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ID: ALA1641572

Journal: Bioorg Med Chem

Title: Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches.

Authors: Torres-Piedra M, Figueroa M, Hernández-Abreu O, Ibarra-Barajas M, Navarrete-Vázquez G, Estrada-Soto S, Estrada-Soto S.

Abstract: In our search for potential antihypertensive agents, a series of structurally-related flavonoids was screened. Ex vivo and in vitro biological evaluations indicated that compounds 1-7 displayed an important vasorelaxant effect on the endothelium-intact (E(+)) and -denuded (E(-)) aortic rings test. Their in vitro anti-calmodulin (CaM) properties were determined by means of the inhibitory effect on the activation of the calmodulin-sensitive cAMP phosphodiesterase (PDE1) assay. Molecular modeling experiments were also performed in order to explore the probable binding site of 1-7 with CaM, and the results indicated that they could bind to the protein in the same pocket as trifluoperazine (TFP), a well-known CaM inhibitor.

CiteXplore: 21129983

DOI: 10.1016/j.bmc.2010.10.063