Xin Z C, Kim E K, Lin C S, Liu W J, Tian L, Yuan Y M, Fu J
Department of Urology, the 1st Hospital, Peking University, 8 Xishiku Street, Xicheng District, Beijing 100034, China.
Asian J Androl. 2003 Mar;5(1):15-8.
To clarify the mechanism of the therapeutic action of icariin on erectile dysfunction (ED).
PDE5 was isolated from the human platelet and PDE4 from the rat liver tissue using the FPLC system (Pharmacia, Milton Keynes, UK) and the Mono Q column. The inhibitory effects of icariin on PDE5 and PDE4 activities were investigated by the two-step radioisotope procedure with [(3)H]-cGMP/[(3)H]-cAMP. Papaverine served as the control drug.
Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. The IC(50) of Icariin and papaverine on PDE5 were 0.432 micromol/L and 0.680 micromol/L, respectively and those on PDE4, 73.50 micromol/L and 3.07 micromol/L, respectively. The potencies of selectivity of icariin and papaverine on PDE5 (PDE4/PDE5 of IC(50)) were 167.67 times and 4.54 times, respectively.
Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED.
阐明淫羊藿苷治疗勃起功能障碍(ED)的作用机制。
使用FPLC系统(英国米尔顿凯恩斯市的Pharmacia公司)和Mono Q柱从人血小板中分离磷酸二酯酶5(PDE5),从大鼠肝组织中分离磷酸二酯酶4(PDE4)。采用两步放射性同位素法,以[(3)H]-环磷酸鸟苷/[(3)H]-环磷酸腺苷研究淫羊藿苷对PDE5和PDE4活性的抑制作用。罂粟碱作为对照药物。
淫羊藿苷和罂粟碱对PDE5和PDE4活性均表现出剂量依赖性抑制作用。淫羊藿苷和罂粟碱对PDE5的半数抑制浓度(IC50)分别为0.432微摩尔/升和0.680微摩尔/升,对PDE4的IC50分别为73.50微摩尔/升和3.07微摩尔/升。淫羊藿苷和罂粟碱对PDE5的选择性效能(IC50的PDE4/PDE5)分别为167.67倍和4.54倍。
淫羊藿苷是一种特异性的环磷酸鸟苷PDE5抑制剂,有望开发成为治疗ED的口服有效药物。