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Polyphenols: Nutrition, Physiology, Metabolism and Health Benefits 2019

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 August 2019) | Viewed by 74815

Special Issue Editors


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Guest Editor
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

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Guest Editor
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 (12 papers)

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Research

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13 pages, 3880 KiB  
Article
Resveratrol Treatment Enhances the Cellular Response to Leptin by Increasing OBRb Content in Palmitate-Induced Steatotic HepG2 Cells
by Andrea Ardid-Ruiz, Maria Ibars, Pedro Mena, Daniele Del Rio, Begoña Muguerza, Lluís Arola, Gerard Aragonès and Manuel Suárez
Int. J. Mol. Sci. 2019, 20(24), 6282; https://doi.org/10.3390/ijms20246282 - 12 Dec 2019
Cited by 13 | Viewed by 4237
Abstract
The interaction of leptin with its hepatic longest receptor (OBRb) promotes the phosphorylation of signal transducer and activator of transcription-3 (STAT3), protecting the liver from lipid accumulation. However, leptin signalling is disrupted in hepatic steatosis, causing leptin resistance. One promising strategy to combat [...] Read more.
The interaction of leptin with its hepatic longest receptor (OBRb) promotes the phosphorylation of signal transducer and activator of transcription-3 (STAT3), protecting the liver from lipid accumulation. However, leptin signalling is disrupted in hepatic steatosis, causing leptin resistance. One promising strategy to combat this problem is the use of bioactive compounds such as polyphenols. Since resveratrol (RSV) is a modulator of lipid homeostasis in the liver, we investigated whether treatment with different doses of RSV restores appropriate leptin action and fat accumulation in palmitate-induced steatotic human hepatoma (HepG2) cells. Both RSV metabolism and the expression of molecules implicated in leptin signalling were analysed. RSV at a 10 μM concentration was entirely metabolized to resveratrol-3-sulfate after 24 and counteracted leptin resistance by increasing the protein levels of OBRb. In addition, RSV downregulated the expression of lipogenic genes including fatty acid synthase (Fas) and stearoyl-CoA desaturase-1 (Scd1) without any significant change in Sirtuin-1 (SIRT1) enzymatic activity. These results demonstrate that RSV restored leptin sensitivity in a cellular model of hepatic steatosis in a SIRT1-independent manner. Full article
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15 pages, 1621 KiB  
Article
Stability and Fermentability of Green Tea Flavonols in In-Vitro-Simulated Gastrointestinal Digestion and Human Fecal Fermentation
by Chan-Su Rha, Hyunbin Seong, Young Sung Jung, Davin Jang, Jun-Gu Kwak, Dae-Ok Kim and Nam Soo Han
Int. J. Mol. Sci. 2019, 20(23), 5890; https://doi.org/10.3390/ijms20235890 - 24 Nov 2019
Cited by 23 | Viewed by 4385
Abstract
Flavonols, the second most abundant flavonoids in green tea, exist mainly in the form of glycosides. Flavonols are known to have a variety of beneficial health effects; however, limited information is available on their fate in the digestive system. We investigated the digestive [...] Read more.
Flavonols, the second most abundant flavonoids in green tea, exist mainly in the form of glycosides. Flavonols are known to have a variety of beneficial health effects; however, limited information is available on their fate in the digestive system. We investigated the digestive stability of flavonol aglycones and glycosides from green tea under simulated digestion and anaerobic human fecal fermentation. Green tea fractions rich in flavonol glycosides and aglycones, termed flavonol-glycoside-rich fraction (FLG) and flavonol-aglycone-rich fraction (FLA) hereafter, were obtained after treatment with cellulase and tannase, respectively. Kaempferol and its glycosides were found to be more stable in simulated gastric and intestinal fluids than the derivatives of quercetin and myricetin. Anaerobic human fecal fermentation with FLG and FLA increased the populations of Lactobacilli spp. and Bifidobacteria spp. and generated various organic acids, such as acetate, butyrate, propionate, and lactate, among which butyrate was produced in the highest amount. Our findings indicate that some stable polyphenols have higher bioaccessibilities in the gastrointestinal tract and that their health-modulating effects result from their interactions with microbes in the gut. Full article
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11 pages, 2158 KiB  
Article
Quercetin Directly Targets JAK2 and PKCδ and Prevents UV-Induced Photoaging in Human Skin
by Eun Ju Shin, Ji Su Lee, Seungpyo Hong, Tae-Gyu Lim and Sanguine Byun
Int. J. Mol. Sci. 2019, 20(21), 5262; https://doi.org/10.3390/ijms20215262 - 23 Oct 2019
Cited by 51 | Viewed by 5646
Abstract
Quercetin is a naturally occurring polyphenol present in various fruits and vegetables. The bioactive properties of quercetin include anti-oxidative, anti-cancer, anti-inflammatory, and anti-diabetic effects. However, the effect of quercetin on skin aging and the direct molecular targets responsible have remained largely unknown. Herein, [...] Read more.
