Hughes A D
Department of Clinical Pharmacology, Imperial School of Science, Technology & Medicine, Paddington, London, UK.
J Hum Hypertens. 1996 Jun;10(6):387-90.
Elevated plasma cholesterol is a well recognised risk factor for cardiovascular disease. Numerous studies have shown that a reduction in circulating cholesterol results in a reduced cardiovascular risk. The statins are a group of cholesterol lowering agents which act by inhibition of a key enzyme in cholesterol synthesis; 3-hydroxy 3-methyliglutaryl coenzyme A (HMG CoA) reductase. This enzyme is responsible for the conversion of HMG CoA to mevalonate. In addition to their efficacy as cholesterol lowering agents, statins inhibit the proliferation, migration and signalling of vascular smooth muscle cells. Inhibition of isoprenoid synthesis and resultant reduction in prenylation of key cellular proteins such members of p21ras and p21rho families may underlie some of these effects.
血浆胆固醇升高是公认的心血管疾病危险因素。大量研究表明,循环胆固醇水平降低会降低心血管疾病风险。他汀类药物是一类降胆固醇药物,其作用机制是抑制胆固醇合成中的一种关键酶,即3-羟基-3-甲基戊二酰辅酶A(HMG CoA)还原酶。该酶负责将HMG CoA转化为甲羟戊酸。除了作为降胆固醇药物的功效外,他汀类药物还能抑制血管平滑肌细胞的增殖、迁移和信号传导。抑制类异戊二烯合成以及由此导致关键细胞蛋白(如p21ras和p21rho家族成员)的异戊二烯化减少可能是这些作用的部分原因。