ISOLATION OF AN IMMUNOSUPPRESSIVE METABOLITE OF FK506 GENERATED BY HUMAN MICROSOME PREPARATIONS

被引：31

作者：

CHRISTIANS, U

RADEKE, HH

KOWNATZKI, R

SCHIEBEL, HM

SCHOTTMANN, R

SEWING, KF

机构：

[1] MED HSCH HANNOVER,INST ALLGEMEINE PHARMAKOL,KONSTANTY GUTSCHOW STR 8,W-3000 HANNOVER 61,GERMANY

[2] HANOVER MED SCH,INST MOLEK PHARMAKOL,W-3000 HANNOVER 61,GERMANY

[3] HANOVER MED SCH,ZENTRUM BIOCHEM,W-3000 HANNOVER 61,GERMANY

[4] TECH UNIV BRAUNSCHWEIG,INST ORGAN CHEM,W-3300 BRAUNSCHWEIG,GERMANY

来源：

CLINICAL BIOCHEMISTRY | 1991年 / 24卷 / 03期

关键词：

FK506; BIOTRANSFORMATION; IMMUNOSUPPRESSIVE AGENTS;

D O I：

10.1016/0009-9120(91)80019-Y

中图分类号：

R446 [实验室诊断]; R-33 [实验医学、医学实验];

学科分类号：

1001 ;

摘要：

Metabolism of FK506, a 23 member macrolide under clinical investigation as immunosuppressant after transplantation, was studied using human liver microsomes. Two fractions isolated by semi-preparative HPLC were identified by negative fast atom bombardment mass spectrometry as FK506 metabolites with mass peaks at m/z = 790 indicating demethylation of the mother compound. The immunosuppressive activity of one metabolite was evaluated in a ConA-stimulated peripheral rat lymphocyte assay. FK506 had an IC50 of 0.186 nmol/L and the metabolite tested of 1.89 nmol/L.

引用

页码：271 / 275

页数：5

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