Major bioactive metabolites derived from Tripterygium wilfordii: structures, mechanisms, and therapeutic potentials
TL;DR
This review provides a comprehensive overview of the chemical classification, pharmacological mechanisms, and clinical translation of major metabolites derived from T. wilfordii that highlight their application in autoimmune diseases, cancer, fibrosis, and metabolic disorders, while addressing current challenges in safety, solubility, and bioavailability.
Abstract
Tripterygium wilfordii, a traditional Chinese botanical drug, has emerged as a rich source of bioactive metabolites with promising therapeutic potential. Among its metabolites, diterpenoids and triterpenoids—such as triptolide, triptonide, and celastrol—exhibit potent immunosuppressive, anti-inflammatory, and anti-tumor properties through modulation of key molecular pathways including NF-κB, JAK/STAT, and TGF-β/Smad. This review provides a comprehensive overview of the chemical classification, pharmacological mechanisms, and clinical translation of major metabolites derived from T. wilfordii. It highlights their application in autoimmune diseases, cancer, fibrosis, and metabolic disorders, while addressing current challenges in safety, solubility, and bioavailability. Advancements in drug delivery systems, structural modification, and precision medicine approaches are also discussed. Together, these insights aim to guide future research and translational development of T. wilfordii-based compoundic therapeutics.