Rice bran has been recognized as an excellence source of bioactive compounds, but only a small amount is consumed by humans. The limitation of using rice bran in a food industry is its rough texture and low concentration of bioactive compounds, when incorporated into food products. The purpose of this study was to improve the concentration of bioactive contents and antioxidant activity of rice bran, through the use of germination and enzymatic treatment. Rough rice was germinated prior to drying and milling to obtain germinated rice bran (GRB), whereas the regular rice bran (RB) was obtained by milling the ungerminated rough rice. In order to prepare a rice bran enzymatic treatment, GRB and RB were dissolved in distilled water prior to adding with neutral protease and alpha amylase. The slurry was sieved, heated and freeze-dried to obtain a rice bran extracted powder. The results indicated that both germination of rough rice and enzymatic treatment improved the levels of γ-oryzanol (452.21 mg 100g ^-1), α-tocopherol (26.14 mg 100g ^-1) and phenolic contents (743.74 mg GAE 100g ^-1) by 2, 3 and 5 times, respectively, compared with that of untreated rice bran, whilst only enzymatic treatment, but germination, increased the concentration of protein, reducing sugar and total amino acid of the rice bran. Four different methods were used to evaluate the antioxidant activity of the rice bran. The germination and enzymatic extraction improved the antioxidant activity of rice ban products, which those obtained from enzymatic treatment (RBE and GRBE) revealed the strongest antioxidant activity.