The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5alpha-reductase inhibitors LTZ-8 and others
文献类型：期刊论文
| 作者 | Xin J(欣坚); Tian WS(田伟生); Sun YY(孙云阳); Tu CH(屠曾宏) |
| 刊名 | Chinese Journal of Pharmacology and Toxicology
 |
| 出版日期 | 2003 |
| 卷号 | 17期号:5页码:395-400 |
| 关键词 | prostatic hyperplasia oxidoreductases testosterone derivatives LTZ-8 LTZ-8 |
| ISSN号 | 1000-3002 |
| 其他题名 | 甾体5alpha-还原酶抑制剂LTZ-8和类似物的筛选及其抗前列腺增生作用 |
| 文献子类 | Article |
| 英文摘要 | AIM To screen new anti-prostatic hyperplasia drugs LTZ-8 and others(testosterone derivatives with different groups at C-3, C-4 and C-17), which are different structures of steroid 5alpha-reductase inhibitors. METHODS Isotope screening method was used to determine the ability of LTZ-8 to inhibit steroid 5alpha-reductase in vitro. Healthy male rats, which were castrated and injected testosterone to induce the regrowth of glandular cells, were selected as animal model. LTZ-8 was given orally once a day (3, 10 and 30 mg*kg-1) for 30 d. Wet and dry prostate weight was quantified and morphological structures of prostate were detected under light microscope. RESULTS LTZ-1, LTZ-5, LTZ-6 and LTZ-8 showed inhibitory effect on the activity of 5alpha-reductase,and LTZ-8 was the most effective one [Ki=(21.02.2)nmol*L-1]. Both the wet and dry prostate weight was reduced by 82% and 86% in LTZ-8 treated group (30 mg*kg-1) compared with control group respectively (P<0.05). Prostatic glandular cell height and acinar luminal area were decreased by LTZ-8 treatment in a dose-dependent manner. CONCLUSIONLTZ-8 inhibits steroid 5alpha-reductase activity in vitro and blocks the prostatic hyperplasia in testosterone-induced castrated rats. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 英语 |
| CSCD记录号 | CSCD:1494406 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268442]  |
| 专题 | 药物安全性评价中心 |
| 作者单位 | 1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, State Key Laboratory of Drug Research, ShangHai 201203, China.; 2.Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, ShangHai 200032, China. |
| 推荐引用方式 GB/T 7714 | Xin J,Tian WS,Sun YY,et al. The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5alpha-reductase inhibitors LTZ-8 and others[J]. Chinese Journal of Pharmacology and Toxicology,2003,17(5):395-400. |
| APA | 欣坚,田伟生,孙云阳,&屠曾宏.(2003).The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5alpha-reductase inhibitors LTZ-8 and others.Chinese Journal of Pharmacology and Toxicology,17(5),395-400. |
| MLA | 欣坚,et al."The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5alpha-reductase inhibitors LTZ-8 and others".Chinese Journal of Pharmacology and Toxicology 17.5(2003):395-400. |
入库方式： OAI收割
来源：上海药物研究所
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