Quercetin is a naturally occurring polyphenol present in various fruits and vegetables. The bioactive properties of quercetin include anti-oxidative, anti-cancer, anti-inflammatory, and anti-diabetic effects. However, the effect of quercetin on skin aging and the direct molecular targets responsible have remained largely unknown. Herein, we investigated the protective effect of quercetin against UV-mediated skin aging and the molecular mechanisms responsible. Treatment with quercetin suppressed UV-induced matrix metalloproteinase-1 (MMP-1) and cyclooxygenase-2 (COX-2) expression and prevented UV-mediated collagen degradation in human skin tissues. Quercetin exerted potent inhibitory effects towards UV-induced activator protein-1 (AP-1) and nuclear factor-kappa B (NF-κB) activity. Further examination of the upstream signaling pathways revealed that quercetin can attenuate UV-mediated phosphorylation of extracellular signal-regulated kinase (ERK), c-Jun N terminal kinases (JNK), protein kinase B (Akt), and signal transducer and activator of transcription 3 (STAT3). Kinase assays using purified protein demonstrated that quercetin can directly inhibit protein kinase C delta (PKCδ) and Janus kinase 2 (JAK2) kinase activity. Quercetin was observed to bind to PKCδ and JAK2 in pull-down assays. These findings suggest that quercetin can directly target PKCδ and JAK2 in the skin to elicit protective effects against UV-mediated skin aging and inflammation. Our results highlight the potential use of quercetin as a natural agent for anti-skin aging applications. Full article
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13 pages, 1201 KiB  
Article
Quercetin, a Promising Clinical Candidate for The Prevention of Contrast-Induced Nephropathy
by Laura Vicente-Vicente, David González-Calle, Alfredo Ginés Casanova, María Teresa Hernández-Sánchez, Marta Prieto, Juan Carlos Rama-Merchán, Javier Martín-Moreiras, Francisco Martín-Herrero, Pedro Luis Sánchez, Francisco J. López-Hernández, Ignacio Cruz-González and Ana Isabel Morales
Int. J. Mol. Sci. 2019, 20(19), 4961; https://doi.org/10.3390/ijms20194961 - 08 Oct 2019
Cited by 16 | Viewed by 5916
Abstract
Iodinated contrast media (CM) are the leading cause of acute renal failure of toxic origin. Between 21% and 50% of patients that receive them develop contrast-induced nephropathy (CIN). All prophylactic measures used so far have failed to provide effective prevention. Since oxidative stress [...] Read more.
Iodinated contrast media (CM) are the leading cause of acute renal failure of toxic origin. Between 21% and 50% of patients that receive them develop contrast-induced nephropathy (CIN). All prophylactic measures used so far have failed to provide effective prevention. Since oxidative stress is involved in the damage, a possible preventive strategy could be the administration of antioxidant substances, such as quercetin. This compound has shown renoprotective effects in experimental studies. The aim of this study was to evaluate whether quercetin may be helpful in preventing CIN in patients undergoing coronary catheterization. A clinical phase II study was conducted. Patients were distributed in two groups, namely, CM (patients who only received contrast media) and CM+Q (patients who were pretreated with quercetin orally for 3–5 days). Results showed less incidence of CIN in the CM+Q group, possibly due to glomerular protection, evidenced by a lower increase in serum creatinine and albuminuria; and a lower decrease in the glomerular filtration rate (GFR). Furthermore, in this group, the relative risk of developing CIN observed in patients that received a high dose of contrast media was inferior. In conclusion, this is the first study that demonstrates that quercetin is a promising safe candidate in preventing CIN. Full article
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24 pages, 3694 KiB  
Article
Quercetin Inhibits the Production of IL-1β-Induced Inflammatory Cytokines and Chemokines in ARPE-19 Cells via the MAPK and NF-κB Signaling Pathways
by Shu-Chen Cheng, Wen-Chung Huang, Jong-Hwei S. Pang, Yi-Hong Wu and Ching-Yi Cheng
Int. J. Mol. Sci. 2019, 20(12), 2957; https://doi.org/10.3390/ijms20122957 - 17 Jun 2019
Cited by 135 | Viewed by 7783
Abstract
Quercetin, a bioflavonoid derived from vegetables and fruits, exerts anti-inflammatory effects in various diseases. Our previous study revealed that quercetin could suppress the expression of matrix metalloprotease-9 (MMP-9) and intercellular adhesion molecule-1 (ICAM-1) to achieve anti-inflammatory effects in tumor necrosis factor-α (TNF-α)-stimulated human [...] Read more.
