Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and In vitro Evaluation of 99mTc-diglucosediethylenetriamine (DGTA) as a Potential Tumor Imaging Agent

  • Lee, Sang-Ju (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine) ;
  • Oh, Seung-Jun (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine) ;
  • Kim, Jung-Young (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine) ;
  • Ryu, Jin-Sook (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine) ;
  • Kim, Seog-Young (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine) ;
  • Moon, Dae-Hyuk (Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine)
  • Received : 2011.05.01
  • Accepted : 2011.06.05
  • Published : 2011.07.20
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Abstract

Using a single step chemical synthesis, we synthesized the potential tumor imaging agent $^{99m}Tc$-diglucose-diethylenetriamine (DGTA) from diethylenetriamine and natural D-glucose. 10 min Incubation of 10 mg of precursor with 50 ${\mu}g$ of $SnCl_2{\cdot}2H_2O$ at room temperature yielded over 95% of $^{99m}Tc$ labeling. The stability for 6 hours in saline or human plasma was over 90%. In vitro tumor cell uptake assays using the SNU-C5 and 9 L cell lines showed that, in 0-400 mg/dL glucose medium, cell uptake of $^{99m}Tc$-DGTA was 1.5-8 times higher than that of [$^{18}F$]FDG. Moreover, [$^{18}F$]FDG uptake was dependent on glucose concentration in the medium, whereas cellular uptake of $^{99m}Tc$-DGTA was not dependent on glucose concentration, suggesting that the two compounds have different uptake mechanisms by tumor cells.

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