Calcium channel blocking activity of calycosin,a major active component of Astragali Radix,on rat aorta  

作　　者：Xiu-li WU Yin-ye WANG Jun CHENG Yu-ying ZHAO 

机构地区：[1]Department of Molecular and Cellular Pharmacology [2]Department of Natural Medicinal Chemistry, School of Pharmaceutical Sciences,Peking University, Beijing 100083, China

出　　处：《Acta Pharmacologica Sinica》2006年第8期1007-1012,共6页中国药理学报（英文版）

基　　金：Project supported by the National Natural Science Foundation of China(№ 30371735).

摘　　要：Aim： To investigate the vasoactivity of calycosin, a major active component of Astragali Radix. Methods： Experiments were performed on isolated rat thoracic aortic rings pre-contracted with phenylephrine （PHE） or KC1. Results：Calycosin produced a concentration-dependent relaxation on the tissue pre-contracted using PHE with 4.46±0.13 of pD2 and 95.85%±2.67% of Emax; or using KC1 with 4.27±0.05 of pD2 and 99.06%±2.15% of Emax, and displaced downwards the concentration-response curves of aortic rings to PHE or KC1. The relaxant effect of calycosin on denuded endothelium aortic rings was the same as on intact endothelium aortic rings, and its vasorelaxant effect was not influenced by L-NAME or indomethacin. In Ca^2＋-free solution, calycosin （30 μmol/L） did not have an effect on PHE （1×10^-6 mol/L）-induced aortic ring contraction. The effects of calycosin and nifedipine where somewhat different; calycosin decreased aortic ring contractions induced by the two agonists, but nifedipine displayed a more potent inhibitory effect on KC1-induced contractions than on PHE-induced contractions, and the vascular relaxing effects of calycosin and nifidipine were additive on PHEinduced contraction but not KC1-induced. Conclusion： Calycosin is a vasorelaxant. Its action is endothelium-independent and is unrelated to intracellular Ca^2＋ release. It is a noncompetitive Ca^2＋ channel blocker. The effect of calycosin on Ca^2＋ channel blockade may be different from that of dihydropyridines. This study demonstrated a novel pharmacological activity of calycosin, and supplied a theoretic foundation for Astragali Radix application.Aim： To investigate the vasoactivity of calycosin, a major active component of Astragali Radix. Methods： Experiments were performed on isolated rat thoracic aortic rings pre-contracted with phenylephrine （PHE） or KC1. Results：Calycosin produced a concentration-dependent relaxation on the tissue pre-contracted using PHE with 4.46±0.13 of pD2 and 95.85%±2.67% of Emax; or using KC1 with 4.27±0.05 of pD2 and 99.06%±2.15% of Emax, and displaced downwards the concentration-response curves of aortic rings to PHE or KC1. The relaxant effect of calycosin on denuded endothelium aortic rings was the same as on intact endothelium aortic rings, and its vasorelaxant effect was not influenced by L-NAME or indomethacin. In Ca^2＋-free solution, calycosin （30 μmol/L） did not have an effect on PHE （1×10^-6 mol/L）-induced aortic ring contraction. The effects of calycosin and nifedipine where somewhat different; calycosin decreased aortic ring contractions induced by the two agonists, but nifedipine displayed a more potent inhibitory effect on KC1-induced contractions than on PHE-induced contractions, and the vascular relaxing effects of calycosin and nifidipine were additive on PHEinduced contraction but not KC1-induced. Conclusion： Calycosin is a vasorelaxant. Its action is endothelium-independent and is unrelated to intracellular Ca^2＋ release. It is a noncompetitive Ca^2＋ channel blocker. The effect of calycosin on Ca^2＋ channel blockade may be different from that of dihydropyridines. This study demonstrated a novel pharmacological activity of calycosin, and supplied a theoretic foundation for Astragali Radix application.

关 键 词：CALYCOSIN rat aorta VASODILATION calcium channel 

分 类 号：R654.3[医药卫生—外科学]