A Glutathione (GSH)-Responsive Near-Infrared (NIR) Theranostic Prodrug for Cancer Therapy and Imaging
A Glutathione (GSH)-Responsive Near-Infrared (NIR) Theranostic Prodrug for Cancer Therapy and Imaging
复制标题
用于癌症治疗和成像的谷胱甘肽 (GSH) 响应性近红外 (NIR) 治疗诊断前药
DOI：
10.1021/acs.analchem.6b01135
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发表时间：
2016-06-21
影响因子：
7.4
通讯作者：
Tang, Bo
中科院分区：
文献类型：
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作者：
Kong, Fanpeng;Liang, Ziye;Tang, Bo
为了减少化疗的副作用，迫切需要由肿瘤微生物活性剂活化的无毒前药用于癌症治疗。在这项工作中，我们开发了前药4肿瘤靶向治疗和成像的抗癌药物在体内释放。利用肿瘤细胞内谷胱甘肽（GSH）浓度高的特点，前体药物4中的二硫键发生断裂，释放出活性抗癌药物，近红外（NIR）荧光染料被激活，且前体药物对肝癌细胞的细胞毒性高于正常HL-7702细胞。因此，前体药物4是一个有前途的平台，为特定的肿瘤激活的药物输送系统，因为它的有利的特点，在原位和体内监测药物释放和治疗效果。
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.