Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 1, Pages 542-546Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.063
Keywords
Flavonoids; Vasorelaxant effect; Calmodulin inhibition; Docking
Funding
- CONACyT [89521, 170049]
- Fondo de Consolidacion-UAEM (Apoyo a Cuerpos Academicos)
- Faculty of Pharmacy
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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