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首页> 外文期刊>Clinical and experimental pharmacology & physiology >Effect of epomediol on ethinyloestradiol-induced changes in bile acid and cholesterol metabolism in rats.
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Effect of epomediol on ethinyloestradiol-induced changes in bile acid and cholesterol metabolism in rats.

机译：环氧雌二醇对乙炔雌二醇诱导的大鼠胆汁酸和胆固醇代谢变化的影响。

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1. Epomediol is a terpenoid compound that has been reported to stimulate bile acid synthesis and to reverse 17alpha- ethinyloestradiol-induced cholestasis. The aim of the present study was to investigate the contribution of changes in bile acid and cholesterol metabolism to the protective effects of epomediol in ethinyloestradiol-treated rats. Animals received epomediol for 5 days at 100 mg/kg daily, i.p., ethinyloestradiol for 5 days at 5 mg/kg, s.c., or a combination of both drugs. 2. When compared with control animals, epomediol treatment resulted in a significant increase in bile flow (+42%) and in the secretion of bile acids (+74%) and cholesterol (+42%). Ethinyloestradiol administration caused a significant decrease in bile flow (-43%), bile acid secretion (-37%) and cholesterol secretion (-45%). Bile flow, bile acid secretion and cholesterol secretion were significantly increased in animals receiving ethinyloestradiol plus epomediol compared with ethinyloestradiol-treated rats (+13, +29 and +31%, respectively). 3. Both cholesterol 7alpha-hydroxylase and hydroxy-3- methylglutaryl coenzyme A reductase activities were significantly increased in epomediol-treated rats (+30 and +96%, respectively). Cholesterol 7alpha-hydroxylase activity was significantly reduced by ethinyloestradiol (-22%) and did not differ from control values in animals receiving epomediol plus ethinyloestradiol. Levels of cholesterol 7alpha-hydroxylase mRNA were elevated (+41%) by epomediol, but were not significantly modified by ethinyloestradiol or ethinyloestradiol plus epomediol. 4. It is concluded that epomediol enhances bile acid secretion by increasing the expression of cholesterol 7alpha-hydroxylase. Changes in bile acid metabolism contribute to the effects of epomediol in rats with ethinyloestradiol-induced cholestasis.
机译：1.环氧丙二醇是一种萜类化合物，据报道可刺激胆汁酸合成并逆转17α-乙炔炔雌二醇引起的胆汁淤积。本研究的目的是研究胆汁酸和胆固醇代谢变化对乙炔雌二醇治疗的大鼠中环氧雌二醇的保护作用的贡献。动物以每天100 mg / kg的剂量接受epomediol 5天，即皮下注射乙炔雌二醇5毫克/ kg的5天，或两种药物的组合。 2.与对照组动物相比，艾美糖醇治疗可显着增加胆汁流量（+ 42％），并增加胆汁酸（+ 74％）和胆固醇（+ 42％）的分泌。乙炔雌二醇的给药导致胆汁流量（-43％），胆汁酸分泌（-37％）和胆固醇分泌（-45％）显着下降。与经乙炔雌二醇治疗的大鼠相比，接受乙炔雌二醇加环氧雌二醇的动物的胆汁流量，胆汁酸分泌和胆固醇分泌显着增加（分别为+13％，+ 29％和+ 31％）。 3.在接受环戊二醇治疗的大鼠中，胆固醇7α-羟化酶和羟-3-甲基戊二酰辅酶A还原酶活性均显着增加（分别为+30和+ 96％）。乙炔雌二醇（-22％）显着降低了胆固醇7α-羟化酶的活性，与接受庚二醇和乙炔雌二醇的动物的胆固醇值没有差异。环氧雌二醇可提高胆固醇7α-羟化酶mRNA的水平（+ 41％），但乙炔雌二醇或乙炔雌二醇加环氧雌二醇未对其进行显着修饰。 4.结论是，环氧雌二醇通过增加胆固醇7α-羟化酶的表达来增强胆汁酸的分泌。胆汁酸代谢的变化有助于乙炔雌二醇诱发的胆汁淤积大鼠中的环氧乙烷的影响。

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