AI Article Synopsis
- A series of structurally-related flavonoids were evaluated as potential antihypertensive agents, focusing on their vasorelaxant effects on aortic rings.
- The compounds demonstrated significant relaxation ability both when the endothelium was intact and when it was removed.
- Molecular modeling suggested that these flavonoids may bind to the same site on calmodulin as trifluoperazine, an established CaM inhibitor, indicating a potential mechanism for their biological activity.
Article 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.
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| http://dx.doi.org/10.1016/j.bmc.2010.10.063 | DOI Listing |
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