Brown rice, barley, and buckwheat contain a variety of functional ingredients, such as vitamins, minerals, and dietary fibers. Germination is an effective technique for improving the digestion and absorption of the constituents in grains. In addition, germination could modify the chemical properties of grains and increase the content of biologically active substances. Many studies have reported that the intake of grains or germinated grains could ameliorate blood glucose level, stimulate the immune system, lower blood pressure, and result in anti-obesity effect. Therefore, grains and germinated grains are being utilized in a variety of functional products. The present study reviews the primary components and bio-functionalities of grains (brown rice, barley, and buckwheat) and germinated grains (germinated brown rice). The development of grain products for promoting health functional properties is also discussed.