Abstract: To discover new cytotoxic constituents from the traditional Chinese folk medicine “Fo Jia Cao” (whole plants of Sedum lineare Thunb.),the isolation and purification of a methanolic extract was performed with medium-pressure column chromatography and preparative HPLC.Chemical Structures of isolated compounds were elucidated by detailed spectral analysis.Cytotoxic activity of compounds was evaluated using the MTT method.Nine pure compounds were obtained and their structures were elucidated as kaempferol (1),luteolin (2), 3,5,7,3',5'-pentahydroxyflavone (3),quercetin (4),astragalin (5),caffeic acid (6),ferulic acid (7),4-hydroxybenzoic acid (8) and β-sitosterol (9).Compounds 1—8 were firstly isolated from the title plant. Compounds 1—7 displayed cytotoxic activity.Phenylpropanoid acids 6 and 7 exhibited better cytotoxic activity than flavonoids 1—5 with IC50 values ranging from 19.7 to 56.4μg/mL.