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Molecules
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Natural Products in the Antioxidant Drug Discovery Process
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Natural Products in the Antioxidant Drug Discovery Process

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

Deadline for manuscript submissions: 31 July 2024 | Viewed by 3128

Special Issue Editors

Prof. Dr. Milena Petkova Popova

E-Mail Website
Guest Editor
Institute of Organic Chemistry with Centre of Phytochemistry (IOCCP), Bulgarian Academy of Sciences, Sofia, Bulgaria
Interests: natural products; biologically active compounds; chemical profiling; structural elucidation; phenols; terpenes; antioxidants
Dr. Kalina Alipieva

E-Mail Website
Guest Editor
Institute of Organic Chemistry with Centre of Phytochemistry (IOCCP), Bulgarian Academy of Sciences, Sofia, Bulgaria
Interests: pharmaceutically valuable metabolites; phenols; phenylethanoids; isolation and structural elucidation; metabolomics

Special Issue Information

Dear Colleagues,

Humans have relied in natural products (NPs) for the prevention and treatment of various ailments for centuries. These NPs are biosynthesized by various natural sources, such as plants, mushrooms, and marine organisms, which offer a unique variety of molecules in terms of chemical diversity and beneficial health properties. Over the years, the NPs have become good candidates for drug discovery and drug leads, in particular against clinical conditions and diseases associated with oxidative stress and radicals and other reactive oxygen species. A number of molecules serving as antioxidants have been discovered, among which polyphenols deserve special attention. In the long and multidisciplinary process of drug discovery, one of the most important and challengeable points is discovering and identifying active molecules—antioxidants which add structures in the chemical libraries used in drug discovery high-throughput screening.

The current Special Issue on “Natural Products in the Antioxidant Drug Discovery Process” aims to collect original research articles as well as review articles related to the potential and utilization of natural sources and their ingredients as antioxidant drug candidates. Recent advances in isolation, characterization, and screening of the antioxidant action of crude extracts and components as well as in small synthetic modifications of natural antioxidants are also appreciated. 

Prof. Dr. Milena Petkova Popova
Dr. Kalina Alipieva
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. 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 2700 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 
  • chemical profiling 
  • isolation and structure elucidation 
  • antioxidants 
  • inflammation 
  • synthetic modifications

Published Papers (2 papers)

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Research

14 pages, 2886 KiB  
Article
Effects of Quince Gel and Hesperidin Mixture on Experimental Endometriosis
by Işılay Sezen Ermiş, Engin Deveci and Fırat Aşır
Molecules 2023, 28(16), 5945; https://doi.org/10.3390/molecules28165945 - 08 Aug 2023
Cited by 3 | Viewed by 1178
Abstract
Objectives: Endometriosis (EM) is the presence of endometrial tissue outside the uterus. This study aimed to examine the effects of quince gel and hesperidin treatment on uterine tissue in an experimental endometriosis model. Materials and Methods: Thirty-two rats were categorized into four groups [...] Read more.
Objectives: Endometriosis (EM) is the presence of endometrial tissue outside the uterus. This study aimed to examine the effects of quince gel and hesperidin treatment on uterine tissue in an experimental endometriosis model. Materials and Methods: Thirty-two rats were categorized into four groups as sham, EM, EM+quince gel (QG), and EM+QG+Hesperidin (HES). The endometriosis (EM) model was induced with surgical intervention. Estradiol benzoate (EB) was used to induce endometrial hyperplasia. In the EM group, EB was given to rats for 7 days. The EM+QG group received 2 cc QG for 21 days. HES treatment was given for 21 days after EM induction. At the end of the experiment, blood was taken from the animals and the serum total antioxidant status (TAS) and total oxidant status (TOS) values were studied. Uterine tissues were dissected and processed for histological paraffin embedding. Tissues were fixed in 4% glutaraldehyde solution and processed for ultrastructural analysis. Results: After EM, QG and HES treatment significantly increased the TAS and decreased the TOS value. EM caused epithelial and glandular degeneration, thinning of the basal membranes, and vascular dilatation with increased fibrosis and edema. QG+HES restored the pathology and showed protective effects in uterine tissues. Caspase-3 expression was increased in the epithelium, glands, and muscle layers of the EM group. In EM+QG+HES, hesperidin protected cell survival and decreased Caspase-3 expression in uterine tissues. TNF-α expression was intense in inflammatory cells and the muscle layer in the EM group. HES reduced inflammation by decreasing the TNF-α expression. MAPK expression was increased after EM induction in epithelial, glandular, and inflammatory cells in the EM group. After HES treatment, MAPK expression was mainly negative in cells of uterine tissue in the EM+QG+HES group. Ultrastructurally, in the EM group, organelles were disrupted and dilated and degenerated after EM induction. QG and HES treatment improved cellular organelles. Conclusion: Local vaginal applications can be an alternative treatment method in the endometriosis model via QG+HES treatment promoting cell proliferation and angiogenesis and preventing cell death. Full article
(This article belongs to the Special Issue Natural Products in the Antioxidant Drug Discovery Process)
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15 pages, 4424 KiB  
Article
The Transport and Uptake of Resveratrol Mediated via Glucose Transporter 1 and Its Antioxidant Effect in Caco-2 Cells
by Zhen-Dong Zhang, Qi Tao, Li-Xia Bai, Zhe Qin, Xi-Wang Liu, Shi-Hong Li, Ya-Jun Yang, Wen-Bo Ge and Jian-Yong Li
Molecules 2023, 28(12), 4569; https://doi.org/10.3390/molecules28124569 - 06 Jun 2023
Cited by 1 | Viewed by 1545
Abstract
Resveratrol has anti-inflammatory, anti-cancer, and anti-aging pharmacological activities. There is currently a gap in academic research regarding the uptake, transport, and reduction of H2O2-induced oxidative damage of resveratrol in the Caco-2 cell model. This study investigated the role of [...] Read more.
Resveratrol has anti-inflammatory, anti-cancer, and anti-aging pharmacological activities. There is currently a gap in academic research regarding the uptake, transport, and reduction of H2O2-induced oxidative damage of resveratrol in the Caco-2 cell model. This study investigated the role of resveratrol in the uptake, transport, and alleviation of H2O2-induced oxidative damage in Caco-2 cells. In the Caco-2 cell transport model, it was observed that the uptake and transport of resveratrol (10, 20, 40, and 80 μM) were time dependent and concentration dependent. Different temperatures (37 °C vs. 4 °C) could significantly affect the uptake and transportation of resveratrol. The apical to basolateral transport of resveratrol was markedly reduced by STF-31, a GLUT1 inhibitor, and siRNA intervention. Furthermore, resveratrol pretreatment (80 μM) improves the viability of Caco-2 cells induced by H2O2. In a cellular metabolite analysis combined with ultra-high performance liquid chromatography-tandem mass spectrometry, 21 metabolites were identified as differentials. These differential metabolites belong to the urea cycle, arginine and proline metabolism, glycine and serine metabolism, ammonia recycling, aspartate metabolism, glutathione metabolism, and other metabolic pathways. The transport, uptake, and metabolism of resveratrol suggest that oral resveratrol could prevent intestinal diseases caused by oxidative stress. Full article
(This article belongs to the Special Issue Natural Products in the Antioxidant Drug Discovery Process)
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