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
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