抗高脂血症新靶点与新药研发.pdfVIP

PROGRESS IN PHARMACEUTICAL SCIENCES 2017,41 1 :56-64 56 ( ) 抗高脂血症：新靶点与新药研发 1 1 2 1 1 * 阮文臣 ，张天宁 ，李佳 ，张陆勇 ，庞涛 （1. 中国药科大学江苏省新药筛选重点实验室，天然药物活性组分与药效国家重点实验室，江苏 南京 210009; 2. 中国科学院上海药物研究所 国家新药筛选中心，上海 201203） [ 摘要 ] 高脂血症是引发各种心脑血管疾病最主要的因素之一，通过调节血脂来降低心脑血管疾病的发生率，具有重大意义。从调控内 源性脂质合成、外源性脂质吸收与胆汁酸重吸收、血浆脂蛋白代谢以及脂质代谢等 4 个方面出发，系统概述抗高脂血症的新靶点与新药 研究进展，旨在为高脂血症的治疗药物开发提供参考。 [ 关键词 ] 高脂血症；胆固醇；三酰甘油；脂质代谢；药物靶点；新药研发 [ 中图分类号 ] R972.6 [ 文献标志码 ] A [ 文章编号 ] 1001-5094（2017）01-0056-09 Anti-hyperlipidemia: New Targets and New Drugs 1 1 2 1 1 RUAN Wenchen , ZHANG Tianning , LI Jia , ZHANG Luyong , PANG Tao (1. Jiangsu Key Laboratory of Drug Screening, State Key Laboratory of Natural Medicines, Nanjing 210009, China; 2. National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China) [Abstract] Hyperlipidemia is one of the major factors causing various cardio-cerebrovascular diseases(CCVD). As a result, it is of great significance to reduce CCVD incidence by regulating blood lipid. In this paper, the research progress in new targets and new drugs against hyperlipidemia was reviewed from four aspects: the regulation of endogenous lipid synthesis, exogenous lipid absorption and bile acid absorption, plasma lipoprotein metabolism and lipid metabolism, in order to provide references for the development of new therapies for hyperlipidemia. [Key words] hyperlipidemia; cholesterol; triglyceride; lipid metabolism; drug target; drug discovery 血脂是对血浆中所含脂类的统称，主要包括三酰 疾病都是导致人类死亡的主要原因。因此，控制血脂 TG TC