Diosgenin [25R-spriost-5-en-3þ-ol], is an important steroidal metabolite found in various plant species. The discovery of diosgenin has made it one of the most researched and studied herbal product. Moreover, there is excellent opportunity to address whether diosgenin plays a role in chemoprevention versus therapy, or both. However, rigorous experimental based evidence in support of ethnomedicine-derived notions would lead to the development of products relevant to drug development. The health beneficial effects of diosgenin are further extended to its potential role to treat other ailments such as HIV and hepatitis-C infections as well as liver diseases. There is little information regarding the bioavailability, pharmacokinetics and pharmacodynamics of diosgenin in relation to its health beneficial effects. It has been reported to have wide spectrum of biological properties that contributes to several diseases in its role as a health beneficial phytochemical by citing new studies.