Cargando…

Flavonoids: Antiplatelet Effect as Inhibitors of COX-1

Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere wit...

Descripción completa

Detalles Bibliográficos
Autores principales: Zaragozá, Cristina, Álvarez-Mon, Miguel Ángel, Zaragozá, Francisco, Villaescusa, Lucinda
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8839657/
https://www.ncbi.nlm.nih.gov/pubmed/35164411
http://dx.doi.org/10.3390/molecules27031146
_version_ 1784650424061526016
author Zaragozá, Cristina
Álvarez-Mon, Miguel Ángel
Zaragozá, Francisco
Villaescusa, Lucinda
author_facet Zaragozá, Cristina
Álvarez-Mon, Miguel Ángel
Zaragozá, Francisco
Villaescusa, Lucinda
author_sort Zaragozá, Cristina
collection PubMed
description Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere with the arachidonic acid (AA) cascade. These assays are designed to measure the antiplatelet aggregation capacity of quercetin, rutin, diosmetin, diosmin, and hidrosmin, as well as to evaluate a potential structure−activity ratio. In this paper, several studies on platelet aggregation at different concentrations (from 0.33 mM to 1.5 mM) of different flavone compounds are conducted, measuring platelet aggregation by impedance aggregometry, and the cyclooxygenase (COX) activity by metabolites generated, including the activity of the pure recombinant enzyme in the presence of these polyphenols. The results obtained showed that quercetin and diosmetin aglycones have a greater antiplatelet effect and inhibit the COX enzyme activity to a greater extent than their heterosides; however, the fact that greater inhibition of the pure recombinant enzyme was achieved by heterosides suggests that these compounds may have difficulty in crossing biological membranes. In any case, in view of the results obtained, it can be concluded that flavonoids could be useful as coadjuvants in the treatment of cardiovascular pathologies.
format Online
Article
Text
id pubmed-8839657
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-88396572022-02-13 Flavonoids: Antiplatelet Effect as Inhibitors of COX-1 Zaragozá, Cristina Álvarez-Mon, Miguel Ángel Zaragozá, Francisco Villaescusa, Lucinda Molecules Article Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere with the arachidonic acid (AA) cascade. These assays are designed to measure the antiplatelet aggregation capacity of quercetin, rutin, diosmetin, diosmin, and hidrosmin, as well as to evaluate a potential structure−activity ratio. In this paper, several studies on platelet aggregation at different concentrations (from 0.33 mM to 1.5 mM) of different flavone compounds are conducted, measuring platelet aggregation by impedance aggregometry, and the cyclooxygenase (COX) activity by metabolites generated, including the activity of the pure recombinant enzyme in the presence of these polyphenols. The results obtained showed that quercetin and diosmetin aglycones have a greater antiplatelet effect and inhibit the COX enzyme activity to a greater extent than their heterosides; however, the fact that greater inhibition of the pure recombinant enzyme was achieved by heterosides suggests that these compounds may have difficulty in crossing biological membranes. In any case, in view of the results obtained, it can be concluded that flavonoids could be useful as coadjuvants in the treatment of cardiovascular pathologies. MDPI 2022-02-08 /pmc/articles/PMC8839657/ /pubmed/35164411 http://dx.doi.org/10.3390/molecules27031146 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Zaragozá, Cristina
Álvarez-Mon, Miguel Ángel
Zaragozá, Francisco
Villaescusa, Lucinda
Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title_full Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title_fullStr Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title_full_unstemmed Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title_short Flavonoids: Antiplatelet Effect as Inhibitors of COX-1
title_sort flavonoids: antiplatelet effect as inhibitors of cox-1
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8839657/
https://www.ncbi.nlm.nih.gov/pubmed/35164411
http://dx.doi.org/10.3390/molecules27031146
work_keys_str_mv AT zaragozacristina flavonoidsantiplateleteffectasinhibitorsofcox1
AT alvarezmonmiguelangel flavonoidsantiplateleteffectasinhibitorsofcox1
AT zaragozafrancisco flavonoidsantiplateleteffectasinhibitorsofcox1
AT villaescusalucinda flavonoidsantiplateleteffectasinhibitorsofcox1