Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
8.8
7.0
Journals
Antioxidants
Special Issues
From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug...
share announcement

From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition

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

Deadline for manuscript submissions: 15 June 2024 | Viewed by 5009

Special Issue Editors

Dr. Gabriele Carullo

E-Mail Website
Guest Editor
Department of Life Sciences, University of Siena, 53100 Siena, Italy
Interests: HDAC; vasorelaxant agents; antioxidant and anti-inflammatory nutraceuticals; leukemia; Pseudomonas aeruginosa; hybrid compounds; retinitis pigmentosa
Special Issues, Collections and Topics in MDPI journals
Dr. Roberta Ibba

E-Mail Website
Guest Editor
Department of Medicine, Surgery and Pharmacy, University of Sassari, Via Muroni 23A, 07100 Sassari, Italy
Interests: medicinal chemistry; drug design; anticancer drugs; antiviral; VEGFR-2; natural compounds; antioxidants; fragment-based drug design
Special Issues, Collections and Topics in MDPI journals
Dr. Valeria Tudino

E-Mail Website
Guest Editor
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy
Interests: medicinal chemistry; HIV; anticancer compounds; antimicrobial agents; nitrogen-based compounds; Pseudomonas aeruginosa
Special Issues, Collections and Topics in MDPI journals
Dr. Maria Dichiara

E-Mail Website
Guest Editor
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy
Interests: medicinal chemistry; drug design; anticancer drugs; infectious diseases; de novo synthetic compounds; neurological disorders
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In view of the great response we received with the previous Special Issue, "From Nature to Synthetic Small Molecule Antioxidants: New Candidates in Drug Discovery", we decided to continue addressing this topic through a Second Edition.

Natural compounds are well known for their invaluable contribution to pharmacological research in several therapeutic areas. Over the years, natural product collections have offered a wide variety of pharmacophores. These have been exploited in drug discovery to provide new lead compounds that are able to tackle even the most difficult screened targets.

This Special Issue, entitled “From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition”, aims to welcome both original articles and extensive reviews related to natural products, their derivatives, and de novo designed compounds in drug discovery efforts. Oxidative-stress-related conditions, reactive oxygen species, oxidative damage, and inflammatory stimuli are topics of great interest for modern medicinal chemistry, and therefore, they will be welcome in this Special Issue. For publication, we will consider the following topics: the bioactivity of medicinal plant extracts, the development of natural-derived compounds, biological applications and synthetic strategies for natural metabolites and/or analogues, and the rational or computer-aided design and development of synthetic small-molecule derivatives with pharmacological interest. Furthermore, applications looking at different disorders, from cancers to infectious diseases, as well as cardiovascular, neurological, and other human conditions, will also be considered.

Dr. Gabriele Carullo
Dr. Roberta Ibba
Dr. Valeria Tudino
Dr. Maria Dichiara
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

  • natural products
  • nutraceuticals
  • antioxidants
  • de novo synthetic compounds
  • GPCRs
  • ion channels
  • anticancer compounds
  • cardiovascular diseases
  • neurological disorders
  • infectious diseases

Published Papers (4 papers)

