Abstract
Vildagliptin is a representative of Dipeptidyl Peptidase-4 (DPP-4) inhibitors, antihyperglycemic drugs, approved for use as monotherapy and combination therapy in type 2 diabetes mellitus. By inhibiting enzymatic decomposition, DPP-4 inhibitors increase the half-life of incretins such as GLP-1 (Glucagon-like peptide-1) and GIP (Gastric inhibitors polypeptide) and prolong their action. Some studies present results suggesting the anti-sclerotic and vasculoprotective effects of vildagliptin reaching beyond glycemic control. Vildagliptin is able to limit inflammation by suppression of the NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) signaling pathway and proinflammatory agents such as TNF-α (tumor necrosis factor α), IL-1β (Interleukin-1β), and IL-8 (Interleukin 8). Moreover, vildagliptin regulates lipid metabolism; attenuates postprandial hypertriglyceridemia; and lowers serum triglycerides, apolipoprotein B, and blood total cholesterol levels. This DPP-4 inhibitor also reduces macrophage foam cell formation, which plays a key role in atheromatous plaque formation and stability. Vildagliptin reduces vascular stiffness via elevation of nitric oxide synthesis, improves vascular relaxation, and results in reduction in both systolic and diastolic blood pressure. Treatment with vildagliptin lowers the level of PAI-1 presenting possible antithrombotic effect. By affecting the endothelium, inflammation, and lipid metabolism, vildagliptin may affect the development of atherosclerosis at its various stages. The article presents a summary of the studies assessing vasculoprotective effects of vildagliptin with special emphasis on atherogenesis.
Highlights
The prevalence of diabetes mellitus type 2 (DM2) is constantly increasing worldwide at an alarming rate
Seo et al (2019) analyzed the molecular mechanisms of vildagliptin-induced vasodilation. They observed that application of the voltage-dependent K+ channel inhibitor or sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA) inhibitor significantly reduced the vasodilatory effects of vildagliptin
The presented results suggest that the benefits of vildagliptin extend far beyond glycemic control
Summary
The prevalence of diabetes mellitus type 2 (DM2) is constantly increasing worldwide at an alarming rate. Vildagliptin is a representative of Dipeptidyl Peptidase-4 (DPP-4) inhibitors which are registered and effectively used in DM2 therapy These class of drugs was designed to increase the half-life of incretins such as GLP-1 (Glucagon-like peptide-1) and GIP (Gastric inhibitors polypeptide) and to prolong their action [3]. Under hyperglycemic state, they stimulate glucose-dependent insulin secretion from pancreatic β-cells and inhibit the secretion of glucagon from α-cells [4]. They stimulate glucose-dependent insulin secretion from pancreatic β-cells and inhibit the secretion of glucagon from α-cells [4] They slow down the rate of absorption of nutrients into the bloodstream by delaying gastric emptying. 2.5 and 5 μM for 24h varied at every stage of the experiment varied at every stage of the experiment varied at every stage of the experiment varied at every stage of the experiment
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