Center for Neuro-Medicine, Brain Science Institute , Korea Institute of Science and Technology , Seoul , 02792 , Korea.
Center for Systems Biology, Massachusetts General Hospital , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Bioconjug Chem. 2018 Oct 17;29(10):3394-3401. doi: 10.1021/acs.bioconjchem.8b00558. Epub 2018 Sep 12.
Fluorescent tracers for glucose-uptake monitoring could be used as chemical tools for diagnosis and for discovery of novel therapeutic agents via the development of phenotypic screening systems. Here we present a new near-infrared fluorescent glucose tracer, Glc-SiR-COH, for monitoring the cellular glucose uptake. By conjugating glucosamine with two different silicon rhodamine fluorochromes, we found that the net charge of fluorochromes has considerable effects on cellular uptake of the probe. Competition assay with d/l-glucose as well as Western blot analysis implied GLUT-dependent uptake mechanism of this probe. Finally, Glc-SiR-COH not only differentiates cancer cells from normal cells, but also allows monitoring anticancer effects in live cells.
用于葡萄糖摄取监测的荧光示踪剂可用作化学工具，通过表型筛选系统的开发用于诊断和新型治疗剂的发现。在这里，我们提出了一种新的近红外荧光葡萄糖示踪剂 Glc-SiR-COH，用于监测细胞葡萄糖摄取。通过将葡糖胺与两种不同的硅罗丹明荧光染料缀合，我们发现荧光染料的净电荷对探针的细胞摄取有相当大的影响。用 d/l-葡萄糖进行竞争测定以及 Western blot 分析表明，该探针具有 GLUT 依赖性摄取机制。最后，Glc-SiR-COH 不仅可以区分癌细胞与正常细胞，还可以在活细胞中监测抗癌效果。
