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

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Xin ZC, Kim EK, Lin CS, Liu WJ, Tian L, Yuan YM, Fu J

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

Asian J Androl. 2003 Mar;5(1):15-8.

PubMed ID

12646997 [ View in PubMed

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Abstract

AIM: To clarify the mechanism of the therapeutic action of icariin on erectile 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 [(3)H]-cGMP/[(3)H]-cAMP. Papaverine served as the control drug. RESULTS: 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. CONCLUSION: Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Papaverine	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	Protein	Humans	Yes	Inhibitor	Details