Abstract: Germinated brown rice is a promising functional food raw material. After germination, brown rice not only improves its eating quality, but also enriches biological active ingredients, thus giving many physiological functions to germinated brown rice. This paper introduced the content changes of the main biological active substances such as γ-aminobutyric acid, γ-oryzanol, vitamin E, higher fatty alcohol and dietary fiber in germinated brown rice during germination, and the effects of germination conditions on the content changes of these main biological active substances. The effects of these bioactive substances on the physiological functions of germinated brown rice, such as anti-oxidation, hypolipidemic, blood pressure lowering, prevention and treatment of cancer, prevention of diabetes and the future research directions and application of germinated brown rice was summarized.