Dushkin M I, Ivanova M V
Ukr Biokhim Zh (1978). 1992 May-Jun;64(3):73-6.
Ketoconazole in vivo has been studied for its effect on the activity of key enzymes of the cholesterol and its esters' biosynthesis in the liver and on the cholesterol concentration in certain fractions of blood lipoproteins in normal and cholesterol-fed rats. It is established that ketoconazole decreases cholesterol concentration in low-density lipoproteins and in very low-density lipoproteins as well as decrease the acyl-CoA-cholesterol acyl-transferase activity and increases the 3-hydroxy-3-methyl-glutaryl-CoA-reductase activity in the liver microsomes of intact and test animals. It is supposed that the possible cause of the observed changes can be a disturbance in regulation of basic links of cholesterol metabolism in the liver.
已对酮康唑在体内对正常大鼠和喂食胆固醇大鼠肝脏中胆固醇及其酯生物合成关键酶活性以及某些血液脂蛋白组分中胆固醇浓度的影响进行了研究。已确定酮康唑可降低低密度脂蛋白和极低密度脂蛋白中的胆固醇浓度,降低酰基辅酶A胆固醇酰基转移酶活性,并增加完整动物和试验动物肝脏微粒体中3-羟基-3-甲基戊二酰辅酶A还原酶活性。据推测,观察到的变化的可能原因可能是肝脏中胆固醇代谢基本环节的调节紊乱。