A Glutathione (GSH)-Responsive Near-Infrared (NIR) Theranostic Prodrug for Cancer Therapy and Imaging

被引：176
作者：
Kong, Fanpeng [1 ]
Liang, Ziye [1 ]
Luan, Dongrui [1 ]
Liu, Xiaojun [1 ]
Xu, Kehua [1 ]
Tang, Bo [1 ]
机构：
[1] Shandong Normal Univ, Collaborat Innovat Ctr Functionalized Probes Chem, Shandong Prov Key Lab Clean Prod Fine Chem,Minist, Coll Chem Chem Engn & Mat Sci,Key Lab Mol & Nano, Jinan 250014, Peoples R China
来源：
ANALYTICAL CHEMISTRY | 2016年 / 88卷 / 12期
基金：
中国国家自然科学基金;
关键词：
RATIOMETRIC FLUORESCENT-PROBE; CHANGES IN-VIVO; DRUG-RELEASE; GEMCITABINE DELIVERY; SELECTIVE DETECTION; LIVING CELLS; NAKED-EYE; ON PROBE; TURN-ON; FLUOROPHORES;
D O I：
10.1021/acs.analchem.6b01135
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
To reduce the side effects of chemotherapy, nontoxic prodrugs activated by the tumor microenvironrnent are urgently required for use in cancer treatment. In this work, we developed prodrug 4 for tumor-targeting treatment and imaging of the anticancer drug release in vivo. Taking advantage of the high glutathione (GSH) concentration in cancer cells, the disulfide bond in prodrug 4 was cleaved, resulting in the release of an active anticancer drug and a near-infrared (NIR) fluorescence dye turn-on. Furthermore, contrast to the free anticancer drug, the prodrug exhibited higher cytotoxicity to hepatoma cells than that to normal HL-7702 cells. Thus, prodrug 4 is a promising platform for specific tumor-activatable drug delivery system, because of its favorable features of in situ and in vivo monitoring of the drug release and therapeutic efficacy.
引用
收藏
页码：6450 / 6456
页数：7
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