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学科主题: 天然产物有机化学
题名: The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5 α-reductase inhibitors LTZ-8 and others
其他题名: 甾体 5 α-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
作者: Xin J(欣坚) ; Tian WS(田伟生) ; Sun YY(孙云阳) ; Du CH(杜曾宏)
通讯作者: 杜曾宏
刊名: 中国药理与毒理学杂志
发表日期: 2003-01-01
卷: 17, 期:5, 页:395-400
部门归属: 中国科学院上海生命科学院上海药物所新教研室重点实验室; 中国科学院上海有机化学研究所生命有机国家重点实验室
英文摘要: AIN to screen new anti-prostatic hypeplasia drugs LTZ-8 and others (testosterone derivatives with different groups at C-3,C-4 and C-17), which are different structures of seroid 5 α-reductase in vitro. Healthyl 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 protate were detected under light microscope. RESULTS LTZ-1, LTZ-5, LTZ-6, and LTZ-8 showed inhibitory effect on the activity of 5 α-reductase, and LTZ-8 was the most effective one [Ki=(21.0±2.2) nmol.L-1]. Both the wet and dry prostate weight was reduced by 82% 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. XONCLUSION LTZ-8 inhibits steroid 5 α-reductase activity in vitro and blocks the prostatic hypeplasia in testosterone-induced castrated rat.
语种: 英语
内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/23836
Appears in Collections:中科院天然产物有机化学重点实验室_期刊论文

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Recommended Citation:
Xin J,Tian WS,Sun YY,et al. The screening and anti-prostatic hyperplasia activity assessment of novel steroid 5 α-reductase inhibitors LTZ-8 and others[J]. 中国药理与毒理学杂志,2003,17(5):395-400.
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