Recent advances in chemical synthesis, biocatalysis, and biological evaluation of diosgenin derivatives - A review

Extracting organic compounds from plants and developing derivatives are essential methods for drug discovery. Diosgenin, extracted from Dioscoreaceae plants, is a type of spirostan steroid with various biological effects, including anti-inflammation, neuro-protection, and apoptosis-induction. Many researchers committed their work to the chemical semi-synthesis of diosgenin derivatives to improve diosgenin's therapeutic bioavailability and expand its range of applications in disease treatment and prevention. Biotransformation, a mild whole-cell biocatalysis method, also made crucial contributions to the structural diversity of diosgenin analogs in recent years. Although the structural modification of diosgenin has made significant progress, it lacks a comprehensive review. Here, we review the chemical modification and biotransformation of diosgenin along with the biological evaluation of diosgenin derivatives to provide a reference for the structural modification strategy and pharmaceutical application of diosgenin derivatives.