In vivo near-infrared imaging and phototherapy of tumors using a cathepsin B-activated fluorescent probe

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• 作者：Xiaoqiang Chen^a ; ^b ; ¹ ; Dayoung Lee^a ; ¹ ; Sungsook Yu^c ; ¹ ; Gyoungmi Kim^a ; Songyi Lee^a ; Yejin Cho^c ; Haengdueng Jeong^c ; Ki Taek Nam^c ; ^{kitaek@yuhs.ac} ; Juyoung Yoon^a ; ^{jyoon@ewha.ac.kr}
• 关键词：Specific phototherapy ; NIR bioimaging ; Enzyme-activated fluorescence ; Multiple functional probe
• 刊名：Biomaterials
• 出版年：2017
• 出版时间：April 2017
• 年：2017
• 卷：122
• 期：Complete
• 页码：130-140
• 全文大小：3240 K
• 卷排序：122

文摘

The development of multifunctional reagents for simultaneous specific near-infrared (NIR) imaging and phototherapy of tumors is of great significance. This work describes the design of a cathepsin B-activated fluorescent probe (CyA-P-CyB) and its applications as an NIR imaging probe for tumor cells and as a phototherapy reagent for tumors. In vitro experiments demonstrated that CyA-P-CyB was activated via the cleavage of a peptide linker by cathepsin B in tumor cells to produce fluorescence in the NIR region based on a FRET mechanism. MTT assays showed that the phototoxicity of CyA-P-CyB toward cells depended on the activity of cathepsin B, and the probe exhibited specific phototoxicity toward tumor cells. CyA-P-CyB was also successfully applied to the in vivo imaging and phototherapy of tumors. Histological analysis indicated that CyA-P-CyB had no cytotoxic effects on seven mouse tissues (lung, liver, heart, kidney, pancreas, spleen and brain) after the CyA-P-CyB treatment and laser irradiation.