A review. Tripterygium wilfordii (Celastraceae) is a wild shrub distributed in southern China. It was used in Traditional Chinese Medicine as an insecticide for killing fly larvae 'maggots and Oncomelania snails, a vector of Schistosoma japonicum. In 1969, the decoction of the radix of T. wilfordii was first used in China to treat patients with rheumatoid arthritis (RA); although efficacious, side effects were observed Subsequently, a partially purified extract called "multiglycoside of the radix" (TWG) was used to treat autoimmune diseases including RA, lupus erythematosus, chronic nephritis and hepatitis. TWG appeared to have fewer side effects compared to the T. wilfordii decoction. In China, TWG is also used to treat various skin disorders, such as psoriasis and leprosy. In an unrelated area, TWG was found to have male spermicidal antifertility activity. Thus far, more than 46 diterpenoids, 20 new triterpenoids, 26 alkaloids and other small mols. have been isolated and identified from the plant. Among them the most potent are triptolide type compounds, which show immunosuppressive, anticancer and antifertility activities. The derivative of triptolide, PG490-88, is being evaluated in phase I clin. trials as an anticancer agent. The natural products structural chem. of T. wilfordii has been well defined with several total syntheses of triptolide reported.