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Characterization of Novel Synthetic Polyphenols: Validation of Antioxidant and Vasculoprotective Activities

Authors
  • Pérez de Vega, María Jesús
  • Moreno-Fernández, Silvia1
  • Pontes-Quero, Gloria María2, 3
  • González-Amor, María4, 5
  • Vázquez-Lasa, Blanca2, 6
  • Sabater-Muñoz, Beatriz
  • Briones, Ana M.4, 5
  • Aguilar, María R.2, 6
  • Miguel, Marta1
  • González-Muñiz, Rosario
  • 1 (M.M.)
  • 2 (M.R.A.)
  • 3 Alodia Farmacéutica SL, Santiago Grisolía 2 D130/L145, 28760 Madrid, Spain
  • 4 (A.M.B.)
  • 5 Centro de Investigación Biomédica en Red de Enfermedades Cardiovasculares (CIBERCV), 28029 Madrid Spain
  • 6 Networking Biomedical Research Centre in Bioengineering, Biomaterials and Nanomedicine, CIBER-BBN, 28029 Madrid, Spain
Type
Published Article
Journal
Antioxidants
Publisher
MDPI AG
Publication Date
Aug 25, 2020
Volume
9
Issue
9
Identifiers
DOI: 10.3390/antiox9090787
PMID: 32854368
PMCID: PMC7555119
Source
PubMed Central
Keywords
License
Green

Abstract

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 .

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