In this study,the effects of orientin and isoorientin on radical-scavenging activities( DPPH·, ABTS+·,H 2 O 2,·OH),lipid peroxidation,Cu2 +/ H 2 O 2 induced BSA and DNA oxidative damage,and BSA protein carbonyls were investigated. The results showed that orientin and isoorientin exhibited high radical-scavenging activities and also effectively protected biological macromolecules including proteins, lipids,and DNA against oxidative damage induced by Cu2 +/ H 2 O 2. Moreover,the MTT assay revealed that orientin and isoorientin inhibited proliferation of HepG2 cells in a dose and time dependent manner, and the antioxidant and anticancer activities of isoorientin was much better than that of orientin. These results demonstrate the remarkable potentiality of isoorientin as a valuable nature antioxidant possessing original anticancer abilities.