Comparison of neara??infrared fluorescent deoxyglucose probes with different dyes for tumor diagnosis in vivo

摘要

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 neara??infrared fluorescent dyes, Cypate and ICGa??Dera??02, with different water solubility, were conjugated to 2a??aminoa??2a??deoxya??da??glucose (2DG) to form Cypatea??2DG and ICGa??Dera??02a??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 ICGa??Dera??02a??2DG with higher hydrophilicity was cleared faster by kidneys than the more lipophilic Cypatea??2DG. Cypatea??2DG had slower but stronger tumor targeting ability compared with ICGa??Dera??02a??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 Cypatea??2DG in tumors was assessed in MCFa??7/estradiol, U87MG, MCFa??7 and MDAa??MBa??435 tumor xenografts, which express different levels of GLUT1. The results show that both Cypatea??2DG and ICGa??Dera??02a??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 glucosea??related pathologies. Copyright ?? 2012 John Wiley & Sons, Ltd.