Solanum procumbens called ``Cà gai leo'' in Vietnam, belonged to the family of Solanaceae, which is a prickly diffuse, bright green perennial shrub, woody at the base. This plant has been sought for plenty of Vietnamese folk remedies for diseases such as rheumatism, back pain, detoxification, cough, pain relief, hemostasis, hepatitis, and cirrhosis. Chemical reports revealed the presence of lots of secondary metabolites such as steroids, triterpenoids, alkaloids, and phenolic compounds that have good biological activities such as antibacterial, antidiabetic, antioxidant, and antimicrobial... By column chromatography method together with thin layer normal-phase chromatography on the ethyl acetate extract of its entire plant, we isolated four compounds including dioscin (1), b -sitosterol (2), daucosterol (3) and 6'-O-acetyl-b -daucosterol (4). The result of theira-glucosidase inhibitory activity showed that compounds 2 and 4 had strong inhibition with IC50 values of 35.2 and 209.5 mM, comparing to the positive control, acarbose with an IC50 value of 214.5 mM. The results of this study have contributed to the scientific data of chemical compositions of Vietnamese medicinal plants, among them S. procumbens would potentially be developed as a plant-based drug to decrease the blood glucose level.