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强心剂舒马唑治疗的大鼠肝微粒体中细胞色素P-450同工酶的诱导作用。

Induction of cytochrome P-450 isozymes in liver microsomes of rats treated with the cardiotonic agent sulmazole.

作者信息

Müller-Enoch D, Dannan G A, Rudolf B, Friedl H P

出版信息

Arzneimittelforschung. 1985;35(4):698-703.

PMID:4015736
Abstract

Pretreatment of adult male rats with sulmazole (AR-L 115 BS) results in a 2-6-fold increase of the liver microsomal scoparone O-demethylation and 7-ethoxycoumarin O-deethylation activity. The change in the ratio of the demethylation products scopoletin to isoscopoletin from 1 : 1.8 +/- 0.1 in control microsomes to 1: 2.5 +/- 0.1 in microsomes from sulmazole pretreated rats is statistically significant. Sulmazole produces a modified type II difference spectrum when added to microsomes of control or sulmazole-pretreated rats. Immunoquantitation of seven cytochromes P-450 showed that two forms, namely P-450 beta NF/ISF-G and P-450 beta NF-B, are increased 3-4-fold in the microsomes of sulmazole-pretreated rats.

摘要

用舒马唑(AR-L 115 BS)对成年雄性大鼠进行预处理,会导致肝微粒体滨蒿内酯O-脱甲基化和7-乙氧基香豆素O-脱乙基化活性增加2至6倍。脱甲基产物滨蒿素与异滨蒿素的比例变化具有统计学意义,从对照微粒体中的1:1.8±0.1变为舒马唑预处理大鼠微粒体中的1:2.5±0.1。当将舒马唑添加到对照或舒马唑预处理大鼠的微粒体中时,会产生一种改良的II型差示光谱。对七种细胞色素P-450进行免疫定量分析表明,在舒马唑预处理大鼠的微粒体中,两种形式,即P-450βNF/ISF-G和P-450βNF-B增加了3至4倍。

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