Two flavonoid aglycons, eight flavonoid glycosides, chlorogenic acid and syringin were isolated from aerial parts of Carthamus lanatus. Isorhamnetin 3-O-β-D-glucoside and chlorogenic acid were found for the first time in the genus Carthamus and respectively, quercimeritrin, astragalin, kaempferol 3-O-β-D-sophoroside and syringin in the species. The ethyl acetate fraction of the methanol extract exhibited a higher antioxidant activity than the butanol fraction measured by the α,α-diphenyl-β -picrazylhydrazyl (DPPH) free radical scavenging assay. Cytotoxicity and antioxidant activities of the main constituent, luteolin 7-O-β-D-glucoside, were evaluated.