Weitz-Schmidt Gabriele
Novartis Pharma AG, Preclinical Research, Basel, Switzerland.
Trends Pharmacol Sci. 2002 Oct;23(10):482-6. doi: 10.1016/s0165-6147(02)02077-1.
The beneficial effects of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) in cardiovascular disease have generally been attributed to their cholesterol-lowering property. However, an increasing number of in vitro and in vivo studies indicate that statins have direct anti-inflammatory effects that are not mediated by their hypocholesterolemic activity. In this article, the HMG-CoA-reductase-dependent and -independent mechanisms by which statins might affect leukocyte adhesion and migration to sites of inflammation are reviewed and the implications for the design of new statin-derived drugs are discussed.
3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂(他汀类药物)在心血管疾病中的有益作用通常归因于其降低胆固醇的特性。然而,越来越多的体外和体内研究表明,他汀类药物具有直接的抗炎作用,这种作用并非由其降胆固醇活性介导。在本文中,我们综述了他汀类药物可能影响白细胞黏附及向炎症部位迁移的HMG-CoA还原酶依赖性和非依赖性机制,并讨论了其对新型他汀类衍生药物设计的意义。