Germination by water soaking is a critical process in promoting the antioxidative activity and bioactive compounds in brown rice. GBR contains much higher levels of antioxidative activity and bioactive compounds than UBR. In order to maximize antioxidative activity and bioactive compounds, germination should be under the conditions of higher temperature (36°C in this study), long soaking time (72 h), darkness, and closed vessel. Also, higher temperature (36°C) during soaking process is a key factor in promoting GABA content in the GBR. Moreover, we find strong correlations between antioxidative activities (DPPH radical scavenging ability, TEAC, and reducing power) and bioactive compounds (γ-oryzanols, tocopherol and tocotrienol) in both cases of and . These results are very useful research references for the development of future functional foods and additives and are also useful information to be used in the prevention of cancers.