Department of Cardiology, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Centre for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, 167 Beilishi Road, Xicheng District, Beijing 100037, People's Republic of China.
Cardiovasc Drugs Ther. 2013 Aug;27(4):297-307. doi: 10.1007/s10557-013-6459-8.
Dipeptidyl peptidase-4 (DPP-4 or CD26) inhibitors, a new class of oral anti-hyperglycemic agents that prolong the bioavailability of the endogenously secreted incretin hormone glucagon-like peptide-1 (GLP-1) and the glucose-dependent insulinotropic polypeptide (GIP), are effective in the treatment of diabetes. Accumulating data have indicated that DPP-4 inhibitors play important protective roles in the cardiovascular system. DPP-4 inhibitors act to decrease myocardial infarct size, stabilize the cardiac electrophysiological state during myocardial ischemia, reduce ischemia/reperfusion injury, and prevent left ventricular remodeling after myocardial infarction. Moreover, DPP-4 inhibitors can mobilize stem/progenitor cells to move to sites of cardiovascular injury, thus further promoting tissue repair. In addition, DPP-4 inhibitors not only improve myocardial metabolism but also regulate cardioactive peptides. DPP-4 inhibitors can also protect the vasculature through their anti-inflammatory and anti-atherosclerotic effects and through the ability of the inhibitors to promote vascular relaxation. Finally, the potential effects of DPP-4 inhibitors on blood pressure and lipid metabolism have also been investigated. However, some reports on the cardioprotective activities of DPP-4 inhibitors are controversial. Herein, we summarize the available data on cardiovascular protection by DPP-4 inhibitors that have emerged in recent years and discuss current position and future perspectives concerning the use of DPP-4 inhibitors in cardiovascular medicine.
二肽基肽酶-4（DPP-4 或 CD26）抑制剂是一类新型的口服抗高血糖药物，可延长内源性分泌的肠促胰岛素激素胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性胰岛素释放肽（GIP）的生物利用度，在糖尿病治疗中有效。越来越多的证据表明，DPP-4 抑制剂在心血管系统中发挥重要的保护作用。DPP-4 抑制剂可减少心肌梗死面积，稳定心肌缺血期间的心脏电生理状态，减少缺血/再灌注损伤，并防止心肌梗死后左心室重构。此外，DPP-4 抑制剂可动员干细胞/祖细胞迁移到心血管损伤部位，从而进一步促进组织修复。此外，DPP-4 抑制剂不仅改善心肌代谢，还调节心活性肽。DPP-4 抑制剂还可以通过抗炎和抗动脉粥样硬化作用以及抑制剂促进血管松弛的能力来保护血管。最后，还研究了 DPP-4 抑制剂对血压和血脂代谢的潜在影响。然而，一些关于 DPP-4 抑制剂的心脏保护活性的报告存在争议。在此，我们总结了近年来出现的 DPP-4 抑制剂在心血管保护方面的可用数据，并讨论了 DPP-4 抑制剂在心血管医学中的应用的当前立场和未来前景。
