In this study, the bioactivities of ethanol (EELS) and water extract (WELS) from the leaf of Lythrum salicaria L. were investigated. In the anti-cancer activity, the growths of both human prostate cancer (DU145) and human colonic carcinoma cell (HT29) were inhibited up 60% by adding 10 mg/ml of EELS. Anti-inflammatory activity of EELS and WELS have been evaluated on lipopolysaccharide (LPS) induced release of nitric oxide (NO) by the macrophage RAW 264.7 cells. EELS and WELS inhibited inflammatory by 57.3 and 46.9% in 10 mg/ml, respectively. In the anti-oxidative activity, IC50 of DPPH radical scavenging activity was respectively 60.71 and 92.90 μg/ml by EELS and WELS. In the anti-diabetic activity, IC50 of α-amylase inhibitory activity of EELS and WELS were respectively 5,250 and 5,020 μg/ml. IC50 of α-glucosidase inhibitory activity was 7.96 and 68.41 μg/ml by EELS and WELS. In the anti-obesity, IC50 of lipase inhibitory activity was 880 and 9,840 μg/ml by EELS and WELS. Finally, EELS and WELS exhibited anti-oxidative, anti-inflammatory, anti-diabetic activity and anti-obesity. It suggests that Lythrum salicaria L. could be potentially used as a resource of bioactive materials for health functional foods.