1. Cyanine-based 1-amino-1-deoxyglucose as fluorescent probes for glucose transporter mediated bioimaging.
- Author
-
Xu, Hu, Liu, Xinyu, Yang, Jinna, Liu, Ran, Li, Taoli, Shi, Yunli, Zhao, Hongxia, and Gao, Qingzhi
- Subjects
- *
GLUCOSE transporters , *FLUORESCENT probes , *BIO-imaging sensors , *CYANINES , *QUERCETIN , *FLUORIMETRY - Abstract
Two novel cyanine-based 1-amino-1-deoxy-β-glucose conjugates (Glu-1N-Cy3 and Glu-1N-Cy5) were designed, synthesized and their fluorescence characteristics were studied. Both Glu-1N-Cy3 and Glu-1N-Cy5 accumulate in living HT29 human colon cancer cells, which overexpress glucose transporters (GLUTs). The cellular uptake of the bioprobes was inhibited by natural GLUT substrate d -glucose and 2-deoxy- d -glucose. The GLUT specificity of the probes was validated with quercetin, which is both a permeant substrate via GLUTs and a high-affinity inhibitor of GLUT-mediated glucose transport. Competitive fluorometric assay for GLUT substrate cell uptake revealed that Glu-1N-Cy3 and Glu-1N-Cy5 are 5 and 10 times more sensitive than 2-NBDG, a leading fluorescent glucose bioprobe. This study provides fundamental data supporting the potential of these two conjugates as new powerful tools for GLUT-mediated theranostics, in vitro and in vivo molecular bioimaging and drug R&D. [ABSTRACT FROM AUTHOR]
- Published
- 2016
- Full Text
- View/download PDF