PS 16-29 GLP-1 RECEPTOR AGONISTIC AND ANTIDIABETIC ACTIVITY OF MEFLOQUINE AGAINST STZ-NA INDUCED DIABETES IN ALBINO WISTAR RATS

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Abstract

Objective:

Mefloquine was retrieved as structurally similar drug molecule to liraglutide with significant binding efficacy towards glucagon like peptide-1 receptor (GLP-1R) and thereby evaluated for its antidiabetic potential.

Design and method:

Non-insulin dependent diabetes mellitus was induced in the overnight fasted experimental animals (100–120 gm) by a single intraperitoneal injection of 60 mg/kg STZ followed by NA (120mg/kg, i.p.). The diabetic animals were randomised and divided into five groups of six animals each, and subjected to the treatment as specified in Table 1 for 12 days. The animals were scrutinized for the paradigms of electrocardiographic and heart rate variability (HRV) on 11th day. The animals were sacrificed by cervical dislocation under light ether anesthesia. Pancreatic and liver tissues were collected for further biochemical estimation.

Results:

Mefloquine demonstrated significant efficacy towards restoring the blood glucose, insulin and distorted lipid profile in the animals treated with STZ-NA. Mefloquine also regulated the inflammatory (COX, LOX and NO) and oxidative stress (TBARs, SOD, catalase, GSH and protein carbonyl) markers in the pancreatic tissue of the STZ-NA treated animals. When scrutinized on the grounds electrocardiographic and heart rate variability (HRV) changes, mefloquine decreased the heart rate, without much affecting the QRS, QT and QTc interval. In the same line, HRV analysis revealed increase in the LF/HF suggesting sympathetic predominance in the diabetic animals, which was very well restored by the mefloquine. Mefloquine was also evident to be less hepatotoxic in comparison to the standard metformin, providing an added advantage as an antidiabetic agent.

Conclusions:

The study concluded that the low dose of metformin can favorably regulate of the blood glucose and other biochemical paradigms in comparison to high dose of metformin.

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