Progress of research on celastrol derivatives as anti-tumor agents
- VernacularTitle:雷公藤红素抗肿瘤类衍生物研究进展
- Author:
Xueling ZHANG
1
;
Na LI
;
Li CHEN
Author Information
1. 中国药科大学 中药学院天然药物化学系, 南京 211198
- Publication Type:Journal Article
- Keywords:
celastrol;
anti-tumor;
structural modification;
structure activity relationship
- From:
Journal of China Pharmaceutical University
2024;55(6):826-836
- CountryChina
- Language:Chinese
-
Abstract:
Celastrol, a pentacyclic triterpenoid compound derived from the root of Chinese herb Tripterygium wilfordii Hook.f.,can inhibit the growth of various types of malignant tumors. However, it still has some limitations, including high toxicity, poor water solubility, and low targeting efficiency. Therefore, structural modification of celastrol has become a research hotspot in recent years. The structural modifications of celstrol reported have focused on C-20-COOH and C-2, C-3, C-6 or multiple sites of AB ring. This review provides an overview of the research progress of anti-tumor celastrol derivatives in recent years according to different structural modification sites and purposes, such as enhancing the inhibitory effect on the Hsp90-Cdc37 protein-protein interaction, and modification methods, including principles of parallelism and targeting specific sites. In addition, it briefly discusses the antitumor activity, mechanism of action, and structure-activity relationship of these derivatives, aiming to provide theoretical guidance for the discovery of new celastrol derivatives with high efficiency, low toxicity, and strong selectivity.
