The present research study was entitled focused on the importance of crude plant extract as promising treatments. In continuation, the active component responsible for medicinal properties from this plant were isolated and assessed for its mechanism by α-glucosidase and DPP IV inhibitory activity. In-vivo toxicity studies and pharmacological activity of extract and isolated compounds were carried out and compared with standard drugs; sitagliptin and miglitol. Experimental work performed in this thesis consists of four parts. The first part dealt with phytochemical evaluation and isolation of active constituents. In second part, the in-vitro enzyme inhibitory activity was carried out and third part involves toxicity assessments of the plant and isolated compounds. Final part dealt with in-vivo efficacy of extract and potent isolated compounds in HFD fed and low STZ induced type 2 DM model. Qualitative phytochemical analysis have shown the presence of flavonoids, tannins, phenolic compound, triterpenoids, glycosides and absence of alkaloids, saponins, steroids and anthraquinone glycosides. Total phenolic content was almost double to the total flavonoid contents. Both these contents were found higher in the methano l extract than aqueous and hydroalcoholic extract. Conclusively, isolated compounds hirtacoumaroflavonoside (HCF) and hirtaflavonoside- A (HFA) and extract as such could be a potential agent for treating diabetes and diabetic dyslipidemia. In addition, they have showed in-vitro enzyme inhibition. Moreover they demonstrated better safety profile. These compounds can be further taken up for the detailed pharmacokinetic (PK) study, pharmacokinetic (PK) and pharmacodynamic (PD) correlation and toxicological studies. If aforementioned experiments provide promising results, preclinical to clinical translation of isolated compounds hirtacoumaroflavonoside (HCF) and hirtaflavonoside-A (HFA) and extract in diabetes is possible. Key words: Glibenclamide, Antihyperlipidemic, Euphorbia hirta, Streptozotocin.