Two new compounds, butyl(Z)-3-((3R,4R)-5-(hydroxymethyl)-3,4-dimethyl-3,4-dihydro-2H-pyran-6-yl)acrylate ( 1) and (2Z,4S)-4,5-dihydroxy-3,4-dimethylpent-2-enoic acid (2) along with seven known ones, stigmast-5,28(29)-dien-3β-ol (3), β-sitosterol (4), carotene ( 5), fraxetin (6), p-coumaric acid (7), cis-p-hydroxycinnamic acid (8), ferulic acid (9) were obtained from the whole plant of Pachysandra terminalis.The structures of these compounds were elucidated by comprehensive spectroscopic methods including 1D, 2D NMR, MS, IR and ECD data analysis.Notably, compounds 3 and 5~8 were isolated from genus Pachysandra for the first time.Moreover, compounds 1~3 and 6~8 were tested their cytotoxic activities against three cancer cells, however, only compound 1 showed inhibitory effect in SW620 cells with IC50 value of 47.7 μM.