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Biomaterials. 2017 Apr;122:130-140. doi: 10.1016/j.biomaterials.2017.01.020. Epub 2017 Jan 16.

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

Author information

1
Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea; State Key Laboratory of Materials-Oriented Chemical Engineering, College of Chemical Engineering, Jiangsu National Synergetic Innovation Center for Advanced Materials (SICAM), Nanjing Tech University, Nanjing 210009, China.
2
Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea.
3
Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea.
4
Severance Biomedical Science Institute, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul 120-752, South Korea. Electronic address: kitaek@yuhs.ac.
5
Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750, South Korea. Electronic address: jyoon@ewha.ac.kr.

Abstract

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.

KEYWORDS:

Enzyme-activated fluorescence; Multiple functional probe; NIR bioimaging; Specific phototherapy

[Indexed for MEDLINE]

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