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近年来,新型抗糖尿病药物二肽基肽酶Ⅳ(DPP-4)抑制剂的多重性作用获得了越来越多的关注.除了降低血糖,改善胰岛素抵抗等作用以外,DPP-4抑制剂在心脏保护、血管再生、造血恢复、抑制炎症反应等方面也表现出了重要作用.这些作用主要通过调节DPP-4广泛存在的底物来实现的,如:胰高血糖素样肽1(GLP-1)、基质细胞衍生因子1α(SDF-1α)、血管内皮生长因子(VEGF)、高迁移率族蛋白B1(HMGB1)等.关于DPP-4抑制剂对心血管疾病的保护作用已有较多的相关报道.本文首次重点关注DPP-4及其抑制剂在促进血管再生方面的作用及相关机制,为将来更好的认识该类药物打下基础.“,”Recently,a new class of antidiabetic drugs,dipeptidyl peptidase-Ⅳ (DPP-4) inhibitors,has gained considerable interest in different fields.In addition to lower glucose and improve insulin resistance,DPP-4 inhibitors have exhibited pleiotropic effects,including cardioprotection,angiogenesis,hematopoiesis recovery and inflammation inhibition via the regulation of the substrates,such as glucagon-likepeptide-1 (GLP-1),stromal cell-derived factor-1et (SDF-1α),vascular endothelial growth factor (VEGF) and high mobility group box 1 (HMGB1) etc.The role of DPP-4 in cardiovascular disease has been fully reported by previous studies,so the goal of this review is focused on the function and mechanism of DPP-4 and its inhibitors in vascular regeneration,and developing a better understanding of the drugs.