Hylocereusundatus is typically the most cultivated vine cactus belonging to the family of Cactaceae, originating natively from Mexico and America. Commonly, it is well known under the name of “dragon fruit” or “pitaya”. In Malaysia, it is also called ‘buahnaga’ which gives the meaning of dragon fruit. Besides its attractive coloration, the fruits of Hylocereusundatus are being prevailed globally because of its rich source of polyphenolic components and their antioxidant activity. A wide ranging of phytochemicals of betalains, polyphenolic compounds and carotenoids are discovered to possess chemo-protective properties against oxidant stress in the body as well as maintain optimum equilibrium between antioxidants and oxidants for the enhancement of human health. The findings of this review are important to deliver an overview of Hylocereusundatus and its functional phytochemicals, with relation to its potential health benefit in providing perspectives of research and application. It presented more environmental benign antioxidant and antibacterial agents that are significant in the fields of healthcare, food processing, nutraceutical and cosmeceutical. Therefore, there should be a collective work by scientists and researchers to maximize the value chain of this fruit to global cultivars in order to expand the global market of dragon fruit.