Description
Sitagliptin is an anti-diabetic/anti-hyperglycemic compound that inhibits dipeptidyl peptidase 4 (DPP4); sitagliptin also exhibits antioxidative and cardioprotective benefit. Sitagliptin decreases release of lactate dehydrogenase, malondialdehyde, and creatine kinase MB, and increases levels of glutathione peroxidase, glucagon-like peptide 1 (GLP-1), and superoxide dismutase; this compound also decreases expression of caspases 3 and 9, causing decreases in cardiac apoptosis and improvements in cardiac function. In hypertensive rats, sitagliptin increases levels of GLP-1, the GLP-1 receptor, cAMP, and eNOS and also increases activation of AMPK, improving vascular endothelial function.
References
Chang G, Zhang P, Ye L, et al. Protective effects of sitagliptin on myocardial injury and cardiac function in an ischemia/reperfusion rat model. Eur J Pharmacol. 2013 Oct 15;718(1-3):105-13. PMID: 24041927.
Kubota Y, Miyamoto M, Takagi G, et al. The dipeptidyl peptidase-4 inhibitor sitagliptin improves vascular endothelial function in type 2 diabetes. J Korean Med Sci. 2012 Nov;27(11):1364-70. PMID: 23166419.
Liu L, Liu J, Wong WT, et al. Dipeptidyl peptidase 4 inhibitor sitagliptin protects endothelial function in hypertension through a glucagon-like peptide 1-dependent mechanism. Hypertension. 2012 Sep;60(3):833-41. PMID: 22868389.
Waget A, Cabou C, Masseboeuf M, et al. Physiological and pharmacological mechanisms through which the DPP-4 inhibitor sitagliptin regulates glycemia in mice. Endocrinology. 2011 Aug;152(8):3018-29. PMID: 21673098.
