1. Bioactive compounds from medicinal plants with anticancer and anti-inflammatory effects have become key resources in drug discovery fields for the treatment of various malignancies and immunological disorders. 2. Tripterygium wilfordii (TW) is a medicinal plant that exhibits profound immunosuppressive effects and has been used in herbal regimens for the treatment of immunological diseases for thousand years in China. 3. Procedures for the isolation and characterization of TW bioactive compounds have been well established. Over the past three decades, more than 46 diterpenoids, 20 new triterpenoids, 26 alkaloids and other small molecules have been identified from TW. 4. Triptolide, celastrol and tripchlorolide are among the bioactive compounds conferring the immunosuppressive and anticancer activities of TW. Accumulated evidence suggests that the TW bioactive compounds exert their pharmacological actions by modulating the transcriptional activity of nuclear factor-κB signalling molecule. 5. Triptolide derivatives with improved water solubility have emerged as promising drug candidates. Clinical trials are being conducted on the derivatives to provide encyclopaedic knowledge on triptolide pharmacokinetics in patients.
© 2011 The Authors. Clinical and Experimental Pharmacology and Physiology © 2011 Blackwell Publishing Asia Pty Ltd.