Quercetin, a bioflavonoid derived from vegetables and fruits, exerts anti-inflammatory effects in various diseases. Our previous study revealed that quercetin could suppress the expression of matrix metalloprotease-9 (MMP-9) and intercellular adhesion molecule-1 (ICAM-1) to achieve anti-inflammatory effects in tumor necrosis factor-α (TNF-α)-stimulated human retinal pigment epithelial (ARPE-19) cells. The present study explored whether quercetin can inhibit the interleukin-1β (IL-1β)-induced production of inflammatory cytokines and chemokines in ARPE-19 cells. Prior to stimulation by IL-1β, ARPE-19 cells were pretreated with quercetin at various concentrations (2.5–20 µM). The results showed that quercetin could dose-dependently decrease the mRNA and protein levels of ICAM-1, IL-6, IL-8 and monocyte chemoattractant protein-1 (MCP-1). It also attenuated the adherence of the human monocytic leukemia cell line THP-1 to IL-1β-stimulated ARPE-19 cells. We also demonstrated that quercetin inhibited signaling pathways related to the inflammatory process, including phosphorylation of mitogen-activated protein kinases (MAPKs), inhibitor of nuclear factor κ-B kinase (IKK)α/β, c-Jun, cAMP response element-binding protein (CREB), activating transcription factor 2 (ATF2) and nuclear factor (NF)-κB p65, and blocked the translocation of NF-κB p65 into the nucleus. Furthermore, MAPK inhibitors including an extracellular signal-regulated kinase (ERK) 1/2 inhibitor (U0126), a p38 inhibitor (SB202190) and a c-Jun N-terminal kinase (JNK) inhibitor (SP600125) decreased the expression of soluble ICAM-1 (sICAM-1), but not ICAM-1. U0126 and SB202190 could inhibit the expression of IL-6, IL-8 and MCP-1, but SP600125 could not. An NF-κB inhibitor (Bay 11-7082) also reduced the expression of ICAM-1, sICAM-1, IL-6, IL-8 and MCP-1. Taken together, these results provide evidence that quercetin protects ARPE-19 cells from the IL-1β-stimulated increase in ICAM-1, sICAM-1, IL-6, IL-8 and MCP-1 production by blocking the activation of MAPK and NF-κB signaling pathways to ameliorate the inflammatory response. Full article
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14 pages, 3289 KiB  
Article
2, 3, 4′, 5-tetrahydroxystilbene-2-0-β-d Glycoside Attenuates Age- and Diet-Associated Non-Alcoholic Steatohepatitis and Atherosclerosis in LDL Receptor Knockout Mice and Its Possible Mechanisms
by Jin Xu, Yi Peng, Yi Zeng, Yi-qiao Hua and Xiao-le Xu
Int. J. Mol. Sci. 2019, 20(7), 1617; https://doi.org/10.3390/ijms20071617 - 01 Apr 2019
Cited by 25 | Viewed by 3482
Abstract
The compound, 2,3,5,4′-tetrahydroxystilbene-2-O-β-d-glucoside (TSG), a primary bioactive polyphenolic component of Polygonum multiflorum exerts numerous pharmacological activities. However, its protective effect against non-alcoholic steatohepatitis (NASH), in the context of metabolic syndrome, remains poorly understood. The aim of the present study is to [...] Read more.
