贝特类抗高血脂药物药理活性研究新进展

Research progress of new pharmacological activities antihyperlipidemic fibrates

贝特类药物是典型的过氧化物酶增殖体激活受体α(peroxisome proliferator-activated receptorα,PPARα)的激动剂,其主要作用是增加甘油三酯分解代谢,临床用于治疗高血脂症及抗动脉粥样硬化。近年研究发现,贝特类药除直接调节脂质代谢外,还可通过抗炎和改善内皮功能发挥抗动脉粥样硬化的作用,同时参与血糖、血压及胆汁酸稳态调控,及细胞色素P450酶(cytochrome P450,CYP)和葡萄糖醛酸基转移酶(UDPglucuronosyltrans-ferase,UGT)有关的外源代谢调控。本文旨在查阅近几年国内外相关文献,总结贝特类药物的药理活性研究新进展,为代谢性疾病中使用贝特类药物提供理论依据。

Fibrates belong to a group of ligands for peroxisome proliferator-activated receptor α （PPARα）. Clinically, fibrates represent a class of drugs widely used for the treatment of hypertriglycer- idemia and mixed hyperlipidemia often associated with atherosclerosis. Besides direct regulation of lipid metabolism, fibrates also improve endothelial function and act against inflammation in antiathero- sclerosis according to recent study. Fibrates also participated in regulating glucose, blood pressureand bile acid homeostasis, as well as CYP and UGT mediated exogenous metabolism. In this review, we studied research progress of fibrates＇new pharmacogical activties, trying to lay a good basis for mechanism investigation and therapeutics of metabolic diseases.