A novel in vitro model to screen steroid 5 alpha-reductase inhibitors against benign prostatic hyperplasia
文献类型:期刊论文
作者 | Sun, ZY; Tu, ZH |
刊名 | METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY
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出版日期 | 1998-05 |
卷号 | 20期号:4页码:283-287 |
关键词 | steroid 5 alpha reductase inhibitors nicotinamide adenine dinucleotide phosphate (NADPH) spectrophotometry drug screening model finasteride |
ISSN号 | 0379-0355 |
文献子类 | Article |
英文摘要 | A convenient and rapid in vitro model to screen steroid 5 alpha-reductase inhibitors, which are effective in the treatment of benign prostatic hyperplasia (BPH), was developed. In the presence of nicotinamide adenine dinucleotide phosphate (NADPH), steroid 5 alpha-reductase converts testosterone to dihydrotestosterone (DHT) which is a major etiologic factor of BPH. NADPH has characteristic absorbance at 340 nm, and the absorbance spectrum may be used to identify NADPH as a kind of the substrate in this enzymatic reaction. In this paper NADPH, steroid 5 alpha-reductase, series concentration of testosterone and finasteride, and 4 ml Tris-HCl buffer were continuously incubated together at 37 degrees C and the NADPH OD values were continually measured. The descending rate of NADPH OD340nm value by linear regression from the beginning to the 10th minute is close to the initial velocity of the enzymatic reaction. The precise activity of the steroid 5 alpha-reductase was the slope after subtracting that of the the blank control. The inhibition constant (K-i) of steroid 5 alpha-reductase inhibitors could be calculated according to the Lineweaver-Burk plots. Two drug screening models, the most common isotope model and the novel model, were compared in this paper: The result showed that the latter one is more economical, quicker and more effective than the former one. (C) 1998 Prous Science. All rights reserved. |
WOS关键词 | FINASTERIDE ; DEFICIENCY ; MEN |
WOS研究方向 | Pharmacology & Pharmacy |
语种 | 英语 |
WOS记录号 | WOS:000074262700001 |
出版者 | PROUS SCIENCE, SA |
源URL | [http://119.78.100.183/handle/2S10ELR8/274843] ![]() |
专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
通讯作者 | Sun, ZY |
作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China |
推荐引用方式 GB/T 7714 | Sun, ZY,Tu, ZH. A novel in vitro model to screen steroid 5 alpha-reductase inhibitors against benign prostatic hyperplasia[J]. METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY,1998,20(4):283-287. |
APA | Sun, ZY,&Tu, ZH.(1998).A novel in vitro model to screen steroid 5 alpha-reductase inhibitors against benign prostatic hyperplasia.METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY,20(4),283-287. |
MLA | Sun, ZY,et al."A novel in vitro model to screen steroid 5 alpha-reductase inhibitors against benign prostatic hyperplasia".METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY 20.4(1998):283-287. |
入库方式: OAI收割
来源:上海药物研究所
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