title: Cytosolic lipogenic enzymes: effect of fibric acid derivatives in vitro.
abstract: The effect of fibric acid derivatives, clofibric acid (CFB), bezafibrate (BFB), and gemfibrozil (GFB) on hepatic cytosolic enzymatic activities involved in saturated fatty acid synthesis has been estudied in vitro. From all the activities tested (fatty acid synthetase, acetyl-CoA carboxylase, ATP-citrate lyase, malic enzyme, malic dehydrogenase, glucose-6-phosphate dehydrogenase, and 6-phosphogluconate dehydrogenase), only acetyl-CoA carboxylase and glucose-6-phosphate dehydrogenase were significantly inhibited by fibrates, with the following order of potency: GFB > BFB > > CFB. The characteristics of the inhibition phenomena (IC50, kinetic analysis, time and protein dependence, etc) and their transcendence to the effects of fibric acid derivatives in vivo are discussed.
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, University of Barcelona, Spain.
authors.forename: R M
authors.initials: RM
authors.lastname: Sánchez
authors.forename: M
authors.initials: M
authors.lastname: Vázquez
authors.forename: M
authors.initials: M
authors.lastname: Alegret
authors.forename: M
authors.initials: M
authors.lastname: Viñals
authors.forename: T
authors.initials: T
authors.lastname: Adzet
authors.forename: M
authors.initials: M
authors.lastname: Merlos
authors.forename: J C
authors.initials: JC
authors.lastname: Laguna
mesh_terms: D000818:Animals; D001629:Bezafibrate / Q000494:pharmacology*; D002995:Clofibric Acid / Q000494:pharmacology*; D003600:Cytosol / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005227:Fatty Acids / Q000096:biosynthesis*; D015248:Gemfibrozil / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology* / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D004791:Enzyme Inhibitors; D005227:Fatty Acids; D002995:Clofibric Acid; D015248:Gemfibrozil; D001629:Bezafibrate