Influence of bezafibrate on hepatic cholesterol metabolism in gallstone patients: Reduced activity of cholesterol 7α-hydroxylase

✍ Scribed by Dagny Ståhlberg; Eva Reihnér; Mats Rudling; Lars Berglund; Kurt Einarsson; Bo Angelin

• Publisher: John Wiley and Sons
• Year: 1995
• Tongue: English
• Weight: 764 KB
• Volume: 21
• Category: Article
• ISSN: 0270-9139
• DOI: 10.1002/hep.1840210421

✦ Synopsis

Bezafibrate is a hypolipidemic fibric acid derivative known to induce cholesterol supersaturation of bile. To characterize its effects on hepatic cholesterol metabolism, 31 normolipidemic, normal-weight patients with gallstones undergoing cholecystectomy were studied, Eleven patients (5 men) were randomized to treatment with bezafibrate, 200 mg three times daily for 4 weeks before operation; the remaining 20 patients (5 men) served as nontreatment controls. At operation, a liver biopsy specimen was obtained under standardized conditions and several important parameters of cholesterol metabolism were assayed. Bezafibrate treatment lowered total plasma cholesterol and triglycerides 30% and 37%, respectively. The hepatic cholesterol 7a-hydroxylase activity was reduced by ~6 0 % in the bezafibrate treated patients compared with the controls, whereas the acyl-coenzyme A: cholesterol acyltransferase (ACAT) activity was similar in the two groups. The total 3-hy-dro~3-methylglutaryl coenzyme A (HMG CoA) reductase activity was increased twofold in the treated patients, whereas the active enzyme remained about the same as in the controls. The low-density lipoprotein (LDL) receptor binding activity was unaffected by the treatment. Bezafibrate treatment significantly reduces cholesterol 7a-hydroxylase activity, and it is suggested that this may play an important role for the development of supersaturated bile during such therapy. (HEPATOL