EtOAc and MeOH different extracts of Pimpinella candolleana Wight et Arn. have shown the α-glucosidase inhibitory and antioxidant activities when they were assayed in vitro. Chemical constituents of both extracts were isolated by column chromatography, and identified by MS and NMR spectroscopic data. Nine compounds were isolated, including 3 sterols, 2 flavones, 1 triterpene, 1 glucoside, 1 phenol derivatives, and 1 other compound. Their structures were identified as ursolic acid (1), luteolin (2), urea (3), stigmasta-5,22-dien-3-ol acetate (4), erythrol (5), isovitexin (6), 1-(4-hydroxyphenyl)-1,2-ethanediol (7), daucosterol (8), and β-sitosterol (9). Compound 1 (IC50 = 4.42 μg ml−1), 2 (IC50 = 5.96 μg ml−1), 4 (IC50 = 67.43 μg ml−1) and 6 (IC50 = 68.71 μg ml−1) showed α-glucosidase inhibitory activity. Compound 2 (IC50 = 0.99 μg ml−1) had antioxidant activity. All compounds except for 1 and 9 were isolated from this genus for the first time.