Download All Papers
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

Jump to: Review

23 pages, 4913 KiB  
Article
7-O-tyrosyl Silybin Derivatives as a Novel Set of Anti-Prostate Cancer Compounds
by Valeria Romanucci, Rita Pagano, Kushal Kandhari, Armando Zarrelli, Maria Petrone, Chapla Agarwal, Rajesh Agarwal and Giovanni Di Fabio
Antioxidants 2024, 13(4), 418; https://doi.org/10.3390/antiox13040418 - 29 Mar 2024
Viewed by 534
Abstract
Silybin is a natural compound extensively studied for its hepatoprotective, neuroprotective and anticancer properties. Envisioning the enhancement of silybin potential by suitable modifications in its chemical structure, here, a series of new 7-O-alkyl silybins derivatives were synthesized by the Mitsunobu reaction [...] Read more.
Silybin is a natural compound extensively studied for its hepatoprotective, neuroprotective and anticancer properties. Envisioning the enhancement of silybin potential by suitable modifications in its chemical structure, here, a series of new 7-O-alkyl silybins derivatives were synthesized by the Mitsunobu reaction starting from the silybins and tyrosol-based phenols, such as tyrosol (TYR, 3), 3-methoxytyrosol (MTYR, 4), and 3-hydroxytyrosol (HTYR, 5). This research sought to explore the antioxidant and anticancer properties of eighteen new derivatives and their mechanisms. In particular, the antioxidant properties of new derivatives outlined by the DPPH assay showed a very pronounced activity depending on the tyrosyl moiety (HTYR > MTYR >> TYR). A significant contribution of the HTYR moiety was observed for silybins and 2,3-dehydro-silybin-based derivatives. According to the very potent antioxidant activity, 2,3-dehydro-silybin derivatives 15ab, 15a, and 15b exerted the most potent anticancer activity in human prostate cancer PC-3 cells. Furthermore, flow cytometric analysis for cell cycle and apoptosis revealed that 15ab, 15a, and 15b induce strong G1 phase arrest and increase late apoptotic population in PC-3 cells. Additionally, Western blotting for apoptotic marker cleaved caspase-3 confirmed apoptosis induction by these silybin derivatives in PC-3 cells. These findings hold significant importance in the investigation of anticancer properties of silybin derivatives and strongly encourage swift investigation in pre-clinical models and clinical trials. Full article
(This article belongs to the Special Issue From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition)
►▼ Show Figures

Graphical abstract

28 pages, 5016 KiB  
Article
Exploring Metabolic and Gut Microbiome Responses to Paraquat Administration in Male Wistar Rats: Implications for Oxidative Stress
by Julia Hernandez-Baixauli, Gertruda Chomiciute, Harry Tracey, Ignasi Mora, Antonio J. Cortés-Espinar, Javier Ávila-Román, Nerea Abasolo, Hector Palacios-Jordan, Elisabet Foguet-Romero, David Suñol, Mar Galofré, Juan María Alcaide-Hidalgo, Laura Baselga-Escudero, Josep M. del Bas and Miquel Mulero
Antioxidants 2024, 13(1), 67; https://doi.org/10.3390/antiox13010067 - 01 Jan 2024
Viewed by 1758
Abstract
In this study, we examined the metabolic and gut microbiome responses to paraquat (PQ) in male Wistar rats, focusing on oxidative stress effects. Rats received a single intraperitoneal injection of PQ at 15 and 30 mg/kg, and various oxidative stress parameters (i.e., MDA, [...] Read more.
In this study, we examined the metabolic and gut microbiome responses to paraquat (PQ) in male Wistar rats, focusing on oxidative stress effects. Rats received a single intraperitoneal injection of PQ at 15 and 30 mg/kg, and various oxidative stress parameters (i.e., MDA, SOD, ROS, 8-isoprostanes) were assessed after three days. To explore the omic profile, GC-qTOF and UHPLC-qTOF were performed to assess the plasma metabolome; 1H-NMR was used to assess the urine metabolome; and shotgun metagenomics sequencing was performed to study the gut microbiome. Our results revealed reductions in body weight and tissue changes, particularly in the liver, were observed, suggesting a systemic effect of PQ. Elevated lipid peroxidation and reactive oxygen species levels in the liver and plasma indicated the induction of oxidative stress. Metabolic profiling revealed changes in the tricarboxylic acid cycle, accumulation of ketone body, and altered levels of key metabolites, such as 3-hydroxybutyric acid and serine, suggesting intricate links between energy metabolism and redox reactions. Plasma metabolomic analysis revealed alterations in mitochondrial metabolism, nicotinamide metabolism, and tryptophan degradation. The gut microbiome showed shifts, with higher PQ doses influencing microbial populations (e.g., Escherichia coli and Akkermansia muciniphila) and metagenomic functions (pyruvate metabolism, fermentation, nucleotide and amino acid biosynthesis). Overall, this study provides comprehensive insights into the complex interplay between PQ exposure, metabolic responses, and gut microbiome dynamics. These findings enhance our understanding of the mechanisms behind oxidative stress-induced metabolic alterations and underscore the connections between xenobiotic exposure, gut microbiota, and host metabolism. Full article
(This article belongs to the Special Issue From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition)
►▼ Show Figures

