title: Comparison of near-infrared fluorescent deoxyglucose probes with different dyes for tumor diagnosis in vivo.
abstract: Glucose plays a central role in the cellular energy metabolism. Malignant tumors exhibit an elevated rate of glycolysis over normal tissues. In this study, two near-infrared fluorescent dyes, Cypate and ICG-Der-02, with different water solubility, were conjugated to 2-amino-2-deoxy-D-glucose (2DG) to form Cypate-2DG and ICG-Der-02-2DG, respectively, for NIR fluorescent imaging of tumors in nude mice. The clear routes and tumor targeting abilities of the two NIR fluorescent 2DG probes were compared. Results showed that ICG-Der-02-2DG with higher hydrophilicity was cleared faster by kidneys than the more lipophilic Cypate-2DG. Cypate-2DG had slower but stronger tumor targeting ability compared with ICG-Der-02-2DG. To investigate the correlation between the targeting ability of the probe and the glucose transporter (GLUT1) expression levels of cancer cells, the accumulation of Cypate-2DG in tumors was assessed in MCF-7/estradiol, U87MG, MCF-7 and MDA-MB-435 tumor xenografts, which express different levels of GLUT1. The results show that both Cypate-2DG and ICG-Der-02-2DG possess tumor targeting ability on all the tumors examined, with a proportional correlation to GLUT1 expression. The findings demonstrate the broad applicability of these molecular probes for optical imaging of tumors and glucose-related pathologies.
authors.affiliation: Department of Biomedical Engineering, State Key Laboratory of Natural Medicines School of Life Science and Technology, China Pharmaceutical University, Nanjing, China. guyueqingsubmission@hotmail.com
authors.forename: Jing
authors.initials: J
authors.lastname: Guo
authors.forename: Changli
authors.initials: C
authors.lastname: Du
authors.forename: Lingling
authors.initials: L
authors.lastname: Shan
authors.forename: Hongyan
authors.initials: H
authors.lastname: Zhu
authors.forename: Bing
authors.initials: B
authors.lastname: Xue
authors.forename: Zhiyu
authors.initials: Z
authors.lastname: Qian
authors.forename: Samuel
authors.initials: S
authors.lastname: Achilefu
authors.forename: Yueqing
authors.initials: Y
authors.lastname: Gu
mesh_terms: D000818:Animals; D002232:Carbocyanines / Q000138:chemical synthesis / Q000493:pharmacokinetics; D004396:Coloring Agents; D003847:Deoxyglucose / Q000737:chemistry; D005260:Female; D005456:Fluorescent Dyes / Q000737:chemistry; D005944:Glucosamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051272:Glucose Transporter Type 1 / Q000378:metabolism; D006801:Humans; D008325:Mammary Neoplasms, Experimental / Q000175:diagnosis* / Q000378:metabolism; D051379:Mice; D008819:Mice, Nude; D019265:Spectroscopy, Near-Infrared; D014018:Tissue Distribution; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
chemical_list: D002232:Carbocyanines; D004396:Coloring Agents; D005456:Fluorescent Dyes; D051272:Glucose Transporter Type 1; C576751:ICG-Der-02-2DG; C576750:cypate-2DG; D003847:Deoxyglucose; D005944:Glucosamine