Pomegranate (Punica granatum L.) have been subject of extensive studies for its abundance of phytochemicals and numerous biological and medicinal properties. It is a fruit-bearing tree, which is widely consumed as a nutraceutical source as well as functional food for putative health benefits. The phenolic components are the characteristic bioactive constitutes of pomegranate, including hydrolysable tannins, flavonoids, and phenolic acids. The whole plant of this tree has many medicinal folkloric uses and good therapeutic effect, such as anticancer, antioxidant, antibacterial, antiviral, hypoglycemic, lipid-lowering, cardioprotection and digestive system protection. Through comprehensive search of available literature, this narrative review can provide an up-to-date overview of the current knowledge of characteristic bioactive constituents's structure and potential health benefits of Pomegranate, which can be used as reference for the future clinical and basic research, and also helpful for the development of pomegranate into functional food and nutraceuticals.