Pharmacology and Ethnopharmacology

Biography

Biography: Yu-Sheng Liu

Abstract

OBJECTIVE Sitagliptin as one of DPP-Ⅳ inhibitors plays its biological role via improving the serum levels of GLP-1. Hence, we sought to determine the effects of sitagliptin on myocardial inflammation, collagen metabolism, lipids content and myocardial apoptosis in diabetic rats. METHODS The type 2 diabetic models were induced by small dosage streptozotocin on the basis of high-fat diet. The characteristics of the diabetic rats were evaluated by ECG, echocardiography and blood analysis. Cardiac inflammation, fibrosis, cardiomyocyte density, lipids accumulation, and RIP3 related to apoptosis were detected by histopathologic analysis, RT-PCR and Western-blot analysis to evaluate the effects of sitagliptin on myocardial remodeling of left ventricle. RESULTS Myocardial hypertrophy or apoptosis, inflammation, lipids accumulation, myocardial fibrosis, elevated collagen contents, RIP3 overexpression, and left ventricular dysfunction were detected in diabetic rats. Furthermore, sitagliptin could down-regulate the overexpression of RIP3 and alleviate cellular apoptosis in the myocardial tissues. Sitagliptin could significantly improve left ventricular systolic pressure (LVSP), +dp/dt max, reduce the E/E＇ratio, left ventricular end diastolic pressure (LVEDP), -dp/dt max and Tau in diabetic rats. CONCLUSIONS Sitagliptin might exert a myocardial protective effect by inhibiting apoptosis, inflammation, lipids accumulation and myocardial fibrosis, implicating its potential role for the improvement of left ventricular function.