The chemical constituents and antimalarial activity of Oxytropis kansuensis Bunge from the alpine region were studied. The compounds were separated and purified by a series of chromatographic techniques, including silica gel chromatography, D101 macroporous resin, and Sephadex LH-20 column chromatography. The structures of the compounds were identified on the basis of physicochemical properties and spectral data, and their antimalarial activities were screened using the SYBR Green I method. Ten compounds were isolated and identified from O. kansuensis, namely β-sitosteryl linolenate (1), lupenone (2), β-sitosterol (3), 9,12,15-octadecatrienoic acid, methyl ester (4), apigenin (5), luteolin (6), 1-O-trans-p-coumaroylglycerol (7), 1-O-p-coumaroyl-3-O-feruloylglycerol (8), daucosterol (9), and andcosmosiin (10). Compound 1 was reported for the first time as a natural product, and its NMR data was also reported for the first time. Compounds 2, 4-8 and 10 were isolated from O. kansuensis for the first time, and compounds 1, 4-6, 8 and 10 showed antimalarial activity against Plasmodium falciparum strain 3D7.