A novel long acting DPP-IV inhibitor PKF-275-055 stimulates β-cell proliferation resulting in improved glucose homeostasis in diabetic rats

Vildagliptin selectively ameliorates GLP-1, GLUT4, SREBP-1c mRNA levels and stimulates β-Cell proliferation resulting in improved glucose homeostasis in rats with streptozotocin-induced diabetes

“…In this model, overt hyperglycemia results from a combination of insulin resistance and defects in insulin secretion induced by single dose STZ treatment (Arulmozhi, Veeranjaneyulu, & Bodhankar, 2004). Although, we discovered previously the glucose lowering and beta cell-preserving capacity of Vildagliptin (Akarte, Srinivasan, & Gandhi, 2012), but in the current study we showed effect of vildagliptin beyond its glycemic regulation. In addition, we have studied the effect of a prolonged treatment with vildagliptin on GLP-1 mRNA expression in the pancreas, GLUT2 protein and SREBP1c mRNA expression in the liver, and GLUT4 protein and mRNA expression in skeletal muscle in n2-STZ model of diabetes mellitus.…”

Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists

“…Male C57BL/6 mice were concurrently dosed with DPP-IV inhibitor (S)-1-(2-(adamantan-2-ylamino)acetyl)pyrrolidine-2-carbonitrile 24 and the indicated compound. Animals were challenged after 1 h with a glucose bolus (3 g/kg, po), and active GLP-1 levels were measured 30 min later.…”

Sitagliptin alleviated myocardial remodeling of the left ventricle and improved cardiac diastolic dysfunction in diabetic rats

“…Sitagliptin is a dipeptidyl peptidase IV (DPP-Ⅳ) inhibitor and has a role in improving the activity of glucagon-like peptide-1 (GLP-1) (9), an incretin hormone secreted from the distal intestine L cells with glucose-dependent release that promotes the secretion of postprandial insulin (10). GLP-1 receptors (GLP-1Rs) exist widely in islets, myocardium and brain tissue.…”