This study was carried out to investigate the antioxidative and antitumor activities of Saussurea lappa for the purpose of developing a functional food. The methanol extract of Saussurea lappa was fractionated with five solvents (hexane, chloroform, EtOAc, BuOH, water) and examined for antioxidative activities and xanthine oxidase inhibitory activity in addition to growth inhibitory activity of human cancer cell (HT-29, SNU-1, HeLa). Total phenol compound contents were higher in EtOAC fraction than other fractions. Also, electron donating ability was over 90% at 500μg/ml (93.1 %) and 1000μg/ml (94.3%). The hexane fraction revealed stronger nitrite scavenging ability than the positive control (ascorbic acid) and its abilities were 22.4% and 42.8% at 500μg/ml and 1000μg/ml, respectively. Xanthine oxidase inhibitory activity had similar tendency to electron donating ability. The EtOAc fraction showed high inhibition to xanthien oxidase activities at 500μg/ml(81.9%) and 1000μg/ml(90.4%). In the antitumor activity test, the hexane fraction exhibited potent growth inhibition activity against HT-29, SNU-1 and HeLa cells. Therefore, we believe that Saussurea lappa can be developed into a functional food with antioxidant activity. Additional studies are required for the hexane and chloroform fractions of Saussurea lappa to develop them into therapeutic supplements for stomach cancer, colon cancer, and cervical cancer.