Abstract
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 ≈60% 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-hydroxy-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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 1025-1030 |
| Number of pages | 6 |
| Journal | Hepatology |
| Volume | 21 |
| Issue number | 4 |
| DOIs | |
| State | Published - 1995 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Hepatology
Cite this
Influence of bezafibrate on hepatic cholesterol metabolism in gallstone patients : Reduced activity of cholesterol 7α-hydroxylase. / Stahlberg, Dagny; Reihner, Eva; Rudling, Mats; Berglund, Lars; Einarsson, Kurt; Angelin, BO O.
In: Hepatology, Vol. 21, No. 4, 1995, p. 1025-1030.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Influence of bezafibrate on hepatic cholesterol metabolism in gallstone patients
T2 - Reduced activity of cholesterol 7α-hydroxylase
AU - Stahlberg, Dagny
AU - Reihner, Eva
AU - Rudling, Mats
AU - Berglund, Lars
AU - Einarsson, Kurt
AU - Angelin, BO O.
PY - 1995
Y1 - 1995
N2 - 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 ≈60% 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-hydroxy-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.
AB - 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 ≈60% 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-hydroxy-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.
UR - http://www.scopus.com/inward/record.url?scp=0028931304&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0028931304&partnerID=8YFLogxK
U2 - 10.1016/0270-9139(95)90250-3
DO - 10.1016/0270-9139(95)90250-3
M3 - Article
C2 - 7705775
VL - 21
SP - 1025
EP - 1030
JO - Hepatology
JF - Hepatology
SN - 0270-9139
IS - 4
ER -