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Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities
Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effect...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7555119/ https://www.ncbi.nlm.nih.gov/pubmed/32854368 http://dx.doi.org/10.3390/antiox9090787 |
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author | Pérez de Vega, María Jesús Moreno-Fernández, Silvia Pontes-Quero, Gloria María González-Amor, María Vázquez-Lasa, Blanca Sabater-Muñoz, Beatriz Briones, Ana M. Aguilar, María R. Miguel, Marta González-Muñiz, Rosario |
author_facet | Pérez de Vega, María Jesús Moreno-Fernández, Silvia Pontes-Quero, Gloria María González-Amor, María Vázquez-Lasa, Blanca Sabater-Muñoz, Beatriz Briones, Ana M. Aguilar, María R. Miguel, Marta González-Muñiz, Rosario |
author_sort | Pérez de Vega, María Jesús |
collection | PubMed |
description | Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effects against free radicals produced by either normal or pathological metabolism in such systems. For instance, resveratrol, a well-known potent antioxidant, has a counteracting effect on the excess of reactive oxygen species (ROS) and has a number of therapeutic benefits, like anti-inflammatory, anti-cancer and cardioprotective activities. Based on previous work from our group, and on the most frequent OH substitutions of natural polyphenols, we designed two series of synthetically accessible bis-polyhydroxyphenyl derivatives, separated by amide or urea linkers. These compounds exhibit high antioxidant ability (oxygen radical absorbance capacity (ORAC) assay) and interesting radical scavenging activity (RSA) values (2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and α,α-diphenyl-β-picrylhydrazyl (DPPH) tests). Some of the best polyphenols were evaluated in two biological systems, endothelial cells (in vitro) and whole aorta (ex vivo), highly susceptible for the deleterious effects of prooxidants under different inflammatory conditions, showing protection against oxidative stress induced by inflammatory stimuli relevant in cardiovascular diseases, i.e., Angiotensin II and IL-1β. Selected compounds also showed strong in vivo antioxidant properties when evaluated in the model organism Saccharomyces cerevisiae. |
format | Online Article Text |
id | pubmed-7555119 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-75551192020-10-14 Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities Pérez de Vega, María Jesús Moreno-Fernández, Silvia Pontes-Quero, Gloria María González-Amor, María Vázquez-Lasa, Blanca Sabater-Muñoz, Beatriz Briones, Ana M. Aguilar, María R. Miguel, Marta González-Muñiz, Rosario Antioxidants (Basel) Article Antioxidant compounds, including polyphenols, have therapeutic effects because of their anti-inflammatory, antihypertensive, antithrombotic and antiproliferative properties. They play important roles in protecting the cardiovascular and neurological systems, by having preventive or protective effects against free radicals produced by either normal or pathological metabolism in such systems. For instance, resveratrol, a well-known potent antioxidant, has a counteracting effect on the excess of reactive oxygen species (ROS) and has a number of therapeutic benefits, like anti-inflammatory, anti-cancer and cardioprotective activities. Based on previous work from our group, and on the most frequent OH substitutions of natural polyphenols, we designed two series of synthetically accessible bis-polyhydroxyphenyl derivatives, separated by amide or urea linkers. These compounds exhibit high antioxidant ability (oxygen radical absorbance capacity (ORAC) assay) and interesting radical scavenging activity (RSA) values (2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and α,α-diphenyl-β-picrylhydrazyl (DPPH) tests). Some of the best polyphenols were evaluated in two biological systems, endothelial cells (in vitro) and whole aorta (ex vivo), highly susceptible for the deleterious effects of prooxidants under different inflammatory conditions, showing protection against oxidative stress induced by inflammatory stimuli relevant in cardiovascular diseases, i.e., Angiotensin II and IL-1β. Selected compounds also showed strong in vivo antioxidant properties when evaluated in the model organism Saccharomyces cerevisiae. MDPI 2020-08-25 /pmc/articles/PMC7555119/ /pubmed/32854368 http://dx.doi.org/10.3390/antiox9090787 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Pérez de Vega, María Jesús Moreno-Fernández, Silvia Pontes-Quero, Gloria María González-Amor, María Vázquez-Lasa, Blanca Sabater-Muñoz, Beatriz Briones, Ana M. Aguilar, María R. Miguel, Marta González-Muñiz, Rosario Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title | Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title_full | Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title_fullStr | Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title_full_unstemmed | Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title_short | Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities |
title_sort | characterization of novel synthetic polyphenols: validation of antioxidant and vasculoprotective activities |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7555119/ https://www.ncbi.nlm.nih.gov/pubmed/32854368 http://dx.doi.org/10.3390/antiox9090787 |
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