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Special Issue "New Trends in Polyphenols and Health"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 30 September 2021.

Special Issue Editors

Dr. Marisa Freitas
E-Mail Website
Guest Editor
LAQV, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: inflammation; polyphenols; structure-activity relationships, nanotoxicity; diabetes
Special Issues and Collections in MDPI journals
Dr. Daniela Ribeiro
E-Mail Website
Guest Editor
LAQV, REQUIMTE, Faculdade de Ciências Agrárias e do Ambiente, Universidade dos Açores, 9700-042 Angra do Heroísmo, Portugal
Interests: antioxidants; inflammation; structure-activity relationships; polyphenols
Special Issues and Collections in MDPI journals
Prof. Dr. Eduarda Fernandes
E-Mail Website
Guest Editor
LAQV, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: antioxidants; inflammation; diabetes; obesity; structure-activity relationships; polyphenols; nanotoxicity

Special Issue Information

Dear Colleagues,

Polyphenols are characterized by the presence of one or more phenolic groups in a chemical structure, varying from simple phenolic molecules to complex high-molecular-weight polymers. Naturally occurring polyphenols are highly diversified and encompass various chemical groups, such as phenolic acids, stilbenes, flavonoids, and lignans, with thousands of members in each group. These compounds have been identified in edible and non-edible plants, and can be found mainly in fruits, vegetables, and cereals. Innumerous biological activities have been attributed to polyphenols, namely, antioxidant, anti-inflammatory, anticancer, antidiabetic, and antiobesity, among others.

There have been several in vitro studies covering the health benefits of polyphenols. However, the poor bioavailability and extensive metabolism of these compounds restrict their biological effects in vivo. Moreover, there is a need to study a high number of compounds in panels of structurally related polyphenols in order to allow the establishment of accurate structure-activity relationships, which will favor the choice of the most promising scaffolds regarding each specific disease.

Therefore, the main, but not exclusive, topics to be dealt with in this Special Issue are the following:

  • Biological activities of different groups of polyphenols;
  • Strategies to overcome the poor bioavailability of polyphenols;
  • Establishment of structure-activity relationships;
  • Validation of new methods to evaluate the beneficial effects of polyphenols on human health.

We would like to invite you to participate in this Special Issue on “New Trends in Polyphenols and Health” by submitting a contribution in the form of an original research paper, short communication, and/or global or specialized critical review according to your field of expertise. Papers will be published upon acceptance, regardless of the Special Issue publication date (30 September 2021).

Dr. Marisa Freitas
Dr. Daniela Ribeiro
Prof. Dr. Eduarda Fernandes
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. Molecules is an international peer-reviewed open access semimonthly 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 2000 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

  • Polyphenols
  • Biological activity
  • Nanoencapsulation
  • Structure-activity relationship

Published Papers (4 papers)

