Bio-Activities and Syntheses Developments of Triptolides

Tripterygium wilfordii Hook.f. has a long history of use in traditional Chinese medicine. The diterpene triepoxide triptolide 1, as the main bioactive constituent of Tripterygium extracts, has been used to treat a variety of autoimmune, inflammation-related conditions and neurodegenerative diseases, and it also displays antiinflammatory activity, antiproliferative and apoptotic effects, antifertility and insecticidal activity. Several synthetic studies and structure-activity relationships (SAR) have been carried out on triptolide as well as others structurally related molecules. This review focused on the biological and pharmacological activities, total syntheses and their structure-activity relationships of triptolide and congeners. Keywords: Tripterygium, Triptolide, Diterpene, Antiinflammatory, Anticancer, Spondylitis, Systemic lupus erythematosus, TWHF, iNOS, Tamelens method, Alvarez-manzanedas method, Lactone ring