In the last few decades, natural products from plants have got immense importance in human health due to their therapeutic multi-functionality. They have also been reported to enhance human gut health, another important factor in the overall human health. Diabetes Mellitus Type 2 (DM 2) is now a global concern with 6.28% of the world's population affected by it. Many hypoglycemic drugs currently available in the market are either directly or indirectly based on a number of plant secondary metabolites. In the current study, we aimed to find out the hypoglycemic secondary metabolites from leaf methanolic extract of Argyreia nervosa (Burm. f.) Bojer (Family: Convolvulaceae). In the in vitro experiment, this extract showed good inhibitory activity against Porcine Pancreatic Alpha-amylase (PPA) with IC₅₀ value of 1.1 mg/ml. Presence of Quercetin and Ursolic acid was identified in the leaf methanolic extract with HPTLC, HPLC and MS analysis. The calculated IC₅₀ values against PPA, for standard Quercetin and Ursolic acid were 16.5 µg/ml and 13.2 µg/ml respectively. In silico studies used both of these compounds as ligands against PPA (PDB ID: 1OSE) in AutoDock 4.2.6. Significant binding energies of -9.89 kcal/mol and -8.96 kcal/mol were seen for Quercetin and Ursolic acid respectively; while Acarbose (drug used as positive control) had binding energy of -12.48 kcal/mol. Both Quercetin and Ursolic acid strongly interacted with the pivotal amino acid residues like Glu233, Asp197 and Asp300, present at the active site of PPA, which upholds our in vitro experimental results. Both the compounds have exhibited beneficial effects on human gut health in DM 2 and related complications. Docking results of them with few intestinal markers significant in gut health would also be discussed.