Active molecule-based theranostic agents for tumor vasculature normalization and antitumor efficacy  

作　　者：Jin Wang Xiaoyan Pan Junyu Zhang Qingqing Zhang Yanchen Li Weiwei Guo Jie Zhang 

机构地区：[1]School of Pharmacy,Health Science Center,Xi’an Jiaotong University,Xi’an 710061,China [2]Center of Advanced Pharmaceuticals and Biomaterials,State Key Laboratory of Natural Medicine,China Pharmaceutical University,Nanjing 210009,China

出　　处：《Chinese Chemical Letters》2024年第8期229-234,共6页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(NSFC,Nos.82373793,82173742);the Science Fund for Distinguished Young Scholars of Shaanxi Province(No.2022JC-54);the Key Research and Development Program of Shaanxi Province(No.2023-YBSF-131).

摘　　要：Tumor vascular normalization has emerged as a promising strategy for synergistic therapy recently.Based on the strategy of“fluorescence turn on-controllable release”,a novel bifunctional candidate was con-structed based on previous developed vascular normalization inducer QDAU5,which could self-assemble to form functional enzyme infrared QDAU5 nanoparticles(FEIRQ NPs).Subsequently,biological evaluation demonstrated that the FEIRQ NPs could induce ferroptosis,endoplasmic reticulum stress,and antigen pre-conditioning and maturation of dendritic cells and CD8^(+)T cells,leading to excellent antitumor efficacy in the absence of cytotoxic drugs.Additionally,FEIRQ NPs show high fluorescence intensity upon expo-sure to theβ-galactosidase(β-Gal)enzyme expressed in ovarian cancer,enabling real-time monitoring of therapeutic effects.Overall,our findings suggest a prospering strategy to early diagnosis and efficient therapy for ovarian cancer without cytotoxicity.

关 键 词：Tumor vasculature normalization Diagnosis and treatment CYTOTOXICITY Depleting glutathione Ferroptosis Immune activation 

分 类 号：R730.5[医药卫生—肿瘤]