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

UNCG Author/Contributor (non-UNCG co-authors, if there are any, appear on document)
Mario Figueroa Saldivar, Adjunct Faculty (Creator)
The University of North Carolina at Greensboro (UNCG )
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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.

Additional Information

Bioorganic and Medicinal Chemistry, 19 (1), pp. 542-546
Language: English
Date: 2011
Flavonoids, Vasorelaxant effect, Calmodulin inhibition, Docking

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