HETEROGENEITY OF CYP3A ISOFORMS METABOLIZING ERYTHROMYCIN AND CORTISOL
HETEROGENEITY OF CYP3A ISOFORMS METABOLIZING ERYTHROMYCIN AND CORTISOL
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DOI：
10.1038/clpt.1992.3
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发表时间：
1992-01-01
影响因子：
6.7
通讯作者：
GUZELIAN, PS
中科院分区：
文献类型：
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作者：
HUNT, CM;WATKINS, PB;GUZELIAN, PS
红霉素的N-去甲基化和皮质醇的6-β-羟基化都是人肝微粒体中糖皮质激素诱导的CYP 3A的功能。 为了确定6-β-羟基化和红霉素N-去甲基化是否由相似或不同的CYP 3A亚型催化，在9名患者中，将最近描述的[C-14]-红霉素呼气试验所反映的红霉素N-去甲基化酶活性与尿6-β-羟基皮质醇/皮质醇比值（皮质醇6-β-羟化酶活性的测量）进行比较。 红霉素N-去甲基化变化四倍，6-β-羟基皮质醇/皮质醇的比例变化七倍，这些活动之间没有发现相关性（r2 = 0.065）。 CYP 3A的新的非侵入性测试强烈表明皮质醇6-β-羟基化和红霉素N-去甲基化由不同的CYP 3A亚型进行。
The N-demethylation of erythromycin and 6-beta-hydroxylation of cortisol are both functions of the glucocorticoid-inducible CYP3A in human liver microsomes. To determine whether 6-beta-hydroxylation and erythromycin N-demethylation are catalyzed by similar or distinct CYP3A isoforms, erythromycin N-demethylase activity, as reflected by the recently described [C-14]-erythromycin breath test, was compared with urinary 6-beta-hydroxycortisol/cortisol ratios, a measure of cortisol 6-beta-hydroxylase activity, in nine patients. Erythromycin N-demethylation varied fourfold and 6-beta-hydroxycortisol/cortisol ratios varied sevenfold among the subjects; no correlation was found between these activities (r2 = 0.065). New noninvasive tests of CYP3A strongly suggest cortisol 6-beta-hydroxylation and erythromycin N-demethylation are performed by distinct CYP3A isoforms.