Chao Y, Chen J S, Hunt V M, Kuron G W, Karkas J D, Liou R, Alberts A W
Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
Eur J Clin Pharmacol. 1991;40 Suppl 1:S11-4.
Lovastatin and simvastatin are potent competitive inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Key inhibit the synthesis of cholesterol in cultured HepG23 cells, rat hepatocytes and in rats. The primary target organ of cholesterol synthesis inhibition by lovastatin and simvastatin is the liver. Lovastating and simvastatin lower levels of plasma cholesterol in rats, dogs and rabbits by inhibition the endogenous cholesterol synthesis and induction of LDL receptor in the liver.
洛伐他汀和辛伐他汀是3-羟基-3-甲基戊二酰辅酶A还原酶的强效竞争性抑制剂。主要抑制培养的HepG23细胞、大鼠肝细胞以及大鼠体内胆固醇的合成。洛伐他汀和辛伐他汀抑制胆固醇合成的主要靶器官是肝脏。洛伐他汀和辛伐他汀通过抑制内源性胆固醇合成以及诱导肝脏中的低密度脂蛋白受体,降低大鼠、狗和兔子的血浆胆固醇水平。