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Saponins are a large group of amphipathic molecules distributed in a considerable number of vascular plants, among which tubers belonging to the genus Dioscorea are notable. Their structure is composed of a hydrophilic moiety and a hydrophobic moiety, called sapogenin. The latter group includes diosgenin, which has been widely used in the medical field, for example, as a typical precursor of steroidal drugs. Therefore, the main purpose of this article is to present recent information on the applications of diosgenin, focusing on three areas of medical interest—cancer, biomaterials and Alzheimer’s disease—in order to display the clinical potential of this molecule.