DPP-4抑制剂的作用机制及在2型糖尿病治疗中的应用

α及母细胞功能障碍在2型糖尿病的发生中发挥重要作用.二肽基肽酶4( DPP-4)抑制剂是一类基于肠促胰素的新型的口服降糖药物,通过增加内源性活性胰升糖素样肽-1( GLP-1)及葡萄糖依赖性促胰岛素分泌多肽(GIP)水平改善α及β细胞功能障碍,表现为α及β细胞对葡萄糖的敏感性增加,葡萄糖依赖性地促进胰岛素分泌并抑制胰升糖素分泌.同时还具有增加胰岛素敏感性及调节血脂代谢等胰腺外作用.并具有较少发生低血糖,对体重的影响中性,不影响胃排空等特点.临床研究证实其无论单药还是与其他药物联合使用均具有较高的有效性及良好的安全性和耐受性.

The mechanism of the action of dipeptidyl peptidase-4 inhibitors and its use in type 2 diabetes

The critical role of α- and β-cell dysfunction in the development of type 2 diabetes has been established.Dipeptidyl peptidase-4 (DPP-4) inhibitors are new class of oral anti-hyperglycemia agents that acts to increase active levels of the incretin hormone glucagon-like peptide-1 ( GLP-1 ) and glucose-dependent insulinotropic polypeptide ( GIP),which improved α- and β-cell function.This action is shown as improved α- and β-cell sensitivity to glucose,increased glucose-dependent insulin secretion and decreased glucagon secretion.DPP-4 inhibitors treatment has also been associated with beneficial extrapancreatic effects,including improved peripheral insulin sensitivity and lipid metabolism.Additionally,DPP-4 inhibitors have shown a minimal risk of hypoglycemia and bodyweight neutrality without effects on gastric emptying.Numerous clinical trials have verified the favorable efficacy,safety,and tolerability of DPP-4 inhibitors treatment in monotherapy or combination with other anti-diabetic agents for patients with type 2 diabetes.