Inhibition of liver microsomal carnitine acyltransferases by sulphonylurea drugs.
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.
Broadway
N M
NM
Department of Biochemistry and Molecular Biology, University College London, UK.
Saggerson
E D
ED
D000818:Animals; D002333:Carnitine Acyltransferases / Q000037:antagonists & inhibitors*; D005905:Glyburide / Q000494:pharmacology*; D008079:Lipoproteins, VLDL / Q000378:metabolism; D008081:Liposomes / Q000378:metabolism; D008297:Male; D008316:Malonyl Coenzyme A / Q000494:pharmacology; D008862:Microsomes, Liver / Q000201:enzymology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014044:Tolbutamide / Q000494:pharmacology*; D014280:Triglycerides / Q000378:metabolism
D008079:Lipoproteins, VLDL; D008081:Liposomes; D014280:Triglycerides; C030106:very low density lipoprotein triglyceride; D008316:Malonyl Coenzyme A; D014044:Tolbutamide; D002333:Carnitine Acyltransferases; D005905:Glyburide