维格列汀通过α细胞和β细胞“双调节”机制改善葡萄糖代谢的研究进展

Research Progress on Vildagliptin Improving Glucose Metabolism with the Two-way Regulatory Effects on the Functions of β and α Cell

维格列汀是一种有效的、具有选择性和可逆性的DPP-4抑制剂,而DPP-4是可致GLP-1和GIP快速失活的酶。GLP-1和GIP增强了胰岛素(β细胞)和胰高血糖素(α细胞)对葡萄糖的敏感性,对维持正常的葡萄糖稳态非常重要。维格列汀显示出了对α细胞和β细胞功能的双向调节作用。在α细胞中,如果葡萄糖水平偏高,GLP-1会减弱胰高血糖素水平,如果葡萄糖水平偏低,GIP会增加胰高血糖素水平。本文综述了维格列汀通过α和β细胞“双调节”机制发挥改善葡萄糖代谢作用的研究进展。

Vildagliptin is a potent, selective and reversible inhibitor of dipeptidyl peptidase-4, the enzyme responsible for rapidinactivation of the incretin hormones glucagon-like peptide-1 and gastric inhibitory polypeptide . GLP-1 and GIP are importantfor the maintenance of normal glucose homeostasis as they enhance the sensitivity of insulin (β cell) and glucagon (α cell)secretion to glucose. Vildagliptin shows the two-way regulatory effects on the functions of α and β cell. Moreover, in the case ofthe α-cell, if glucose levels are high, GLP-1 attenuates the glucagon levels and if glucose levels are low, GIP increases glucagonlevels. This review summarizes the research progress on the two-way regulatory effects on the functions of α and β cell of theVildagliptin to improve glucose metabolism.