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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Effect of Polyphenols From Campomanesia adamantium on Platelet Aggregation and Inhibition of Cyclooxygenases: Molecular Docking and in Vitro Analysis

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Author(s):
Lescano, Caroline H. [1] ; de Lima, Fernando Freitas [2] ; Mendes-Silverio, Camila B. [1] ; Justo, Alberto F. O. [1] ; Baldivia, Debora da Silva [3] ; Vieira, Cristiano P. [1] ; Sanjinez-Argandona, Eliana J. [3] ; Cardoso, Claudia A. L. [4] ; Monica, Fabiola Z. [1] ; de Oliveira, Ivan Pires [5]
Total Authors: 10
Affiliation:
[1] Univ Estadual Campinas, Dept Pharmacol, Campinas, SP - Brazil
[2] Univ Estadual Campinas, Dept Chem Engn, Campinas, SP - Brazil
[3] Fed Univ Grande Dourados, Fac Biol & Environm Sci, Dourados - Brazil
[4] Univ Mato Grosso Sul, Ctr Nat Resource Studies, Dourados - Brazil
[5] Univ Sao Paulo, Inst Biomed Sci, Dept Pharmacol, Sao Paulo - Brazil
Total Affiliations: 5
Document type: Journal article
Source: FRONTIERS IN PHARMACOLOGY; v. 9, JUN 12 2018.
Web of Science Citations: 4
Abstract

Campomanesia adamantium is a medicinal plant of the Brazilian Cerrado. Different parts of its fruits are used in popular medicine to treat gastrointestinal disorders, rheumatism, urinary tract infections and inflammations. Despite its widespread use by the local population, the mechanisms involving platelet aggregation and the inhibition of cyclooxygenase by C. adamantium are unknown. This study evaluated the chemical composition, antioxidant activities and potential benefits of the C. adamantium peel extract (CAPE) and its components in the platelet aggregation induced by arachidonic acid in platelet-rich plasma. Aspects of the pharmacological mechanism were investigated as follows: platelet viability, calcium mobilization, levels of the cyclic nucleotides cAMP and cGMP, thromboxane B-2 levels, and the inhibitory effects on COX-1 and COX-2 were studied in vitro and using molecular docking in the catalytic domain of these proteins. The major CAPE constituents standing out from the chemical analysis are the flavonoids, namely those of the flavones and chalcones class. The results showed that CAPE, quercetin and myricetin significantly decreased arachidonic acid-induced platelet aggregation; the assays showed that CAPE and quercetin decreased the mobilization of calcium and thromboxane B-2 levels in platelets and increased cAMP and cGMP levels. Moreover, CAPE inhibited the activity of COX-1 and COX-2, highlighting that quercetin could potentially prevent the access of arachidonic acid more to the catalytic site of COX-1 than COX-2. These results highlight CAPE's potential as a promising therapeutic candidate for the prevention and treatment of diseases associated with platelet aggregation. (AU)

FAPESP's process: 17/02201-4 - Study of the inhibition of the accumulation of cyclic nucleotide by pyridopyrimidine derivatives using molecular dynamics simulations
Grantee:Ivan Pires de Oliveira
Support Opportunities: Scholarships in Brazil - Post-Doctoral