新型口服降糖药DPP-4抑制剂:从胰岛α细胞看2型糖尿病治疗的新进展

New anti-diabetic agents-DPP-4 inhibitors:Viewing the advance of treatment for T2DM from pancreatic α-cells

胰岛α细胞分泌的胰升糖素是升高血糖的重要激素之一。GLP-1参与机体血糖的稳态调节,其机制包括抑制胰岛α细胞的胰升糖素分泌。然而,体内的GLP-1极易被DPP-4所降解。DPP-4抑制剂可选择性抑制DPP-4的活性,减少内源性GLP-1的降解,可作为治疗T2DM的一类新型药物。

Glucagon secreted from the pancreatic islet a cells is one of the factors resulting in elevated blood glucose. Glueagon-like peptide-1 （GLP-1） has an important role in the maintenance of blood glucose homeostasis through several mechanisms including inhibition of glucagon secretion from islet a cells. However, endogenous intact GLP-1 is degraded by dipeptidyl peptidease-4 （DPP-4） into inactive forms. DPP-4 inhibitors selectively block the activity of DPP-4 and prevent endogenous GLP-1 from quick inactivation. Therefore, DPP-4 inhibitors have been used as new agents for the treatment of T2DM.