雷公藤醇
活性氧
前药
化学
生物利用度
螯合作用
三磷酸腺苷
癌细胞
药理学
生物物理学
癌症研究
生物化学
癌症
医学
细胞凋亡
生物
有机化学
内科学
作者
Hanrong Li,Yifan Li,Lingpu Zhang,Li Wang,Dong Lu,Dongsheng Tang,Yitong Lv,Jinbo Zhang,H. P. Yan,He Gong,Ming Zhang,Kaili Nie,Yi Hou,Yingjie Yu,Haihua Xiao,Chaoyong Liu
出处
期刊:Science Advances
[American Association for the Advancement of Science (AAAS)]
日期:2024-07-12
卷期号:10 (28)
被引量:5
标识
DOI:10.1126/sciadv.adn0960
摘要
Celastrol (CEL), an active compound isolated from the root of Tripterygium wilfordii , exhibits broad anticancer activities. However, its poor stability, narrow therapeutic window and numerous adverse effects limit its applications in vivo. In this study, an adenosine triphosphate (ATP) activatable CEL-Fe(III) chelate was designed, synthesized, and then encapsulated with a reactive oxygen species (ROS)–responsive polymer to obtain CEL-Fe nanoparticles (CEL-Fe NPs). In normal tissues, CEL-Fe NPs maintain structural stability and exhibit reduced systemic toxicity, while at the tumor site, an ATP-ROS–rich tumor microenvironment, drug release is triggered by ROS, and antitumor potency is restored by competitive binding of ATP. This intelligent CEL delivery system improves the biosafety and bioavailability of CEL for cancer therapy. Such a CEL-metal chelate strategy not only mitigates the challenges associated with CEL but also opens avenues for the generation of CEL derivatives, thereby expanding the therapeutic potential of CEL in clinical settings.
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