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Antioxidants
Special Issues
Bioactive Metabolites of Antioxidants
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Bioactive Metabolites of Antioxidants

A special issue of Antioxidants (ISSN 2076-3921). This special issue belongs to the section "Natural and Synthetic Antioxidants".

Deadline for manuscript submissions: closed (10 December 2022) | Viewed by 2163

Special Issue Editors

Dr. Attila Hunyadi

E-Mail Website
Guest Editor
1. Institute of Pharmacognosy, Interdisciplinary Excellence Centre, University of Szeged, Eötvös str. 6, H-6720 Szeged, Hungary
2. Interdisciplinary Centre for Natural Products, University of Szeged, Eötvös str. 6, H-6720 Szeged, Hungary
Interests: antioxidant-inspired drug discovery; chemistry and bioactivity of antioxidant metabolites; efflux-mediated multi-drug resistance
Special Issues, Collections and Topics in MDPI journals
Dr. György Tibor Balogh

E-Mail Website
Guest Editor
Department of Chemical and Environmental Process Engineering, Budapest University of Technology and Economics, Műegyetem Quay 3, H-1111 Budapest, Hungary
Interests: medicinal chemistry; analytical chemistry; antioxidant-inspired drug; characterization
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Small-molecule dietary antioxidants exert a remarkably broad range of bioactivities, and many of these can be explained by the influence of antioxidants on redox homeostasis. Such compounds help to modulate the levels of harmful reactive oxygen/nitrogen species (ROS/RNS), and therefore participate in the regulation of various redox signaling pathways. However, upon ingestion, antioxidants usually undergo extensive metabolic transformation, which generates a wide range of bioactive metabolites that all contribute to the complex and frequently hard-to-decipher bioactivity profile observed upon treatment with their parent compound. It is also an intriguing notion that antioxidants by nature are sensitive to any kind of oxidation, including that by ROS/RNS, and minor, locally produced “chemical metabolites” should therefore also contribute to the complexity of antioxidant metabolite patterns.

Because of this, every small-molecule antioxidant should also be considered as a core to a vast and diverse chemical space of many metabolites, and exploring the corresponding chemical-pharmacological complexity is of key importance to solving the challenging puzzle of any antioxidant’s bioactivity.

The present Special Issue of Antioxidants is dedicated to outstanding research and review papers within the scope of bioactive metabolites of small-molecule antioxidants. Research papers focusing on any aspects of antioxidant metabolites are welcome, including but not limited to their formation, chemical, physicochemical, pharmacokinetic and pharmacodynamic description, and possible drug discovery potential either through a better understanding of how the parent antioxidant works, or as semi-synthetic derivatives to be used in their own right. Authors of review papers are kindly requested to make a pre-submission inquiry with a brief outline to the Guest Editors.

We are looking forward to your valuable contribution(s).

Sincerely yours,

Dr. Attila Hunyadi
Dr. György Tibor Balogh
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 submissions that pass pre-check are 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. Antioxidants 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 2900 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

  • antioxidant metabolites
  • redox metabolism
  • chemical space expansion
  • biomimetic oxidation
  • drug discovery

Published Papers (1 paper)

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Research

14 pages, 914 KiB  
Article
Oxidized Resveratrol Metabolites as Potent Antioxidants and Xanthine Oxidase Inhibitors
by Orinamhe G. Agbadua, Norbert Kúsz, Róbert Berkecz, Tamás Gáti, Gábor Tóth and Attila Hunyadi
Antioxidants 2022, 11(9), 1832; https://doi.org/10.3390/antiox11091832 - 17 Sep 2022
Cited by 6 | Viewed by 1660
Abstract
Resveratrol is a well-known natural polyphenol with a plethora of pharmacological activities. As a potent antioxidant, resveratrol is highly oxidizable and readily reacts with reactive oxygen species (ROS). Such a reaction not only leads to a decrease in ROS levels in a biological [...] Read more.
Resveratrol is a well-known natural polyphenol with a plethora of pharmacological activities. As a potent antioxidant, resveratrol is highly oxidizable and readily reacts with reactive oxygen species (ROS). Such a reaction not only leads to a decrease in ROS levels in a biological environment but may also generate a wide range of metabolites with altered bioactivities. Inspired by this notion, in the current study, our aim was to take a diversity-oriented chemical approach to study the chemical space of oxidized resveratrol metabolites. Chemical oxidation of resveratrol and a bioactivity-guided isolation strategy using xanthine oxidase (XO) and radical scavenging activities led to the isolation of a diverse group of compounds, including a chlorine-substituted compound (2), two iodine-substituted compounds (3 and 4), two viniferins (5 and 6), an ethoxy-substituted compound (7), and two ethoxy-substitute,0d dimers (8 and 9). Compounds 4, 7, 8, and 9 are reported here for the first time. All compounds without ethoxy substitution exerted stronger XO inhibition than their parent compound, resveratrol. By enzyme kinetic and in silico docking studies, compounds 2 and 4 were identified as potent competitive inhibitors of the enzyme, while compound 3 and the viniferins acted as mixed-type inhibitors. Further, compounds 2 and 9 had better DPPH scavenging activity and oxygen radical absorbing capacity than resveratrol. Our results suggest that the antioxidant activity of resveratrol is modulated by the effect of a cascade of chemically stable oxidized metabolites, several of which have significantly altered target specificity as compared to their parent compound. Full article
(This article belongs to the Special Issue Bioactive Metabolites of Antioxidants)
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