The compound, 2,3,5,4′-tetrahydroxystilbene-2-O-β-d-glucoside (TSG), a primary bioactive polyphenolic component of Polygonum multiflorum exerts numerous pharmacological activities. However, its protective effect against non-alcoholic steatohepatitis (NASH), in the context of metabolic syndrome, remains poorly understood. The aim of the present study is to evaluate the effects of TSG treatment on middle-aged (12-mo-old) male LDLr−/− mice, which were fed a high fat diet for 12 weeks to induce metabolic syndrome and NASH. At the end of the experiment, the blood samples of mice were collected for determination of metabolic parameters. Liver and aorta tissues were collected for analysis, such as histology, immunofluorescence, hepatic lipid content, real-time PCR, and western blot. Our data show that TSG treatment improved the different aspects of NASH (steatosis, inflammation, and fibrosis) and atherosclerosis, as well as some of the metabolic basal characteristics. These modulatory effects of TSG are mediated, at least in part, through regulating key regulators of lipid metabolism (SREBP1c, PPARα and their target genes, ABCG5 and CYP7A1), inflammation (CD68, TNF-α, IL-6 and ICAM), fibrosis (α-SMA and TNFβ) and oxidative stress (NADPH-oxidase 2/4, CYP2E1 and antioxidant enzymes). These results suggest that TSG may be a promising candidate for preventing and treating the progression of NASH. Full article
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10 pages, 1057 KiB  
Communication
Intestinal Permeability Study of Clinically Relevant Formulations of Silibinin in Caco-2 Cell Monolayers
by Almudena Pérez-Sánchez, Elisabet Cuyàs, Verónica Ruiz-Torres, Luz Agulló-Chazarra, Sara Verdura, Isabel González-Álvarez, Marival Bermejo, Jorge Joven, Vicente Micol, Joaquim Bosch-Barrera and Javier A. Menendez
Int. J. Mol. Sci. 2019, 20(7), 1606; https://doi.org/10.3390/ijms20071606 - 31 Mar 2019
Cited by 32 | Viewed by 6428
Abstract
An ever-growing number of preclinical studies have investigated the tumoricidal activity of the milk thistle flavonolignan silibinin. The clinical value of silibinin as a bona fide anti-cancer therapy, however, remains uncertain with respect to its bioavailability and blood–brain barrier (BBB) permeability. To shed [...] Read more.
An ever-growing number of preclinical studies have investigated the tumoricidal activity of the milk thistle flavonolignan silibinin. The clinical value of silibinin as a bona fide anti-cancer therapy, however, remains uncertain with respect to its bioavailability and blood–brain barrier (BBB) permeability. To shed some light on the absorption and bioavailability of silibinin, we utilized the Caco-2 cell monolayer model of human intestinal absorption to evaluate the permeation properties of three different formulations of silibinin: silibinin-meglumine, a water-soluble form of silibinin complexed with the amino-sugar meglumine; silibinin-phosphatidylcholine, the phytolipid delivery system Siliphos; and Eurosil85/Euromed, a milk thistle extract that is the active component of the nutraceutical Legasil with enhanced bioavailability. Our approach predicted differential mechanisms of transport and blood–brain barrier permeabilities between the silibinin formulations tested. Our assessment might provide valuable information about an idoneous silibinin formulation capable of reaching target cancer tissues and accounting for the observed clinical effects of silibinin, including a recently reported meaningful central nervous system activity against brain metastases. Full article
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16 pages, 979 KiB  
Article
Polyphenols and IUGR Pregnancies: Effects of Maternal Hydroxytyrosol Supplementation on Placental Gene Expression and Fetal Antioxidant Status, DNA-Methylation and Phenotype
by Consolación Garcia-Contreras, Marta Vazquez-Gomez, Alicia Barbero, José Luis Pesantez, Angelo Zinellu, Fiammetta Berlinguer, Pedro Gonzalez-Añover, Jorge Gonzalez, Teresa Encinas, Laura Torres-Rovira, Yolanda Nuñez, Jaime Ballesteros, Miriam Ayuso, Susana Astiz, Beatriz Isabel, Cristina Ovilo and Antonio Gonzalez-Bulnes
Int. J. Mol. Sci. 2019, 20(5), 1187; https://doi.org/10.3390/ijms20051187 - 08 Mar 2019
Cited by 27 | Viewed by 4016
Abstract
The use of polyphenols is a promising strategy for preventing or alleviating intrauterine growth restriction (IUGR) because polyphenol supplementation increases plasma antioxidant capacity and improves oxidative stress at the feto-placental unit; which are recognized as main issues in IUGR. However, there is a [...] Read more.
