Background: The increasing frequency of diabetes patients and the reported side effects of commercially available anti-hyperglycemic drugs have gathered the attention of researchers towards the search for new therapeutic approaches. Inhibition of activities of carbohydrate hydrolyzing enzymes is one of the approaches to reduce postprandial hyperglycemia by delaying digestion and absorption of carbohydrates. Objectives: The objective of the study was to investigate phytochemicals, antioxidants, digestive enzymes inhibitory effect, and molecular docking of potent extract. Materials and Methods: In this study, we carry out the substratebased α-glucosidase and α-amylase inhibitory activity of Asparagus racemosus, Bergenia ciliata, Calotropis gigantea, Mimosa pudica, Phyllanthus emblica, and Solanum nigrum along with the determination of total phenolic and flavonoids contents. Likewise, the antioxidant activity was evaluated by measuring the scavenging of DPPH radical. Additionally, antibacterial activity was also studied by Agar well diffusion method. Molecular docking of bioactive compounds from B. ciliata was performed via AutoDock vina. Results: B. ciliata, M. pudica, and P. emblica exhibit significant inhibitory activity against the α-glucosidase and α-amylase with IC50 (μg/ml) of (2.24 ± 0.01, 46.19 ± 1.06), (35.73 ± 0.65, 99.93 ± 0.9) and (8.12 ± 0.29, no significant activity) respectively indicating a good source for isolating a potential drug candidate for diabetes. These plant extracts also showed significant antioxidant activity with the IC50 ranges from 13.2 to 26.5 μg/mL along with the significant antibacterial activity towards Staphylococcus aureus and Klebsiella pneumonia. Conclusion: Bergenia extract appeared to be a potent α-glucosidase and α-amylase inhibitor. Further research should be carried out to characterize inhibitor compounds.