Multi-Target Profile of Antioxidant Compounds, including Repurposing and Combination Strategies

A special issue of Antioxidants (ISSN 2076-3921). This special issue belongs to the section "Health Outcomes of Antioxidants and Oxidative Stress".

Deadline for manuscript submissions: 30 September 2024 | Viewed by 3201

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Guest Editor
Dipartimento di Scienze della Salute, Università “Magna Graecia” di Catanzaro, Campus “Salvatore Venuta”, Viale Europa, 88100 Catanzaro, Italy
Interests: docking; nucleic acids; drug design; molecular modeling; molecular dynamics; virtual screening; drug repurposing; natural products
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Special Issue Information

Dear Colleagues,

Cancer, neurodegenerative disorders and stroke are just some examples of multifactorial diseases and often oxidative stress is a common event that occurs. Currently, there is no efficient and effective cure for these diseases; consequently, researchers have taken advantage of the multi-targeting drug approach to design molecules which may be developed as useful agents for their treatment. In this scenario, in silico techniques are considered as useful and powerful tools to enhance rational drug design in the medicinal chemistry field. The discovery, design, synthesis and biological evaluation of multi-targeting molecules combining antioxidant and/or anti-inflammatory properties are expected to be beneficial in the treatment of different multifactorial diseases.

The aim of the current Special Issue is to cover promising, recent, and novel research trends in the polypharmacologic field, focusing on antioxidant compounds. In particular, advancements in the design and synthesis of novel polypharmacological agents, especially those that highlight new strategies and approaches, are appreciated. Additionally, repurposing or the discovery of new mechanisms of action for antioxidants compounds are considered.

We welcome original research, review, mini review and perspective articles on themes including, but not limited to:

  • the development of new multi-target antioxidant entities;
  • multi-target rational drug design of antioxidant molecules;
  • drug repurposing proposals of antioxidant compounds;
  • discovery of off-target effects for antioxidant compounds;
  • application of different approaches to polypharmacology;
  • rational design and synthesis of hybrid compounds.

Dr. Roberta Rocca
Guest Editor

Manuscript Submission Information

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Keywords

  • polypharmacology
  • multi-target ligands
  • rational drug design
  • repurposing
  • off-target effects
  • computational techniques

Published Papers (2 papers)

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Research

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12 pages, 38099 KiB  
Article
Anticancer Effects of High Glucosinolate Synthesis Lines of Brassica rapa on Colorectal Cancer Cells
by Jung Sun Kim, Sanghee Han, Hail Kim, So Youn Won, Hyun Woo Park, Hyunjin Choi, Minji Choi, Min Young Lee, In Jin Ha and Seok-Geun Lee
Antioxidants 2022, 11(12), 2463; https://doi.org/10.3390/antiox11122463 - 14 Dec 2022
Cited by 2 | Viewed by 1360
Abstract
Chemoprevention is a method of health control in modern industrialized societies. Traditional breeding (hybridization) has been widely used to produce new (sub)species with beneficial phenotypes. Previously, we produced a number of doubled haploid (DH) lines of Brassica rapa with a high glucosinolate (GSL) [...] Read more.
Chemoprevention is a method of health control in modern industrialized societies. Traditional breeding (hybridization) has been widely used to produce new (sub)species with beneficial phenotypes. Previously, we produced a number of doubled haploid (DH) lines of Brassica rapa with a high glucosinolate (GSL) content. In this study, we evaluated the anticancer activities of extracts from three selected high-GSL (HGSL)-containing DH lines (DHLs) of Brassica rapa in human colorectal cancer (CRC) cells. The three HGSL DHL extracts showed anti-proliferative activities in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium assay and pro-apoptotic activities in the cell cycle or annexin V analysis with the induction of pro-apoptotic protein expression in CRC cells. Mechanistically, HGSL DHL extracts inhibited the NF-κB and ERK pathways, leading to a reduction in the nuclear localization of NF-κB p65. In addition, reactive oxygen species were induced by HGSL DHL extract treatment in CRC cells. In conclusion, our data suggest that the newly developed HGSL DHLs possess enhanced anticancer activities and are potentially helpful as a daily vegetable supplement with chemopreventive activities. Full article
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Review

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18 pages, 1366 KiB  
Review
A Critical Appraisal of the Protective Activity of Polyphenolic Antioxidants against Iatrogenic Effects of Anticancer Chemotherapeutics
by Rosa Purgatorio, Angelina Boccarelli, Leonardo Pisani, Modesto de Candia, Marco Catto and Cosimo D. Altomare
Antioxidants 2024, 13(1), 133; https://doi.org/10.3390/antiox13010133 - 22 Jan 2024
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Abstract
Polyphenolic compounds, encompassing flavonoids (e.g., quercetin, rutin, and cyanidin) and non-flavonoids (e.g., gallic acid, resveratrol, and curcumin), show several health-related beneficial effects, which include antioxidant, anti-inflammatory, hepatoprotective, antiviral, and anticarcinogenic properties, as well as the prevention of coronary heart diseases. Polyphenols have also [...] Read more.
Polyphenolic compounds, encompassing flavonoids (e.g., quercetin, rutin, and cyanidin) and non-flavonoids (e.g., gallic acid, resveratrol, and curcumin), show several health-related beneficial effects, which include antioxidant, anti-inflammatory, hepatoprotective, antiviral, and anticarcinogenic properties, as well as the prevention of coronary heart diseases. Polyphenols have also been investigated for their counteraction against the adverse effects of common anticancer chemotherapeutics. This review evaluates the outcomes of clinical studies (and related preclinical data) over the last ten years, with a focus on the use of polyphenols in chemotherapy as auxiliary agents acting against oxidative stress toxicity induced by antitumor drugs. While further clinical studies are needed to establish adequate doses and optimal delivery systems, the improvement in polyphenols’ metabolic stability and bioavailability, through the implementation of nanotechnologies that are currently being investigated, could improve therapeutic applications of their pharmaceutical or nutraceutical preparations in tumor chemotherapy. Full article
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