Graphical abstract

22 pages, 7026 KiB  
Article
Anti-Browning Effect of 2-Mercaptobenzo[d]imidazole Analogs with Antioxidant Activity on Freshly-Cut Apple Slices and Their Highly Potent Tyrosinase Inhibitory Activity
by Jieun Lee, Hye Soo Park, Hee Jin Jung, Yu Jung Park, Min Kyung Kang, Hye Jin Kim, Dahye Yoon, Sultan Ullah, Dongwan Kang, Yujin Park, Pusoon Chun, Hae Young Chung and Hyung Ryong Moon
Antioxidants 2023, 12(10), 1814; https://doi.org/10.3390/antiox12101814 - 29 Sep 2023
Cited by 2 | Viewed by 899
Abstract
Ten 2-mercaptobenzimidazole (2-MBI) analogs were synthesized as potential tyrosinase inhibitors because mercapto-containing compounds can bind to copper ions at the active site of tyrosinase to inhibit enzyme activity. Nine 2-MBI analogs showed sub-micromolar IC50 values for mushroom tyrosinase monophenolase activity; analog 4 [...] Read more.
Ten 2-mercaptobenzimidazole (2-MBI) analogs were synthesized as potential tyrosinase inhibitors because mercapto-containing compounds can bind to copper ions at the active site of tyrosinase to inhibit enzyme activity. Nine 2-MBI analogs showed sub-micromolar IC50 values for mushroom tyrosinase monophenolase activity; analog 4 was 280-fold more potent than kojic acid, and in diphenolase activity, 6 was 970-fold more potent than kojic acid. The inhibition mode of the 2-MBI analogs was investigated using kinetic studies supported by docking simulations. Benzimidazoles without the 2-mercapto substituent of the 2-MBI analogs lost their tyrosinase inhibitory activity, implying that the 2-mercapto substituent plays an important role in tyrosinase inhibition. The 2-MBI analogs exerted potent antioxidant effects against 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and reactive oxygen species (ROS). The results obtained from apple slices and human embryonic kidney cells (HEK-293) suggest that most 2-MBI analogs are sufficiently safe candidates to delay the browning of apple slices effectively. Thus, these results support the potential use of 2-MBI analogs as anti-browning agents in foods such as mushrooms, vegetables, and fruits. Full article
(This article belongs to the Special Issue From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition)
►▼ Show Figures

Graphical abstract

Review

Jump to: Research

21 pages, 1510 KiB  
Review
An Update on Recent Studies Focusing on the Antioxidant Properties of Salvia Species
by Domenico Iacopetta, Jessica Ceramella, Domenica Scumaci, Alessia Catalano, Maria Stefania Sinicropi, Rosa Tundis, Stefano Alcaro and Fernanda Borges
Antioxidants 2023, 12(12), 2106; https://doi.org/10.3390/antiox12122106 - 13 Dec 2023
Viewed by 1414
Abstract
Nutrition has crucial effects and a significant role in disease prevention. Recently, nutraceuticals have attracted much attention in scientific research due to their pleiotropic effects and relatively non-toxic behavior. Among the biological effects displayed by plants belonging to the Lamiaceae family, such as [...] Read more.
Nutrition has crucial effects and a significant role in disease prevention. Recently, nutraceuticals have attracted much attention in scientific research due to their pleiotropic effects and relatively non-toxic behavior. Among the biological effects displayed by plants belonging to the Lamiaceae family, such as antibacterial, anticancer, anti-inflammatory, and anticholinesterase, sage is well known for its antioxidant properties and is a rich source of numerous compounds that are biologically active, amongst them polyphenols, with more than 160 types identified. In this review we summarized some of the significant studies published in the last decade reporting the most employed extraction methods and the different assays that are useful for establishing the antioxidant properties of some sage species. Even though the scientific literature contains plenty of data regarding the antioxidant properties of many sage species, further studies are needed in order to gain a deeper understanding of the mechanism of action and the compounds responsible for their antioxidant activity. Finally, it should be taken into account that the data on the antioxidant properties of sage extracts are often difficult to compare with each other, since a series of variables in the extraction procedures, the type of assay used, and standardization may affect the final result. Full article
(This article belongs to the Special Issue From Natural to Synthetic Small-Molecule Antioxidants: New Candidates in Drug Discovery—Second Edition)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-4
Back to TopTop