Southern Africa is one of two world centres of diversity in the Hyacinthaceae, harbouring approximately half the worlds family representatives. Some 368 species in 27 genera are locally represented. Plants are well distributed throughout the region, with a predominance in the Western Cape of South Africa. Some 23 species in nine genera have been phytochemically investigated, revealing compounds belonging to a diverse range of chemical classes. The chemical constituents from plants of this family have been divided into four classes, namely, homoisoflavanones, steroidal compounds, bufadienolides and miscellaneous compounds. A single report on the occurrence of Amaryllidaceae alkaloids in Urginea altissima is questioned following a reinvestigation of this species. Plants are employed for traditional medicinal purposes ranging from the treatment of hangovers, rheumatic fever, sprains and syphilis to cancer. A number of species have been toxicologically assessed following human deaths and livestock losses after ingestion. The bioactivity and ethnobotany of southern African hyacinthacs is reviewed, as is the pharmacology of isolated constituents and crude extracts.