The use of polyphenols is a promising strategy for preventing or alleviating intrauterine growth restriction (IUGR) because polyphenol supplementation increases plasma antioxidant capacity and improves oxidative stress at the feto-placental unit; which are recognized as main issues in IUGR. However, there is a scarcity of experimental data on both realistic benefits and potential hazards of polyphenol supplementation during gestation. Hence, we aimed to use a swine model of IUGR pregnancy to determine possible effects of maternal supplementation with polyphenols (hydroxytyrosol) on placental expression of genes involved in antioxidant homeostasis, vascularization and fetal growth and thus on antioxidant status, DNA-methylation and phenotypic traits (morphology and homeostasis) of the fetus. Hydroxytyrosol improves placental gene expression and fetal antioxidant status and glucose metabolism in a sex-dependent manner, in which males were favored in spite of developmental failures. Concomitantly, hydroxytyrosol prevented hypomethylation of DNA associated with oxidative stress. Finally, no major deleterious effects of hydroxytyrosol supplementation on constriction of the ductus arteriosus, a possible secondary effect of polyphenols during pregnancy, were found. Full article
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Review

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14 pages, 2119 KiB  
Review
Tumor PD-L1 Induction by Resveratrol/Piceatannol May Function as a Search, Enhance, and Engage (“SEE”) Signal to Facilitate the Elimination of “Cold, Non-Responsive” Low PD-L1-Expressing Tumors by PD-L1 Blockade
by Tze-Chen Hsieh and Joseph M. Wu
Int. J. Mol. Sci. 2019, 20(23), 5969; https://doi.org/10.3390/ijms20235969 - 27 Nov 2019
Cited by 9 | Viewed by 3656
Abstract
Programmed cell death ligand 1 (PD-L1) is an immune regulatory protein that facilitates tumor escape from host immune surveillance. In the clinic, tumors with high level of PD-L1 have been used to identify patients who might respond favorably to treatment by anti-PD-L1 antibodies [...] Read more.
Programmed cell death ligand 1 (PD-L1) is an immune regulatory protein that facilitates tumor escape from host immune surveillance. In the clinic, tumors with high level of PD-L1 have been used to identify patients who might respond favorably to treatment by anti-PD-L1 antibodies (PD-L1 blockade, PLB). Typically, a progression-free response of 9–20% to PLB has been observed, the basis for the low success rate is largely unknown. Recently, we show upregulation of PD-L1 in cancer cells by ≥IC50 supra-pharmacological dose of grape polyphenol resveratrol and piceatannol, alone and combined. Herein, we summarize recent published studies on the regulation of tumor PD-L1 by flavonoids and grape polyphenols. We hypothesize that the induced tumor PD-L1 by resveratrol and/or piceatannol may serve as a Search, Enhance, and Engage (“SEE”) signal to sensitize and augment the recognition and detection of low PD-L1-expressing “cold, non-responsive” tumors. The “SEE” strategy enhances the “visibility” of previously unidentified tumor cells for targeting and eventual eradication by the host antitumor activity. This strategy expands the selection criteria for patients with improved sensitivity and potential responsiveness when used in combination with PLB. The modulation of tumor PD-L1 by flavonoids or polyphenols is proposed to improve the response to PLB in low PD-L1 tumors. Full article
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42 pages, 7424 KiB  
Review
Combinatorial Epigenetics Impact of Polyphenols and Phytochemicals in Cancer Prevention and Therapy
by Itika Arora, Manvi Sharma and Trygve O. Tollefsbol
Int. J. Mol. Sci. 2019, 20(18), 4567; https://doi.org/10.3390/ijms20184567 - 14 Sep 2019
Cited by 116 | Viewed by 11000
Abstract
Polyphenols are potent micronutrients that can be found in large quantities in various food sources and spices. These compounds, also known as phenolics due to their phenolic structure, play a vital nutrient-based role in the prevention of various diseases such as diabetes, cardiovascular [...] Read more.
