognitive status, many inconsistent data are present in literature. Therefore, definitive recommendations for the use of these compounds in the prevention of cardiovascular disease and cognitive decline are currently not applicable. Once pivotal aspects for the definition of polyphenol bioactivity, such as the characterization of pharmacokinetics and safety, are addressed, it will be possible to have a clear picture of the realistic potential of polyphenols for disease prevention. Full article
(This article belongs to the Special Issue Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits)
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15 pages, 1595 KiB  
Review
Current Disease-Targets for Oleocanthal as Promising Natural Therapeutic Agent
by Antonio Segura-Carretero and Jose Antonio Curiel
Int. J. Mol. Sci. 2018, 19(10), 2899; https://doi.org/10.3390/ijms19102899 - 24 Sep 2018
Cited by 24 | Viewed by 6870
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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