Schriewer H, Rauen H M
Arzneimittelforschung. 1977;27(9):1691-4.
The effect of silybin dihemisuccinate on the hepatic biosynthesis of cholesterol was studied by measuring the incorporation of [1-14C]-acetate and [2-14C]-mevalonate in the postmitochondrial supernatant of liver homogenates. 2. Under absolute in vitro conditions, silybin dihemisuccinate inhibits the biosynthesis of cholesterol in dependence on its concentration. With [1-14C]-acetate or [2-14C]-mevalonate the concentrations of silybin for 50% inhibition are 0.37 mM or 0.40 mM, resp. 3. 30 min after i.v. injection of 150.6 mg silybin dihemisuccinate/kg with both precursors the biosynthesis of cholesterol studied in vitro is diminished in comparison to controls. 60 min or 24 h after i.v. injection of silybin no effects on in vitro biosynthesis of cholesterol can be observed.
通过测量[1-14C]-乙酸盐和[2-14C]-甲羟戊酸在肝脏匀浆线粒体后上清液中的掺入情况，研究了二琥珀酸半酯水飞蓟宾对肝脏胆固醇生物合成的影响。2. 在绝对体外条件下，二琥珀酸半酯水飞蓟宾依其浓度抑制胆固醇的生物合成。对于[1-14C]-乙酸盐或[2-14C]-甲羟戊酸，50%抑制所需的水飞蓟宾浓度分别为0.37 mM或0.40 mM。3. 静脉注射150.6 mg二琥珀酸半酯水飞蓟宾/kg 30分钟后，与对照组相比，用两种前体物质在体外研究的胆固醇生物合成减少。静脉注射水飞蓟宾60分钟或24小时后，未观察到对胆固醇体外生物合成的影响。
