The fruits of Malpighia glabra and M. emarginata (Family: Malpighiaceae) are commonly known as ‘Acerola cherry’ or ‘Barbados cherry’. Acerola fruits are well known for their high content of vitamin C, phenolic compounds, including benzoic acid derivatives, phenylpropanoids, flavonoids, anthocyanins, and carotenoids. In recent years, there is a growing interest in the role of Acerola as a nutraceutical or functional food with increasing market value. Extracts and bioactive compounds isolated from Acerola are studied for their various health promoting activities and biological activities such as antioxidant, antitumor, antihyperglycemic and skin protecting/skin whitening. This article reviewed the scientific studies regarding the bioactive chemical constituents and the health beneficial effects of Acerola extracts and isolated compounds. These findings may help in future research concerning Acerola and Acerola based nutritional products. Acerola fruits can be considered as good candidates for the development of novel functional foods. However, detailed in vitro, in vivo and clinical studies, particularly mechanism-based studies are needed for the development of evidence-based functional food products in future.