Objective: This study characterizes the isolated compounds from the aerial parts of A. pilosa and evaluates their PTP1B and a-glucosidase inhibitory properties. Materials and methods: Ethanol extract of A. pilosa was found to inhibit 64% PTP1B activity at 30 mg/mL. The ethanol extract was partitioned with methylene chloride, ethyl acetate, n-butanol, and water fractions. Among these, the ethyl acetate fraction displayed the most potent PTP1B activity. The ethyl acetate extract was separated by chromatographic methods to obtain flavonoids and triterpenoids (1-11); which were evaluated for their inhibitory effects on PTP1B activity with p-nitrophenyl phosphate (p-NPP) as a substrate, and also a-glucosidase enzyme. Results: Compounds 1-11 were identified as apigenin-ursolic acid, tormentic acid, methyl 2-hydroxyl tricosanoate, and palmitic acid. Compounds 8, 9, and 11 displayed inhibitory effects on PTP1B activity with IC 50 values of 3.47 ± 0.02, 0.50 ± 0.06, and 0.10 ± 0.03 mM, respectively. Compounds 3, 4, 6, and 9 exhibited inhibition of the a-glucosidase activity with IC 50 values of 11.2 ± 0.2, 29.6 ± 0.9, 28.5 ± 0.1, and 23.8 ± 0.4 mM, respectively. Discussion and conclusion: As major ingredients of A. pilosa, compounds 1, 6, 8, and 9 showed the greatest inhibitory potency on PTP1B activity. Compounds 3, 6, 8, and 9 also showed potent inhibitory effects on a-glucosidase enzyme. This result suggested the potential of these compounds for developing antidiabetic agents.