紫外分光光度法体外筛选5α-还原酶抑制药  

UV-spectrophotometric Screening of 5α-Reductase Inhibitors in vitro

作　　者：周本宏[1,2] 郭敏[1] 吴丽宁[2] 陈栋[2] 

机构地区：[1]武汉大学人民医院药学部,武汉430060 [2]武汉大学药学院

出　　处：《中国药师》2011年第12期1714-1716,共3页China Pharmacist

摘　　要：目的:从天然产物中筛选5α-还原酶抑制药用于前列腺增生(BPH)的治疗。方法:从SD雄性大鼠前列腺组织中提取5α-还原酶,以睾酮为底物,加入还原型辅酶Ⅱ(NADPH),加入天然产物提取物建立酶反应体系,在37℃连续孵育,采用分光光度法在340 nm波长处检测辅酶NADPH 10 min内吸光度值变化,以前列康醇提物和生理盐水分别为阳性对照和阴性对照,筛选5α-还原酶抑制药,并对其活性成分进行初步确定。结果:8种天然产物中,槟榔、地榆提取物对5α-还原酶有一定抑制作用,且地榆醇提液,槟榔水提液和醇提液酶抑制活性较强。结论:紫外分光光度法操作简单、经济可行,适用于5α-还原酶抑制药的初步筛选。Objective： To screen 5α-reductase inhibitors from the natural products for the treatment of benign prostatic hyperplasia （BPH）. Method： Testosterone as the substrate and NADPH as the hydrogen donor,5α-reduetase extracted from the prostate tissue of male rats was added into the extracts of natural products to establish the enzyme reaction system by continuous incubation at 37℃. The change of enzymatic activity was recorded by the detection of NADPH with UV-spectrophotometry at the wavelength of 340 nm. Conprata pulean and physiological saline was chosen as the positive control and negative control, respectively for the screen of the 5α-reduetase. The obtained active ingredients were preliminarily identified by a spectrophotometer. Result： Among the 8 kinds of natural products, areca and sanguisorbae showed inhibition against 5α-reduetase. Conclusion： The economical, simple and quick method can be used to screen 5α-reduetase inhibitors.

关 键 词：5α-还原酶抑制药 紫外-可见分光光度法 还原型辅酶Ⅱ 天然产物 

分 类 号：R285.5[医药卫生—中药学]