The purpose of this study was to examine biological activities, including total contents of polyphenol, antioxidant activities, inhibitory activities of tyrosinase, and protective effect against oxidative stress in the HepG2 cells of ethanol extracts from wheat sprout. The antioxidant activity of extracts was determined by ABTS and DPPH radical scavenging activities. Ethanol extracts were tested using different ethanol concentrations (0%, 30%, 50%, 80% and 95%, respectively). The highest amount of total polyphenol was extracted by 50% and 80% ethanol which was 26.3 and 26.8 mg gallic acid equivalents/g sample, respectively. High levels of ABTS and DPPH radical scavenging activity were found in 50% ethanol (26.7 and 15.0 mg TEAC/g sample, respectively) and 80% (24.3 and 16.1 mg TEAC/g sample, respectively) ethanol extracts. Also, 50% and 80% ethanol extracts indicated higher inhibitory activities of tyrosinase compared with other extracts. In the cell-based assay, pre-treatment of the HepG2 cells with wheat sprout extracts prevented the cell damage induced by TBHP (tert-butyl hydroperoxide). The results of this study indicate that wheat sprout has significantly higher diverse biological activities and apparently has significant health benefits.