| Effects of icariin on cGMP—specific PDE5 and cAMP—specific PDE4 activities |
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| 作者姓名： | Xin ZC Kim EK Lin CS Liu WJ Tian L Yuan YM Fu J |
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| 作者单位： | [1]DepartmentofUrology,thelstHospital,PekingUniversity,Beijing100034,China [2]DepartmentofLifeScience,PhangUniversityofScienceandTechnology,Pohang,Korea [3]KunppeMolecularUrologyLaboratory,DepartmentofUrology,UCSF,USA |
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| 基金项目： | PresentedattheFirstAsia-PacificForumonAndrology,17-21October2002,Shanghai,China. |
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| 摘 要： | 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 form 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]-c GMP/^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 0.432μ mol/L and 0.680μmol/L,respectively and those on PDE4,73.50μmol/L and 3.07μmol/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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| 关 键 词： | 淫羊霍苷 PDE5 cGMP 阴茎勃起障碍 |
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[J].Asian Journal of Andrology,2003,5(1):15-18. |
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| Authors: | Xin Z C Kim E K Lin C S Liu W J Tian L Yuan Y M Fu J |
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| Institution: | Department of Urology, the 1st Hospital, Peking University, 8 Xishiku Street, Xicheng District, Beijing 100034, China. xinzc@bjmu.edu.cn |
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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. |
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| Keywords: | icariin PDE5 cGMP penile erection |
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