Journal
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Volume 474, Issue 2, Pages 240-246Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2016.03.133
Keywords
Fluorescent probe; Glucose transporter; Fluorometric competition; Cyanine-based glycoconjugate
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Funding
- Tianjin Municipal Applied Basic and Key Research Scheme of China [11JCYBJC14400, 12ZCDZSY11500, 13JCZD27500]
- Project of National Basic Research (973) Program of China [2015CB856500]
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Two novel cyanine-based 1-amino-1-deoxy-beta-glucose conjugates (Glu-1N-Cy3 and Glu-1N-Cy5) were designed, synthesized and their fluorescence characteristics were studied. Both Giu-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 per meant 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. (C) 2016 Elsevier Inc. All rights reserved.
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