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Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells
Ning, Hongxiu; Xin, Zhong-Cheng; Lin, Guiting; Banie, Lia; Lue, Tom F.; Lin, Ching-Shwun
刊名UROLOGY
2006-12-01
DOI10.1016/j.urology.2006.09.031
68期:6页:1350-1354
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Urology & Nephrology
研究领域[WOS]Urology & Nephrology
关键词[WOS]NITRIC-OXIDE ; CGMP ; EXPRESSION ; ISOFORMS ; APOPTOSIS ; BINDING
英文摘要

Objectives. To investigate the effect of icariin on the cyclic guanosine monophosphate (cGMP)-hydrolytic activity of phosphodiesterase-5 (PDE5) isoforms and the cGMP levels in cavernous smooth muscle cells treated with sodium nitroprusside (SNP).

Methods. PDE5 isoforms (PDE5A1, A2, and A3) were isolated from sf9 insect cells infected with baculoviruses carrying PDE5 isoform cDNA. Icariin was isolated from Epimedii herba. Varying amounts (10(-6) to 10(-11) M) of icariin or zaprinast were added to reaction mixtures containing PDE5 isoforms and cGMP. The inhibitory effects of icariin and zaprinast were analyzed by GraphPad Software and are expressed as concentration that inhibits 50% (IC50) values. Cavernous smooth muscle cells were isolated from 3-month-old rats, treated with icariin (100 and 200 mu M) or zaprinast (200 mu M) for 15 minutes, and then with 10 mu M SNP for 30, 60, 120, 240, and 360 minutes. The cells were then analyzed for the cGMP concentration using an enzyme immunoassay system.

Results. Icariin inhibited PDE5A1, A2, and A3 with an ICS, value of 1.0, 0.75, and 1.1 mu M, respectively. The corresponding ICS, values for zaprinast were 0.33, 0.23, and 0.32 mu M. Icariin consistently outperformed the control (SNP-only treatment) in maintaining greater cGMP levels, particularly at the greater concentration of 200 mu M. In contrast, zaprinast at 200 g,M did better than the control only at 60 and 360 minutes.

Conclusions. Icariin was inhibitory to all three PDE5 isoforms with similar IC50 values, which were approximately three times greater than those for zaprinast. Icariin was able to enhance cGMP levels in SNP-treated cavernous smooth muscle cells.

语种英语
WOS记录号WOS:000242869900053
引用统计
被引频次:45[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/55836
专题北京大学第一临床医学院_男科中心
作者单位1.Univ Calif San Francisco, Sch Med, Knuppe Mol Urol Lab, Dept Urol, San Francisco, CA 94115 USA
2.Peking Univ, Hosp 1, Androl Ctr, Beijing 100871, Peoples R China
推荐引用方式
GB/T 7714
Ning, Hongxiu,Xin, Zhong-Cheng,Lin, Guiting,et al. Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells[J]. UROLOGY,2006,68(6):1350-1354.
APA Ning, Hongxiu,Xin, Zhong-Cheng,Lin, Guiting,Banie, Lia,Lue, Tom F.,&Lin, Ching-Shwun.(2006).Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells.UROLOGY,68(6),1350-1354.
MLA Ning, Hongxiu,et al."Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells".UROLOGY 68.6(2006):1350-1354.
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