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目的:体内及试管内研究汉族人美托洛尔 (Met)α-羟化能力.方法:反相离子对高效液相色谱法测定Met和α-羟基美托洛尔(HM).结果:96名汉族人尿Met和HM比值(MR)的对数示单基因遗传特征性双态频率分布,仅发现1例弱代谢者(MR=199.3),95例强代谢者MR为3.1±2.5.性别、吸烟、饮茶对尿Met,HM及MR均无影响.试管内研究发现NADH对人肝微粒体Met α-羟化酶活性无影响,该酶K_m为89.6 μmol L~(-1),V_(max)为39.5 ngmg~(-1)min~(-1).在8例汉族人肝微粒体中未发现该酶缺陷者,测得其活性为31.4±22.1 ngmg~(-1) min~(-1).结论:中国汉族人Met α-羟化弱代谢者发生率低,NADH未参与人肝微粒体Met α-羟化反应.
OBJECTIVE: To study the α-hydroxylation ability of metoprolol in Han Chinese in vitro and in vitro.METHODS: Met and α-hydroxy metoprolol were determined by reversed-phase high performance liquid chromatography.RESULTS: 96 The logarithm of the urinary Met and HM ratio (MR) in the Han Chinese population showed a characteristic two-state frequency distribution of single-gene inheritance. Only 1 poor metabolizer (MR = 199.3) was found and 95 MRs were 3.1 ± 2.5. , Smoking and drinking tea had no effect on urinary Met, HM and MR.It was found in vitro that NADH had no effect on the activity of Met-hydroxylase in human liver microsomes, K_m of the enzyme was 89.6 μmol L -1, (max) was 39.5 ngmg -1 min -1 .The activity of the enzyme was found to be 31.4 ± 22.1 ng mg ~ (-1) min ~ (-1) in eight Han Han microsomes, (-1) .Conclusion: The incidence of Met-hydroxylation in Chinese Han population is low, and NADH is not involved in Met-hydroxylation of human liver microsome.