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Research

Article
Efficacy of Caffeic Acid on Diabetes and Its Complications in the Mouse
Molecules 2021, 26(11), 3262; https://doi.org/10.3390/molecules26113262 - 28 May 2021
Viewed by 514
Abstract
Diabetic dyslipidemia and hyperglycemia contribute to excessive reactive oxygen species (ROS) production, leading to deleterious complications, such as nephropathy, atherosclerosis and cardiac dysfunction, and target major organs in the body. The aim of this study was to investigate the effect of caffeic acid [...] Read more.
Diabetic dyslipidemia and hyperglycemia contribute to excessive reactive oxygen species (ROS) production, leading to deleterious complications, such as nephropathy, atherosclerosis and cardiac dysfunction, and target major organs in the body. The aim of this study was to investigate the effect of caffeic acid (CA) on mouse weight and survival, serum level of fasting blood glucose (FBG), serum lipid parameters and atherogenic indices, oxidative damage in blood, liver and kidney tissue, pathophysiological changes and their function markers in healthy and alloxan-induced type 1 diabetic mice. Diabetes was induced in mice with a single intravenous injection of alloxan (75 mg kg−1). Two days later, CA (50 mg kg−1) was given intraperitoneally for seven days in diabetic mice. Diabetes affected glucose level, lipid profile, hematological and biochemical parameters, induced DNA damage and apoptotic/necrotic death in whole blood cells, liver and kidney, leading to weight loss and a decreased lifespan. CA treatment of diabetic mice revealed a protective effect on the liver and kidney, hypoglycemic and hypolipidemic properties and high protection against atherogenic outcomes. The obtained results suggest that CA is a safe and potent agent against diabetes that acts as an effective antioxidant in reducing serum glucose, lipid profile and atherogenic indices, leading to increased lifespan in mice. Full article
(This article belongs to the Special Issue New Trends in Polyphenols and Health)
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Article
Novel Semi-Synthetic Cu (II)–Cardamonin Complex Exerts Potent Anticancer Activity against Triple-Negative Breast and Pancreatic Cancer Cells via Inhibition of the Akt Signaling Pathway
Molecules 2021, 26(8), 2166; https://doi.org/10.3390/molecules26082166 - 09 Apr 2021
Viewed by 415
Abstract
Cardamonin is a polyphenolic natural product that has been shown to possess cytotoxic activity against a variety of cancer cell lines. We previously reported the semi-synthesis of a novel Cu (II)–cardamonin complex (19) that demonstrated potent antitumour activity. In this study, [...] Read more.
Cardamonin is a polyphenolic natural product that has been shown to possess cytotoxic activity against a variety of cancer cell lines. We previously reported the semi-synthesis of a novel Cu (II)–cardamonin complex (19) that demonstrated potent antitumour activity. In this study, we further investigated the bioactivity of 19 against MDA-MB-468 and PANC-1 cancer cells in an attempt to discover an effective treatment for triple-negative breast cancer (TNBC) and pancreatic cancer, respectively. Results revealed that 19 abolished the formation of MDA-MB-468 and PANC-1 colonies, exerted growth-inhibitory activity, and inhibited cancer cell migration. Further mechanistic studies showed that 19 induced DNA damage resulting in gap 2 (G2)/mitosis (M) phase arrest and microtubule network disruption. Moreover, 19 generated reactive oxygen species (ROS) that may contribute to induction of apoptosis, corroborated by activation of caspase-3/7, PARP cleavage, and downregulation of Mcl-1. Complex 19 also decreased the expression levels of p-Akt and p-4EBP1, which indicates that the compound exerts its activity, at least in part, via inhibition of Akt signalling. Furthermore, 19 decreased the expression of c-Myc in PANC-1 cells only, which suggests that it may exert its bioactivity via multiple mechanisms of action. These results demonstrate the potential of 19 as a therapeutic agent for TNBC and pancreatic cancer. Full article
(This article belongs to the Special Issue New Trends in Polyphenols and Health)
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Article
The Potential of Parsley Polyphenols and Their Antioxidant Capacity to Help in the Treatment of Depression and Anxiety: An In Vivo Subacute Study
Molecules 2021, 26(7), 2009; https://doi.org/10.3390/molecules26072009 - 01 Apr 2021
Viewed by 431
Abstract
Depression and anxiety are major mental health problems in all parts of the world. These illnesses are associated with a number of risk factors, including oxidative stress. Psychotropic drugs of a chemical nature have demonstrated several side effects that elevated the impact of [...] Read more.
Depression and anxiety are major mental health problems in all parts of the world. These illnesses are associated with a number of risk factors, including oxidative stress. Psychotropic drugs of a chemical nature have demonstrated several side effects that elevated the impact of those illnesses. Faced with this situation, natural products appear to be a promising alternative. The aim of this study was to evaluate the anxiolytic and antidepressant effects of the Petroselinum sativum polyphenols in vivo, as well as its correlated antioxidant properties in vitro. Anxiolytic activity of the extract (50 and 100 mg/kg) was evaluated using the open field and the light-dark chamber tests, while the antidepressant activity was evaluated using the forced swimming test. The antioxidant activity of the extract was evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical test and the FRAP (iron-reducing capacity) test. The phenolic extract showed very powerful anxiolytic and antidepressant-like effects, especially at a dose of 100 mg/kg, decreasing the depressive behavior in mice (decreased immobility time) and also the anxiolytic behavior (tendency for discovery in the center and illuminated areas) better even than those of paroxetine and bromazepam (classic drugs) concomitant with those results the extract also showed an important antioxidant capacity. These preliminary results suggest that Petroselinum sativum exhibits anxiolytic and antidepressant potential for use as a complement or independent phytomedicine to treat depression and anxiety. Full article
(This article belongs to the Special Issue New Trends in Polyphenols and Health)
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Article
Synthesis of Rottlerone Analogues and Evaluation of Their α-Glucosidase and DPP-4 Dual Inhibitory and Glucose Consumption-Promoting Activity
Molecules 2021, 26(4), 1024; https://doi.org/10.3390/molecules26041024 - 15 Feb 2021
Viewed by 615
Abstract
Our previous study found that desmethylxanthohumol (1) inhibited α-glucosidase in vitro. Recently, further investigations revealed that dehydrocyclodesmethylxanthohumol (2) and its dimer analogue rottlerone (3) exhibited more potent α-glucosidase inhibitory activity than 1. The aim of this [...] Read more.
Our previous study found that desmethylxanthohumol (1) inhibited α-glucosidase in vitro. Recently, further investigations revealed that dehydrocyclodesmethylxanthohumol (2) and its dimer analogue rottlerone (3) exhibited more potent α-glucosidase inhibitory activity than 1. The aim of this study was to synthesize a series of rottlerone analogues and evaluate their α-glucosidase and DPP-4 dual inhibitory activity. The results showed that compounds 4d and 5d irreversibly and potently inhibited α-glucosidase (IC50 = 0.22 and 0.12 μM) and moderately inhibited DPP-4 (IC50 = 23.59 and 26.19 μM), respectively. In addition, compounds 4d and 5d significantly promoted glucose consumption, with the activity of 5d at 0.2 μM being comparable to that of metformin at a concentration of 1 mM. Full article
(This article belongs to the Special Issue New Trends in Polyphenols and Health)
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