氟他胺对大鼠肝脏中5α-还原酶、5β-还原酶和3-羟基类固醇脱氢酶的影响。

Effect of flutamide on 5 alpha-reductases, 5 beta-reductases, and 3-hydroxysteroid dehydrogenases in rat liver.

作者信息

Graef V, Golf S W, Tyrell C, Fehler M

机构信息

Institute of Clinical Chemistry and Pathobiochemistry, University Medical School, Giessen, FRG.

出版信息

Steroids. 1987 Jun;49(6):553-60. doi: 10.1016/0039-128x(87)90095-x.

DOI:10.1016/0039-128x(87)90095-x

PMID:3483296

Abstract

Flutamide (0.5 mM) decreased in vitro the activity of NADH-5 alpha-reductase (substrate testosterone) in liver homogenate of male and female rats, whereas no change of activity of NADPH-5 alpha-reductase was observed. NADH- and NADPH-5 beta-reductase activity increased only in liver of female, but not of male rats. NAD+-3 beta-hydroxysteroid dehydrogenase and NAD+-3 alpha-hydroxysteroid dehydrogenase (substrate 5 alpha-dihydro-testosterone) in liver homogenate from female rats were inhibited by flutamide (0.5 mM), whereas the activity of NADP+-3 alpha-hydroxysteroid dehydrogenase (substrate 5 alpha-dihydrotestosterone) and of NAD+-3 alpha-hydroxysteroid dehydrogenase (substrate 5 beta-dihydrotestosterone) increased in presence of flutamide. The activity of NADH- and NADPH-5 alpha-reductase decreased after flutamide administration to female rats at a dose of 5 mg per day for 7 days.

摘要

氟他胺（0.5毫摩尔）在体外降低了雄性和雌性大鼠肝脏匀浆中NADH - 5α - 还原酶（底物为睾酮）的活性，而NADPH - 5α - 还原酶的活性未观察到变化。NADH - 和NADPH - 5β - 还原酶活性仅在雌性大鼠肝脏中增加，而在雄性大鼠肝脏中未增加。氟他胺（0.5毫摩尔）抑制了雌性大鼠肝脏匀浆中的NAD⁺ - 3β - 羟基类固醇脱氢酶和NAD⁺ - 3α - 羟基类固醇脱氢酶（底物为5α - 二氢睾酮），而在氟他胺存在的情况下，NADP⁺ - 3α - 羟基类固醇脱氢酶（底物为5α - 二氢睾酮）和NAD⁺ - 3α - 羟基类固醇脱氢酶（底物为5β - 二氢睾酮）的活性增加。以每天5毫克的剂量给雌性大鼠连续给药7天氟他胺后，NADH - 和NADPH - 5α - 还原酶的活性降低。