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Synthesis of a new deoxyglucose derivative modified near-infrared fluorescent probe for tumor diagnosis

Sun, Chunlong, Du, Wen, Wang, Baoqin, Yao, Zhigang, Liu, Junhua, Wang, Jun, Xie, Wenjun, Wu, Tao, Fan, Yanhui, Yang, Hongjun
Biochemical and biophysical research communications 2017
3-mercaptopropionic acid, acute toxicity, deoxyglucose, fluorescence, fluorescent dyes, glucose, glycolysis, image analysis, membrane permeability, mice, neoplasm cells, neoplasms, photostability, tissues, toxicity testing
Malignant neoplasms exhibit an elevated rate of glycolysis and a high demand for glucose over normal cells. This characteristic can be exploited for in vivo imaging and tumor targeting examined. In this manuscript, we describe the synthesis of near-infrared (NIR) fluorochrome IR-822-labeled 2-amino-2-deoxy-d-glucose (DG) for optical imaging of tumors in mice. NIR fluorescent dye IR-820 was subsequently conjugated with 3-Mercaptopropionic acid and 2-amino-2-deoxy-d-glucose to form IR-822-DG. The cell experiments and acute toxicity studies demonstrated the low toxicity of IR-822-DG to normal cells/tissues. The dynamic behavior and targeting ability of IR-822-DG in normal mice was investigated with a NIR fluorescence imaging system. The in vitro and in vivo tumor targeting capabilities of IR-822-DG were evaluated in tumor cells and tumor bearing mice, respectively. Results demonstrated that IR-822-DG actively and efficiently accumulated at the site of the tumor. The probe also exhibited good photostability and excellent cell membrane permeability. The study indicates the broad applicability of IR-822-DG for tumors diagnosis, especially in the glucose-related pathologies.