Plants belonging to the family Agavaceae are used in folkloric medicinal practices worldwide and chemical investigations of these plants have shown that they are an abundant source of steroidal saponins and sapogenins. Despite the large number of secondary metabolites isolated from this family so far, there have been few reports on the bioactivity of these compounds. This article provides a comprehensive review of the steroidal constituents of plants from the genera Agave, Cordyline, Dracaena, Furcraea, Nolina, Sansevieria and Yucca up to June 2006, and reports on the bioactivity of these compounds where available.