Ursolic acid with large amount (0.67% of dried plant weight) along with 7 compounds, namely as spatozoate (1), kaurenoic acid (2), ursonic acid (3), 3-hydroxy-11-ursen-28,13-olide (4), ursolic acid (5), vindoline (6) and mixture of beta-sitosterol and stigmasterol were isolated from dichloromethane and ethyl acetate extracts which have shown anti-glucosidase activity of the whole plant of C.roseus. Some isolated compounds and their derivatives were also tested for anti-glucosidase and cytotoxicity. Ursolic acid was examined for hypoglycemic activity in alloxan-induced diabetic mice with dose of 200 and 300 mg/kg/day, respectively. The results have shown that the blood glucose level were reduced by 45.75% and 51.31% to compare with the control group. This study has confirmed that the main component of Vietnamese C. roseus has had significant anti-hyperglycemia activity.