The current work is aimed to preliminary screen and characterize the bioactive fractions and compounds of local medicinal plants whichcould be responsible for the hypoglycemic activities. For this purpose, the endemic medicinal plants will be collected and processed for activity-guided isolation. Several chromatographic techniques will be used for the activity guided isolation and purification of individual compound, the purified compounds will be thoroughly characterized by UV, NMR, FTIR, EIMS, HREIMS and their chemical structures will be determined. Enzymes inhibitory activities of the fractions and purified compounds will be evaluated and their relevant IC₅₀ values, dose-dependent inhibition, mode of inhibition, and kinetic analysis will be determined. The ligand-receptor interaction, binding affinities & energies will be evaluated by molecular docking simulation. The successful completion of this work will help to discover the responsible lead structures from endemic medicinal plants and would contribute to the ongoing efforts of drug discovery and treatment of diabetes.