A Study on the Inhibitory Potential of Dpp-Iv Enzyme by Lobeline through In silico and In vivo Approaches

Aims: To evaluate the inhibitory activity of Lobeline natural alkaloid against dipeptidyl peptidase IV (DPP IV) enzyme by in silico and in vivo experiments.

Study Design: Evaluation of Antidiabetic Activity of Lobeline alkaloid.

Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Aleppo University, Aleppo, Syria, between March 2020 and December 2020.

Methodology: in silico study was carried out using iGEM docking software to predict the binding affinity of lobeline with DPP IV enzyme in comparison with the reference synthetic compound Sitagliptin. Then in vivo experiment was performed on HFD/alloxan induced diabetic mice to evaluate the anti hyperglycemic effect of lobeline. After treatment duration of 21 days, FBG and the inhibitory effect on DPP IV enzyme activity were measured.

Results: Lobeline bound efficiently to the active site of DPP IV enzyme and consumed less binding energy than Sitagliptin. This finding was confirmed by the in vivo study.

Administration of lobe line at a dose of 25 mg/kg in HFD/alloxan induced diabetic mice produced a significant reduction in blood glucose level and in DPP IV activity compared to the diabetic control group (P value> .01).

Conclusion: Lobe line could be a good candidate to be developed as a natural compound for treating diabetes mellitus.