Ethanolic and aqueous extracts of the leaves and flowers of Alstonia scholaris were evaluated for their antioxidant activity by investigating their effect on blood glutathione levels in alloxan-induced diabetic rats. The ethanolic extract of the leaves was the most active; therefore, its cytotoxicity against HepG2 cells was also tested. Promising GI₅₀ values of 1.96, 4.34 and 4.65 µg mL⁻¹ were observed for the extract, its chloroform and ethyl acetate fractions, respectively. The chloroform active subfraction I (GI₅₀ = 2.97 µg mL⁻¹) yielded betulin (1), betulinic acid (2) and ursolic acid (3) upon purification. Compounds 1-3 were identified using spectroscopic techniques and by comparison with reported data. GLC of unsaponifiable and saponifiable fractions of the hexane extract revealed β-sitosterol (7.37%) and n-tetracosane (54.4%) to be the major sterol and hydrocarbon components, respectively. Linoleic acid (48.89%) was the predominant fatty acid.