苯巴比妥或3-甲基胆蒽预诱导的雄性大鼠肝微粒体中苯并硝唑和硝呋替莫的硝基还原酶活性。
Benznidazole and nifurtimox nitroreductase activity in liver microsomes from male rats preinduced with phenobarbital or 3-methylcholanthrene.
作者信息
Aguilar E G, de Arranz C K, de Toranzo E G, Castro J A
出版信息
Res Commun Chem Pathol Pharmacol. 1985 Dec;50(3):443-6.
Liver microsomes from Sprague-Dawley male rats are able to biotransform Benznidazole (Bz) or Nifurtimox (NFX) by nitroreduction. Pretreatment of the rats during three days with phenobarbital (80 mg/kg/day, ip) but not with 3-methylcholanthrene (35 mg/kg/day ip) increased both Bz and NFX nitroreductase activity. Results suggest that cytochrome P-450 but not cytochrome P-448 is involved in the nitroreduction of these two chemotherapeutic agents against Chagas' disease. Possible pharmacological and toxicological implications of these observations are discussed.
来自斯普拉格-道利雄性大鼠的肝微粒体能够通过硝基还原作用对苯硝唑（Bz）或硝呋替莫（NFX）进行生物转化。用苯巴比妥（80毫克/千克/天，腹腔注射）对大鼠进行三天预处理可增加Bz和NFX的硝基还原酶活性，但用3-甲基胆蒽（35毫克/千克/天，腹腔注射）预处理则不会。结果表明，细胞色素P-450而非细胞色素P-448参与了这两种治疗恰加斯病的化疗药物的硝基还原过程。讨论了这些观察结果可能的药理学和毒理学意义。
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