Background Innula cappa (Buch.-Ham. ex D. Don) DC (Compositae) is used in folkloric medicine to treat diabetes and other ailments. The current study aimed to assess the anti-hyperglycemic and antioxidant effects of methanolic extract and solvent fractions of I. cappa leaves as well as bioassay guided isolation of active compounds from the active extract. Method The α-amylase and α-glucosidase inhibition of the extracts was evaluated by colorimetric assays, and the anti-diabetic activity was tested on alloxan-induced diabetic mice model. Moreover, flame emission and atomic absorption spectrometry techniques were employed to analyze the chemical composition of the plant. Compounds were identified and isolated from the leaf latex of I. cappa using FTIR, GCMS, silica gel column chromatography, and their structures were determined using 1H-NMR, 13C-NMR, and ESI-MS spectral data. Results The results showed that the ME showed significant α-amylase, α-glucosidase inhibitory hyperglycemic activities, significantly improving body weight, glucose tolerance, lipid profiles, and hematological markers. The UV-FTIR spectra revealed diagnostic peaks corresponding to several functional groups whereas GC-MS spectral analysis revealed 35 phytochemical components with different retention times in the ME of I. cappa. Spectroscopic isolation of the ME led to the isolation 5 compounds including ursolic acid, benzoic acid, 2-hydroxybenzoic acid, stigmasterol and β -sitosterol. Conclusion ME exert significant antihyperglycemic and antioxidant effects demonstrating the medicinal value of I. cappa and emphasize its significance as unexplored natural reservoirs of phytogenic chemicals that require further investigation using cutting-edge analytical techniques.