Tripterygium wilfordii: Historical origins, pharmacological mechanisms, and biosynthesis of triptolide and celastrol
10.1097/st9.0000000000000114
- Author:
Yuhan JIA
1
;
Xinyi HU
1
;
Ziming ZHU
1
;
Yuan LI
1
;
Xuan LIU
1
;
Jinxuan YU
1
;
Jiadian WANG
1
;
Yating HU
1
Author Information
1. Department of Natural Medicine Resources and Chemistry of Chinese Materia Medica, School of Traditional Chinese Medicine, Capital Medical University, Beijing, China
- Publication Type:Journal Article
- Keywords:
Tripterygium wilfordii;
Triptolide;
Celastrol;
Pharmacological mechanisms;
Structural modification;
Biosynthesis
- From:
Science of Traditional Chinese Medicine
2026;4(3):211-224
- CountryChina
- Language:English
-
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 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.
