The present investigation is aimed at screening the bioactive compounds present in the leaves of Pergularia tomentosa L. an important ethnomedicinal plant. The qualitative analysis for the present phytochemicals was performed using MeOH/H2O extracts. Phytochemical analysis showed the existence of some primary and secondary metabolites, phenolic, flavonoids, cardenolides, tannins, alkaloids, quinones, terpenoids and glycoside; leaves contained the highest amounts of all these compounds. The highest total phenolic content and total tannins was observed in aqueous extract which is 2.59±0.49 mg GAE/g DW and 0.436±0.00 mg CE/g DW respectively. In addition, the highest total flavonoid content was observed in butanol extract which is 0.486±0.01mg QE/g DW. Reducing power assay and DPPH were employed to measure antioxidant activity in vitro, extracts were the most powerful antioxidants for the two-assay in vitro system. In addition, we investigated in vitro anti-diabetic activity of different extracts. The dichloromethane extract of Pergularia tomentosa L. showed strong antidiabetic antidiabetic activity.