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

共 50 条

[1] Methylation of 6-mercaptopurine and 6-thioguanine by thiopurine S-methyltransferase A comparison of activity in red blood cell samples of 199 blood donorsA comparison of activity in red blood cell samples of 199 blood donors
T. Kröplin
H. Iven
[J]. European Journal of Clinical Pharmacology, 2000, 56 : 343 - 345
[2] Comparison of 6-mercaptopurine with 6-thioguanine for the analysis of thiopurine S-methyltransferase activity in human erythrocyte by LC-MS/MS
Mei, Shenghui
Li, Xindi
Gong, Xiaoqing
Zhang, Xiaoyi
Li, Xingang
Yang, Li
Zhu, Leting
Zhou, Heng
Liu, Yonghong
Zhou, Anna
Zhang, Xinghu
Zhao, Zhigang
[J]. BIOMEDICAL CHROMATOGRAPHY, 2017, 31 (09)
[3] Azathioprine, 6-mercaptopurine and thiopurine S-methyltransferase
Roberts-Thomson, C
Butler, WJ
[J]. JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY, 2005, 20 (06) : 955 - 955
[4] Individualizing therapy with 6-mercaptopurine and 6-thioguanine related to the thiopurine methyltransferase genetic polymorphism
Lennard, L
Lilleyman, JS
[J]. THERAPEUTIC DRUG MONITORING, 1996, 18 (04) : 328 - 334
[5] Why measure thiopurine methyltransferase activity? Direct administration of 6-thioguanine might be the alternative for 6-mercaptopurine or azathioprine
de Jong, D
Mulder, CJJ
van Sorge, AA
[J]. GUT, 2001, 49 (06) : 874 - 874
[6] ASSAY OF 6-THIOGUANINE NUCLEOTIDE, A MAJOR METABOLITE OF AZATHIOPRINE, 6-MERCAPTOPURINE AND 6-THIOGUANINE, IN HUMAN RED-BLOOD-CELLS
LENNARD, L
MADDOCKS, JL
[J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 1983, 35 (01) : 15 - 18
[7] Thiopurine S-methyltransferase activity in Japanese subjects:: metabolic activity of 6-mercaptopurine 6-methylation in different TPMT genotypes
Nishida, A
Kubota, T
Yamada, Y
Higashi, K
Kitamura, K
Nakahara, K
Iga, T
[J]. CLINICA CHIMICA ACTA, 2002, 323 (1-2) : 147 - 150
[8] High thiopurine methyltransferase expression confers different levels of resistance with 6-thioguanine compared to 6-mercaptopurine
Coulthard, S
Hogarth, L
Minto, L
Redfern, C
Hall, A
[J]. BRITISH JOURNAL OF CANCER, 2000, 83 : 64 - 64
[9] Differential role of thiopurine methyltransferase in the cytotoxic effects of 6-mercaptopurine and 6-thioguanine on human leukemia cells
Karim, Hazhar
Ghalali, Aram
Lafolie, Pierre
Vitols, Sigurd
Fotoohi, Alan K.
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2013, 437 (02) : 280 - 286
[10] Reference intervals for thiopurine S-methyltransferase activity in red blood cells using 6-thioguanine as substrate and rapid non-extraction liquid chromatography
Ford, LT
Cooper, SC
Lewis, MJV
Berg, JD
[J]. ANNALS OF CLINICAL BIOCHEMISTRY, 2004, 41 : 303 - 308

← 1 2 3 4 5 →