Sphenocentrum jollyanum Pierre is a member of a diverse family of plants known as Menispermaceae. They are famous for a plethora of important biological functions. S. jollyanum is a shrub native to the tropical forest zones of West Africa and thrives in deep shade. It is widely cultivated in Cameroun, Sierra Leone, Nigeria, Ghana, and Côte d’Ivoire. S. jollyanum is employed in folk medicine as a cure for wounds, fever, coughs, high blood pressure, breast tumor, constipation, and as an aphrodisiac. Phytochemical investigations revealed that the plant is a rich source of secondary metabolites such as annin, alkaloids, saponins, and flavonoids. Pharmacological activities include anti-diabetic, anti-inflammatory, anti-bacterial, anti-viral, anti-malarial, angiogenic, and anxiogenic. Thus, this present review summarizes the phytochemical and nutritional constituents and important biological studies on various crude extracts, fractions, and isolated principles of all morphological organs of S. jollyanum.