This study aims to investigate the chemical constituents and anti-inflammatory activities of Angelicae Sinensis Radix. Compounds from the ethyl acetate of Angelicae Sinensis Radix were isolated by various chromatography techniques like silica gel column chromatography, Sephadex LH-20 gel column chromatography, and semi-preparative HPLC, etc. Their structures were identified by spectral data such as NMR and MS. Twenty compounds were isolated and identified as psoralen (1), xanthotoxin (2), isopimpinellin (3), bergapten (4), umbelliferine (5), scopoletin (6), 6-hydroxy-7,8-dimethoxycoumarin (7), nepetoidin F (8), 1-(4-hydroxy-3-methoxy)-benzene-1, 2, 3-glycerol (9), farrerol (10), vanillin (11), vanillic acid (12), ethyl 4-[2-formyl-(5-(ethoxymethyl)-1H-pyrrol-1-yl)] butanoate (13), indole-3-carboxaldehyde (14), maltol (15), 5-hydroxymaltol (16), 4-hydroxy-5-methyl-furan-3-carboxylic acid (17), 5-methylfurfural (18), β-sitosterol (19), daucosterol (20). Compounds 3, 7, 8, 10, 13, 14 and 16 were isolated from A. sinensis for the first time, and compounds 8, 10, and 13 were also isolated from the genus Angelica for the first time. The results of in vitro anti-inflammatory activities showed that compounds 10, 11, 13 and 16 reduced the release of NO. At the same concentration (20 µmol/L), the inhibition rates of compounds 11, 13, and 16 on NO production were 37.06% ± 4.57%, 28.13% ± 2.11%, and 34.33% ± 2.64%, respectively, which were superior to the inhibitory effect of the positive drug (dexamethasone) on NO production.