In this study, we were performed to elucidate the antioxidant and anticancer activity by leaves extracts from Acer tegmentosum (AT-L). In DPPH, ABTS radical scavenging activity, the AT-L revealed the high scavenging activity. Especially, the AT-L measured the highest ABTS radical scavenging activity, which is higher than ascorbic acid. The types of human cancer cells for evaluating the anticancer activity were colorectal cancer (SW480), prostate cancer (PC-3), breast cancer (MCF-7), pancreatic cancer (AsPC-1), lung cancer (A549) and liver cancer (HepG2). Human cancer cell viability was measured using MTT assay. Treatment of the AT-L decreased the cell viability and induced apoptosis in SW480 cells. These results suggest that extracts of the AT-L can be used as supplementary material for developing the natural antioxidant and anticancer drug for human cancer cells.