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Type: Artigo de periódico
Title: Quercetin As An Inhibitor Of Snake Venom Secretory Phospholipase A2.
Author: Cotrim, Camila Aparecida
de Oliveira, Simone Cristina Buzzo
Diz Filho, Eduardo B S
Fonseca, Fabiana Vieira
Baldissera, Lineu
Antunes, Edson
Ximenes, Rafael Matos
Monteiro, Helena Serra Azul
Rabello, Marcelo Montenegro
Hernandes, Marcelo Zaldini
de Oliveira Toyama, Daniela
Toyama, Marcos Hikari
Abstract: As polyphenolic compounds isolated from plants extracts, flavonoids have been applied to various pharmaceutical uses in recent decades due to their anti-inflammatory, cancer preventive, and cardiovascular protective activities. In this study, we evaluated the effects of the flavonoid quercetin on Crotalus durissus terrificus secretory phospholipase A2 (sPLA2), an important protein involved in the release of arachidonic acid from phospholipid membranes. The protein was chemically modified by treatment with quercetin, which resulted in modifications in the secondary structure as evidenced through circular dichroism. In addition, quercetin was able to inhibit the enzymatic activity and some pharmacological activities of sPLA2, including its antibacterial activity, its ability to induce platelet aggregation, and its myotoxicity by approximately 40%, but was not able to reduce the inflammatory and neurotoxic activities of sPLA2. These results suggest the existence of two pharmacological sites in the protein, one that is correlated with the enzymatic site and another that is distinct from it. We also performed molecular docking to better understand the possible interactions between quercetin and sPLA2. Our docking data showed the existence of hydrogen-bonded, polar interactions and hydrophobic interactions, suggesting that other flavonoids with similar structures could bind to sPLA2. Further research is warranted to investigate the potential use of flavonoids as sPLA2 inhibitors.
Subject: Animals
Biological Assay
Circular Dichroism
Crotalid Venoms
Models, Molecular
Phospholipases A2, Secretory
Platelet Aggregation
Spectrometry, Mass, Matrix-assisted Laser Desorption-ionization
Citation: Chemico-biological Interactions. v. 189, n. 1-2, p. 9-16, 2011-Jan.
Rights: fechado
Identifier DOI: 10.1016/j.cbi.2010.10.016
Date Issue: 2011
Appears in Collections:Unicamp - Artigos e Outros Documentos

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