INHIBITION OF LIVER MICROSOMAL CARNITINE ACYLTRANSFERASES BY SULFONYLUREA DRUGS

被引：10

作者：

BROADWAY, NM ^{[1
]}

SAGGERSON, ED ^{[1
]}

机构：

[1] UNIV LONDON UNIV COLL,DEPT BIOCHEM & MOLEC BIOL,LONDON WC1E 6BT,ENGLAND

来源：

FEBS LETTERS | 1995年 / 371卷 / 02期

基金：

英国医学研究理事会;

关键词：

CARNITINE ACYLTRANSFERASES; GLIBENCLAMIDE; LIVER; MICROSOME; SULFONYLUREAS; TOLBUTAMIDE;

D O I：

10.1016/0014-5793(95)00877-C

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The sulphonylureas glibenclamide and tolbutamide inhibited carnitine acyltransferase activities in rat liver microsomes. Glibenclamide was a more potent inhibitor than tolbutamide. The effect of tolbutamide on the malonyl-CoA-inhibitable transferase was influenced by the phospholipid/detergent environment ,whereas the effect of glibenclamide was not. Glibenclamide was a more potent inhibitor of the malonyl-CoA-inhibitable transferase than of the malonyl-CoA-insensitive enzyme. The extent of inhibition of the malonyl-CoA-inhibitable transferase by tolbutamide,was similar to its effect on VLDL triacylglycerol secretion as reported by Wiggins and Gibbons [Biochem. J. 284 (1992) 457-462] possibly supporting the suggestion that microsomal carnitine acyltransferases are involved in VLDL triacylglycerol assembly/secretion.

引用

页码：137 / 139

页数：3

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