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Volume 5, Issue 1 (March 2003) 5, 15–18;

Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities

Z.C. Xin, E.K. Kim, C.S. Lin, W.J. Liu, L. Tian, Y.M. Yuan, J. Fu

1.Department of Urology, the 1st Hospital, Peking University, Beijing 100034, China
    2.Department of Life Science, Pohang University of Science and Technology, Pohang, Korea
    3.Knuppe Molecular Urology Laboratory, Department of Urology, UCSF, USA

Advance online publication 1 March 2003


Aim: To clarify the mechanism of the therapeutic action of icariin on erectlile dysfunction (ED). Methods: 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 [3H]-cGMP/[3H]-cAMP. Papaverine served as the control drug. Results: Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. The IC50 of Icariin and papaverine on PDE5 were 0.432 µmol/L and 0.680 µmol/L, respectively and those on PDE4, 73.50 µmol/L and 3.07 µmol/L, respectively. The potencies of selectivity of icariin and papaverine on PDE5 (PDE4/PDE5 of IC50) were 167.67 times and 4.54 times, respectively. Conclusion: Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED.

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