Comparative induction of drug-metabolizing enzymes by hypolipidaemic compounds

General Pharmacology
A F Boiteux-AntoineG Siest

Abstract

1. The inducing effect of hypolipidaemic compounds containing arylcarboxylic structure (fenofibrate, bezafibrate, ciprofibrate) on drug-metabolizing enzymes was compared with that of other chemically different molecules (probucol, 1-benzylimidazole) in rat liver. 2. Hepatomegaly was closely associated to the decrease in triglycerides and cholesterol contents in plasma. 3. Lauric acid hydroxylation and hydratation of trans-stilbene oxide by the cytosolic epoxide hydrolase were markedly increased by the arylcarboxylic acids (fenofibrate, bezafibrate and ciprofibrate). The determination of the concentration in microsomal epoxide hydrolase by immunoassay revealed no change in the protein amount within the membrane; only the specific activity was enhanced by bezafibrate and 1-benzylimidazole, suggesting an activation process. 4. Bilirubin glucuronidation was increased by the arylcarboxylic structures and by 1-benzylimidazole; by contrast probucol decreased this activity.

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Citations

Aug 15, 2009·PPAR Research·Melissa Runge-Morris, Thomas A Kocarek
Oct 23, 1998·Experimental and Toxicologic Pathology : Official Journal of the Gesellschaft Für Toxikologische Pathologie·W KlingerW Kühnel
Jul 25, 2003·Experimental and Toxicologic Pathology : Official Journal of the Gesellschaft Für Toxikologische Pathologie·Amelie LuppChristian Fleck
Sep 19, 2003·Biochemical and Biophysical Research Communications·Patricia von DippeDaniel Levy

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