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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 7
BKCSDE 32(7)
July 20, 2011 

Synthesis and In vitro Evaluation of 99mTc-diglucosediethylenetriamine (DGTA) as a Potential Tumor Imaging Agent
Sang Ju Lee, Seung Jun Oh, * Jung Young Kim, Jin Sook Ryu, Seog-Young Kim, Dae Hyuk Moon
Glucose, 99mTc, SPECT, Tumor, Tumor imaging
Using a single step chemical synthesis, we synthesized the potential tumor imaging agent 99mTc-diglucosediethylenetriamine (DGTA) from diethylenetriamine and natural D-glucose. 10 min Incubation of 10 mg of precursor with 50 μg of SnCl2·2H2O at room temperature yielded over 95% of 99mTc 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 99mTc-DGTA was 1.5-8 times higher than that of [18F]FDG. Moreover, [18F]FDG uptake was dependent on glucose concentration in the medium, whereas cellular uptake of 99mTc-DGTA was not dependent on glucose concentration, suggesting that the two compounds have different uptake mechanisms by tumor cells.
2410 - 2412
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