Effects of clofibrate on the main regulatory enzymes of cholesterogenesis.
The in vivo effect of clofibrate on the main regulatory enzymes of cholesterogenesis has been comparatively studied for the first time in chick liver and brain. 3-Hydroxy-3-methylglutaryl-CoA reductase and mevalonate 5-pyrophosphate decarboxylase from chick liver were significantly inhibited by this hypocholesterolenic drug, while mevalonate kinase and mevalonate 5-phosphate kinase were not affected. No enzyme from chick brain was significantly inhibited by the in vivo treatment. However, both liver and brain reductase activity was inhibited in vitro by clofibrate, inhibition that was progressive with increasing concentrations (1.25-5.00 mM) of drug.
Castillo
M
M
Department of Biochemistry and Molecular Biology, University of Granada, Spain.
Burgos
C
C
Rodríguez-Vico
F
F
Zafra
M F
MF
García-Peregrín
E
E
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000201:enzymology; D002262:Carboxy-Lyases / Q000037:antagonists & inhibitors; D002784:Cholesterol / Q000096:biosynthesis*; D002994:Clofibrate / Q000494:pharmacology*; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D008297:Male; D010770:Phosphotransferases / Q000037:antagonists & inhibitors; D017853:Phosphotransferases (Alcohol Group Acceptor); D017856:Phosphotransferases (Phosphate Group Acceptor)
D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D002784:Cholesterol; D010770:Phosphotransferases; D017853:Phosphotransferases (Alcohol Group Acceptor); C021796:mevalonate kinase; D017856:Phosphotransferases (Phosphate Group Acceptor); C022371:phosphomevalonate kinase; D002262:Carboxy-Lyases; C022503:pyrophosphomevalonate decarboxylase; D002994:Clofibrate