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目的:比较不同中国人肝微粒体中几种重要细胞色素P450(CYP)的酶含量和活性。方法:运用West-ern斑点分析和光密度扫描,对17个汉族、17个壮族和8个苗族受试者肝微粒体中的细胞色素P4501A2(CYP1A2)、2C9及3A4进行定量;非那西丁、甲磺丁脲、异喹胍和奥美拉唑分别用于体外测量CYP1A2、2C9、2D6及3A4的活性。结果:CYP1A2、2C9及3A4的含量和活性具有很大的个体间变异,另外CYP2D6的活性在各样本间也有很大差异;CYP3A4(32％)是中国人肝微粒体中含量最丰富的CYP,CYP2C9(19％)和CYP1A2(16％)的含量也很可观;除了CYP1A2的含量和活性具有一定的种族和性别差异外,未发现其它CYP具有种族和性别差异;CYP1A2、2C9和3A4的酶蛋白含量分别和它们的活性具有很好的相关性。结论:我们的结果为在中国人中进行药物代谢研究提供了非常有价值的信息。
OBJECTIVE: To compare the enzyme activities and activities of several important cytochrome P450s (CYP) in different Chinese human liver microsomes. METHODS: Cytochrome P4501A2 (CYP1A2), 2C9 and 3A4 in liver microsomes from 17 Han, 17 Zhuang and 8 Hmong subjects were quantified using West-ern speckle analysis and optical density scanning. Phenacetin, Metbutulbulin, isoquinidine and omeprazole were used to measure the activities of CYP1A2, 2C9, 2D6 and 3A4, respectively. Results: The content and activity of CYP1A2, 2C9 and 3A4 had great interindividual variation. In addition, the activity of CYP2D6 was also significantly different among samples. CYP3A4 (32%) was the most abundant CYP in Chinese human liver microsomes, The content of CYP2C9 (19%) and CYP1A2 (16%) were also significant. No other CYP was found to have racial and gender differences except for the content and activity of CYP1A2. CYP1A2, 2C9 and 3A4 Content and their activity, respectively, has a good correlation. Conclusion: Our results provide very valuable information for the study of drug metabolism in Chinese.