二肽基肽酶Ⅳ抑制剂的研究进展  

Recent progress in research and development of dipeptidyl peptidase IV inhibitors

作　　者：李祎亮[1,2] 王菊仙[1] 吴香玫[1] 邹美香[2] 李卓荣[1] 王玉成[1] 

机构地区：[1]中国医学科学院,北京协和医学院医药生物技术研究所,北京100050 [2]天津药物研究院,天津300193

出　　处：《中国新药杂志》2008年第20期1739-1745,共7页Chinese Journal of New Drugs

基　　金：中央级公益性科研院所基本科研业务专项资金(IMBF-20060403)

摘　　要：胰高血糖素样肽-1(GLP-1)是一种肠促胰岛素,它通过刺激和保护胰岛β细胞,促进胰岛素的合成和分泌,降低餐后血糖。二肽基肽酶Ⅳ(DPP-IV)抑制剂能增强GLP-1的活性,降低2型糖尿病患者的高血糖症状,是一类新型的抗糖尿病治疗药物。临床研究表明DPP-IV单用或与二甲双胍、吡格列酮合用都有明显的降血糖作用,具有治疗效果显著、服用安全,耐受性好,不良反应少等特点,近年来已经成为糖尿病药物研究开发的热点。文中就其作用机制、国内外开发现状、构效关系及研究进展等进行综述。Glucagon-like peptide-1 （GLP-1） is an intestine-derived insulinotropic hormone that stimulates glucose dependent insulin production and secretion from pancreatic β-cells. GLP-1 also exerts cytoprotective and antiapoptotic effects on β-cells, and decreases postprandial blood glucose via complicated mechanisms. Dipeptidyl peptidase Ⅳ （DPP-Ⅳ） inhibitors, a novel type of antidiabetic agents, can enhance GLP-1 bioactivity and decrease the high levels of blood glucose in type 2 diabetes patients. These inhibitors have been proved as an orally active and safe agent for the treatment of type 2 diabetes. Monotherapy or combination with metformin or pioglitazone is efficacious, well tolerated, and safe in clinical application. The mechanism, development, structure-activity relationship, and progress of dipeptidyl peptidase Ⅳ inhibitors were reviewed in this paper.

关 键 词：二肽基肽酶Ⅳ抑制剂 2型糖尿病 胰高血糖样肽-1 

分 类 号：R977.15[医药卫生—药品] R914.5[医药卫生—药学]