Abstract

Owing to its cardiovascular therapeutical effects, icariin, a flavonoid isolated from Epimedii herba, is considered to be the major active constituent of Epimedii herba. The aim of this study is to investigate the effect of icariin on precontracted coronary artery isolated from canine. Coronary artery segments were isolated from normal anesthetized Beagle dogs and cut into 5-mm rings. The rings were mounted in an organ chamber and contracted by either 40 mM KCl or 10 microM PGF2alpha, and vasorelaxant tone to icariin was measured. Treatment of icariin could significantly produce a relaxation of precontracted coronary arterial rings with intact endothelium in a concentration-dependent manner. Comparatively, the vasorelaxation disappeared in denuded-endothelium rings. Furthermore, the vasorelaxant effect of icariin was blocked by Nomega-Nitro- L-arginine Methyl Ester (L-NAME), 1H-[1, 2, 4]-oxadiazolo [4, 3-a] quinoxalin-1-one (ODQ) but not by indomethacin and glibenclamide, respectively. Tetraethylammonium (TEA) could partly antagonize the vasorelaxant effect triggered by icariin. There was no significant gene expression difference of the endothelial nitric oxide synthase (eNOS) gene in coronary arterial rings among the different concentrations of icariin by RT-PCR, but the activity of eNOS was increased in a concentration-dependent manner after icariin exposure. These results suggest that icariin produces NO-dependent relaxation in the isolated canine coronary artery, and the possible mechanism is involved in the activation of eNOS protein and NO-cGMP pathway.