Methylation of 6-mercaptopurine and 6-thioguanine by thiopurine S-methyltransferase -: A comparison of activity in red blood cell samples of 199 blood donors

被引：25

作者：

Kröplin, T ^{[1
]}

Iven, H ^{[1
]}

机构：

[1] Med Univ Lubeck, Dept Expt & Clin Pharmacol & Toxicol, D-23538 Lubeck, Germany

来源：

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY | 2000年 / 56卷 / 04期

关键词：

6-thioguanine; 6-mercaptopurine; thiopurine S-methyltransferase;

D O I：

10.1007/s002280000137

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Objectives: To compare 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) as substrates for the methylation reaction catalysed by the enzyme thiopurine S-methyltransferase (TPMT). Methods: TPMT activity in haemolysed red blood cells of healthy blood donors was determined twice, using the same experimental setting and equal molar concentrations of 6-TG and 6-MP as substrates. After extraction, the reaction products 6-methyl-TG and 6-methyl-MP were quantified using specific high-performance liquid chromatography procedures. Results: The medians of the TPMT activities from 199 blood donors were 54.4 nmol 6-MTG g(-1) Hb h(-1) when measured with 6-TG as the substrate and 35.8 nmol 6-MMP g(-1) Hb h(-1) when measured with 6-MP. The correlation coefficient for the 199 pairs of values was 0.8695. On average, TPMT activity was 34% lower with 6-MP as substrate than with 6-TG as substrate.

引用

页码：343 / 345

页数：3

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