Agapanthus is a monocotyledonous genus native to South Africa and distribute from the Cape Peninsula to the mountainous areas south of the Limpopo River. The traditional uses of this genus against reproductive and central nervous systems disorders were conspicuous. The biological efficacy of Agapanthus has revealed its promising, anti-inflammatory, antioxidant, antibacterial, antifungal, uterotonic, anti-hypertension, and cAMP phosphodiesterase inhibition effects in addition to CNS activities. The antifungal activity of Agapanthus species was the most promising. Among all the genus species, Agapanthus africanus (L.) Hoffmanns., has the highest antimicrobial properties. A total of 28 secondary metabolites of this genus have been reported, including sterols, saponins, sapogenins, flavonoids, lignan, and lignan precursors. Saponins were the most abundant isolated phytoconstituents, and agapanthussaponin A and B showed the most promise as effective fungicidal medicines among the isolated saponins. Some species such as Agapanthus coddii Leighton and Agapanthus caulescens Spreng., still require extensive phytochemical and biological investigation. A toxicological study on this genus is also required. However, to date, there is no review of literature summarizing the traditional applications, bioactive compounds and biological activities on this genus. This encouraged us to present a review focused on its current traditional uses, phytoconstituents, pharmacological activities, and future prospects. In attempt to do this, a comprehensive review of all published literature was carried out using numerous available science-based datasets. • This is the first comprehensive review on the genus Agapanthus . • This review provides valuable information about the traditional uses, various active constituents, and biological activities of genus Agapanthus . • In South African cultural life, Agapanthus species have been used widely for immemorial time in the traditional medical systems. • Saponins and flavonoids are the major isolated bioactive metabolites, in addition to, sterols, lignan, and lignan precursor. • Agapanthus has a wide range of pharmacological properties according to numerous reports.