Tripterygium wilfordii: Historical origins, pharmacological mechanisms, and biosynthesis of triptolide and celastrol
Year: 2026
Type: article
Abstract: Tripterygium wilfordii is a traditional Chinese medicinal herb with a long history of therapeutic use but remains controversial in modern medicine because of its potent toxicity. Among its diverse chemical constituents, the diterpenoid triptolide and the triterpenoid celastrol have emerged as prominent compounds due to their remarkable pharmacological activities, including antitumor, immunosuppressive, anti-obesity, and neuroprotective effects. However, their clinical translation is limited by toxicity concerns and restricted natural availability. This review systematically summarizes the medicinal history and chemical constituents of T. wilfordii, with particular emphasis on the pharmacological mechanisms, structural modification strategies, and recent advances in the biosynthesis of triptolide and celastrol. In addition, we discuss perspectives on toxicity mitigation and lead compound development, aiming to provide theoretical guidance and valuable references for modern drug development and the green manufacturing of T. wilfordii -derived resources.
Institution: Capital Medical University
Language: English
Subfield: Complementary and alternative medicine
Field: Medicine
Domain: Health Sciences
Open Access status: diamond
OpenAlex ID: W7155077980