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某些红霉素衍生物在大鼠体内是一种细胞色素P - 450的强诱导剂,该细胞色素P - 450与由16α - 孕烯醇酮腈诱导产生的细胞色素P - 450非常相似。

Some erythromycin derivatives are strong inducers in rats of a cytochrome P-450 very similar to that induced by 16 alpha-pregnenolone carbonitrile.

作者信息

Sartori E, Delaforge M, Mansuy D, Beaune P

出版信息

Biochem Biophys Res Commun. 1985 May 16;128(3):1434-9. doi: 10.1016/0006-291x(85)91100-3.

Abstract

Erythromycin derivatives having lost the cladinose moiety, erythralosamine and its mono- and diacetate, are strong inducers of liver cytochrome P-450, better than troleandomycin, in rats. The major cytochrome P-450 form induced by all these macrolides is electrophoretically and immunologically indistinguishable from the major form induced in rats by pregnenolone carbonitrile. This form is particularly able to metabolize the macrolides and to lead to the corresponding 456 nm absorbing cytochrome P-450 metabolite complexes in vivo and in vitro.

摘要

失去了克拉定糖部分的红霉素衍生物、红霉胺及其单乙酸酯和二乙酸酯,在大鼠体内是肝脏细胞色素P - 450的强诱导剂,比醋竹桃霉素更强。所有这些大环内酯类药物诱导的主要细胞色素P - 450形式,在电泳和免疫方面与孕烯醇酮腈在大鼠体内诱导的主要形式无法区分。这种形式特别能够代谢大环内酯类药物,并在体内和体外导致相应的在456 nm处有吸收的细胞色素P - 450代谢物复合物。

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