The vasorelaxant effect of evocarpine (cas 15266-38-3) in isolated aortic strips: mode of action

Add time:08/03/2019    Source:sciencedirect.com

The effect of evocarpine (cas 15266-38-3) (EVO), a quinolone alkaloid isolated from Evodiae fructus, on Ca2+-blocking activity has been examined. In the isolated rat thoracic aorta evocarpine significantly inhibited the contraction induced by 60 mM K+ with an IC50 of 9.8 μM, and that induced by external Ca2+ in the depolarized muscle in concentrations of 10–100 μM. The relaxant effect of evocarpine and verapamil was antagonized by Bay K8644. The increase of 45Ca2+-influx induced by 60 mM K+ was significantly inhibited by 100 μM evocarpine. In the isolated rabbit thoracic aorta 100 μM evocarpine had no efffect on norepinephrine-induced contraction in normal medium or on the phasic contraction in Ca2+-free medium or the transient relaxation induced by activation of the Na+ pump. The content of cyclic AMP or cyclic GMP was unchanged. These results suggests that evocarpine inhibits Ca2+ influx through voltage-dependent calcium channels.

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