Polyphenols are potent micronutrients that can be found in large quantities in various food sources and spices. These compounds, also known as phenolics due to their phenolic structure, play a vital nutrient-based role in the prevention of various diseases such as diabetes, cardiovascular diseases, neurodegenerative diseases, liver disease, and cancers. However, the function of polyphenols in disease prevention and therapy depends on their dietary consumption and biological properties. According to American Cancer Society statistics, there will be an expected rise of 23.6 million new cancer cases by 2030. Due to the severity of the increased risk, it is important to evaluate various preventive measures associated with cancer. Relatively recently, numerous studies have indicated that various dietary polyphenols and phytochemicals possess properties of modifying epigenetic mechanisms that modulate gene expression resulting in regulation of cancer. These polyphenols and phytochemicals, when administrated in a dose-dependent and combinatorial-based manner, can have an enhanced effect on epigenetic changes, which play a crucial role in cancer prevention and therapy. Hence, this review will focus on the mechanisms of combined polyphenols and phytochemicals that can impact various epigenetic modifications such as DNA methylation and histone modifications as well as regulation of non-coding miRNAs expression for treatment and prevention of various types of cancer. Full article
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23 pages, 1881 KiB  
Review
Overview of the Anticancer Profile of Avenanthramides from Oat
by Eleonora Turrini, Francesca Maffei, Andrea Milelli, Cinzia Calcabrini and Carmela Fimognari
Int. J. Mol. Sci. 2019, 20(18), 4536; https://doi.org/10.3390/ijms20184536 - 13 Sep 2019
Cited by 34 | Viewed by 5508
Abstract
Cancer represents one of the leading causes of death worldwide. Progresses in treatment of cancer have continued at a rapid pace. However, undesirable side effects and drug resistance remain major challenges for therapeutic success. Natural products represent a valuable starting point to develop [...] Read more.
Cancer represents one of the leading causes of death worldwide. Progresses in treatment of cancer have continued at a rapid pace. However, undesirable side effects and drug resistance remain major challenges for therapeutic success. Natural products represent a valuable starting point to develop new anticancer strategies. Polyphenols, well-known as antioxidant, exert anticancer effects through the modulation of multiple pathways and mechanisms. Oat (Avena sativa L., Poaceae) is a unique source of avenanthramides (AVAs), a group of polyphenolic alkaloids, considered as its signature compounds. The present review aims to offer a comprehensive and critical perspective on the chemopreventive and chemotherapeutic potential of AVAs. AVAs prevent cancer mainly by blocking reactive species. Moreover, they exhibit potential therapeutic activity through the modulation of different pathways including the activation of apoptosis and senescence, the block of cell proliferation, and the inhibition of epithelial mesenchymal transition and metastatization. AVAs are promising chemopreventive and anticancer phytochemicals, which need further clinical trials and toxicological studies to define their efficacy in preventing and reducing the burden of cancer diseases. Full article
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42 pages, 1316 KiB  
Review
Is Chickpea a Potential Substitute for Soybean? Phenolic Bioactives and Potential Health Benefits
by Adriano Costa de Camargo, Bruno Trevenzoli Favero, Maressa Caldeira Morzelle, Marcelo Franchin, Emilio Alvarez-Parrilla, Laura A. de la Rosa, Marina Vilar Geraldi, Mário Roberto Maróstica Júnior, Fereidoon Shahidi and Andrés R. Schwember
Int. J. Mol. Sci. 2019, 20(11), 2644; https://doi.org/10.3390/ijms20112644 - 29 May 2019
Cited by 85 | Viewed by 11848
Abstract
Legume seeds are rich sources of protein, fiber, and minerals. In addition, their phenolic compounds as secondary metabolites render health benefits beyond basic nutrition. Lowering apolipoprotein B secretion from HepG2 cells and decreasing the level of low-density lipoprotein (LDL)-cholesterol oxidation are mechanisms related [...] Read more.
Legume seeds are rich sources of protein, fiber, and minerals. In addition, their phenolic compounds as secondary metabolites render health benefits beyond basic nutrition. Lowering apolipoprotein B secretion from HepG2 cells and decreasing the level of low-density lipoprotein (LDL)-cholesterol oxidation are mechanisms related to the prevention of cardiovascular diseases (CVD). Likewise, low-level chronic inflammation and related disorders of the immune system are clinical predictors of cardiovascular pathology. Furthermore, DNA-damage signaling and repair are crucial pathways to the etiology of human cancers. Along CVD and cancer, the prevalence of obesity and diabetes is constantly increasing. Screening the ability of polyphenols in inactivating digestive enzymes is a good option in pre-clinical studies. In addition, in vivo studies support the role of polyphenols in the prevention and/or management of diabetes and obesity. Soybean, a well-recognized source of phenolic isoflavones, exerts health benefits by decreasing oxidative stress and inflammation related to the above-mentioned chronic ailments. Similar to soybeans, chickpeas are good sources of nutrients and phenolic compounds, especially isoflavones. This review summarizes the potential of chickpea as a substitute for soybean in terms of health beneficial outcomes. Therefore, this contribution may guide the industry in manufacturing functional foods and/or ingredients by using an undervalued feedstock. Full article
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