This paper studies the chemical constituents of Acanthopanax senticosus Harms and its inhibition of diacylglycerol acyltransferase (DGAT) activity.A. senticosus was extracted with 75% ethanol,and purified by silica gel,ODS and semi-preparative HPLC.The structures of the compounds were identified by physicochemical properties and spectral data.Twelve compounds were identified as erythro-guaiacylglycerol-β-O-4′-dihydroconiferyl alcohol (1),(E)-3-(2,2-dimethyl-2H-chromen-6-yl)prop-2-enal (2),7′E-4,9-dihydroxy-3,3′,5′-trimethoxy-8,4′-oxyneolign-7′-en-9′-al (3),5-methoxydehydroconiferyl alcohol (4),dehydroconiferyl alcohol (5),5,5′-dimethoxylariciresinol (6),5,5′-dimethoxysecoisolariciresinol (7),(7′S,8′S)-4′-O-methylcleomiscosin D (8),(+)-9′-O-(Z)-feruloyl-5,5′-dimethoxylariciresinol (9),(+)-9′-O-(E)-feruloyl-5,5′-dimethoxylariciresinol (10),daidzin (11) and 3′-methoxydaidzin (12),respectively.Compounds 1-3 and 8-10 were isolated from this plant for the first time.Compounds 1,3-7,9 and 10 showed inhibitory effect on DGAT1 activity with IC₅₀ values ranging from 81.5±1.2 to 123.2±1.1 μM.