Rhizoma of Smilax china has been used as anti-inflammatory and analgesic, antiedemic agent in Korean folk medicine. In order to investigate the efficacy of anti-oxidative activity, the activity-guided fractionation and the isolation were performed. Each fractions (H2O fraction, 20%, 40%, 60%, 100% MeOH fractions and CHCl3 fraction) was examined anti-oxidant activity by 1,1- diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging potential. It was revealed that 40%, 20% MeOH fractions and H2O fractions have significant anti- oxidative activity. From 40% and 20% MeOH fractions two flavonoid glycosides and one procyanidin were isolated and elucidated apigenin-7-O-a-L-rhamnopyranosyl(1→2)-β-D- glucopyranoside, apigenin-7-O-a-L-rhamnopyranosyl(1→6)-β-D-glucopyranoside and catechin(4a→6)epicatechin through their physicochemical data and IR, FAB-MS, 13C-NMR, and 1NMR analysis with authentics, respectively. The isolated compounds were examined by DPPH method. Apigenin-7-O-a-L-rhamnopyranosyl(1→ 2)-β-D-glucopyranoside and catechin (4a→6) epicatechin showed powerful radical scavenging activities on DPPH radical among three compounds.