Research progress on strategies for toxicity reduction and efficacy enhancement of triptolide
- VernacularTitle:雷公藤甲素的减毒增效策略研究进展
- Author:
Xiaoqing ZHENG
1
;
Ying DING
1
;
Shanshan XU
2
;
Long WANG
3
;
Shanshan HAN
3
;
Yaping XING
1
;
Meng ZHANG
1
;
Wenhao LI
2
Author Information
1. Pediatric Hospital of the First Affiliated Hospital of Henan University of Traditional Chinese Medicine，Zhengzhou 450000，China;Medical College of Pediatrics，Henan University of Chinese Medicine，Zhengzhou 450000，China
2. Pediatric Hospital of the First Affiliated Hospital of Henan University of Traditional Chinese Medicine，Zhengzhou 450000，China
3. Medical College of Pediatrics，Henan University of Chinese Medicine，Zhengzhou 450000，China
- Publication Type:Journal Article
- Keywords:
triptolide;
toxicity reduction and efficacy enhancement;
structural modification;
dosage form improvement;
herbal compatibility;
external therapy of traditional Chinese medicine
- From:
China Pharmacy
2026;37(11):1496-1501
- CountryChina
- Language:Chinese
-
Abstract:
Triptolide （TP）， the core active component of the traditional Chinese medicine Tripterygium wilfordii ， exhibits remarkable pharmacological activities including anti-inflammatory， immunosuppressive and anti-tumor effects， and holds broad application prospects in the treatment of major diseases such as autoimmune diseases and malignant tumors. However， TP has a narrow therapeutic window and causes multi-organ toxicities including liver， kidney and reproductive toxicities， which severely restrict its safe clinical application and new drug development. Therefore， toxicity reduction and efficacy enhancement has become a core scientific problem urgently to be solved in this field. This paper systematically reviews the four core strategies for TP toxicity reduction and efficacy enhancement， including structural modification， dosage form improvement， herbal compatibility， and external therapies of traditional Chinese medicine. Among them， structural modification optimizes the toxic and efficacy characteristics of TP from the molecular structure level， with typica l derivatives including （5 R ）-5-hydroxy triptolide， ZT01， PG490-88， etc. Dosage form modification achieves toxicity reduction and efficacy enhancement via targeted and sustained-controlled drug release of diverse delivery systems. It includes triptolide preparations such as nanoparticles， liposomes， microemulsion gels and liquid crystals， possessing favorable clinical transformation potential. The herbal compatibility and external therapies of traditional Chinese medicine conform to the holistic view of traditional Chinese medicine and have a profound clinical application foundation， but their mechanisms of action are insufficiently elucidated， and they lack unified standardized specifications and high-quality evidence-based proof. In the future， we should rely on multi-omics technology to elucidate the toxic and efficacy mechanisms， integrate technologies to optimize preparations， improve the evaluation system and promote clinical transformation.
