Abstract
Linagliptin is a representative of dipeptidyl peptidase 4 (DPP-4) inhibitors which are registered and used effectively in a treatment of diabetes mellitus type 2. They increase the levels of active forms of endogenous incretins such as GLP-1 and GIP by inhibiting their enzymatic decomposition. Scientific reports suggest beneficial effects of linagliptin administration via immunological and biochemical pathways involved in neuroprotective processes of CNS. Linagliptin’s administration leads to a decrease in the concentration of proinflammatory factors such as: TNF-α, IL-6 and increases the number of anti-inflammatory patrolling monocytes CX3CR1bright. Significant reduction in Aβ42 level has been associated with the use of linagliptin implying potential application in Alzheimer’s disease. Linagliptin improved vascular functions by increasing production of nitric oxide (NO) and limiting concentration of apolipoprotein B. Linagliptin-induced decrease in macrophages infiltration may provide improvement in atheromatous plaque stabilization. Premedication with linagliptin increases neuron’s survival after stroke and augments neuronal stem cells proliferation. It seems to be connected with SDF-1α/CXCR4 signaling pathway. Linagliptin prevented abnormal proliferation and migration of rat brain microvascular endothelial cells in a state of hypoperfusion via SIRT1/HIF-1α/VEGF pathway. The article presents a summary of the studies assessing neuroprotective properties of linagliptin with special emphasis on cerebral ischemia, vascular dysfunction and neurodegenerative diseases.
Highlights
A high percentage of the population struggling with cardiovascular diseases imply a substantial need for new therapeutic methods
Recent experimental studies indicate that dipeptidyl peptidase 4 (DPP-4) (Dipeptidyl peptidase 4) inhibitor called linagliptin may possess neuroprotective properties
Unlike the other DPP-4 inhibitors, 85% of the drug is eliminated unchanged in the feces and only 5% is metabolized by the kidneys and excreted in urine so it can be safely used in patients with kidney diseases [9]
Summary
A high percentage of the population struggling with cardiovascular diseases imply a substantial need for new therapeutic methods. Recent experimental studies indicate that DPP-4 (Dipeptidyl peptidase 4) inhibitor called linagliptin may possess neuroprotective properties. They slow down enzymatic degradation of endogenous incretins such as GLP-1 (Glucagon-like peptide-1) and GIP (Gastric inhibitors polypeptide) and prolong their action. GLP-1 and GIP inhibit the secretion of glucagon from pancreatic alpha cells and reduce gluconeogenesis in the liver. They support the biosynthesis of insulin and its release from pancreatic beta cells. Unlike the other DPP-4 inhibitors, 85% of the drug is eliminated unchanged in the feces and only 5% is metabolized by the kidneys and excreted in urine so it can be safely used in patients with kidney diseases [9]. 83 mg/kg for one week, 166mg/kg for three weeks varied at every stage of the experiment
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