MedChemComm
Research Article
pipetted and counted in a well γ-counter. The experiment Acknowledgements
was repeated three times. The partition coefficient, P, was
This work was financially supported, in part, by the National
Natural Science Foundation of China (21171024, 21541001).
calculated by using the following equation: P = (cpm in
octanol − cpm in background)/(cpm in buffer − cpm in back-
ground). The final partition coefficient value was expressed
as log P SD.
Notes and references
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Biodistribution studies
The mice models were established according to the literature
method.17 In brief, approximately 2 × 106 murine sarcoma
S180 cells (obtained from tumor mouse in ascites) were hypo-
dermically injected into the left front leg of Kunming female
mice. Over a week, tumors grew to 10–15 mm in diameter.
0.1 mL of 99mTcN-3a (3.7 × 105 Bq) was injected into the Kun-
ming female mice (18–20 g) bearing S180 tumor via a tail
vein. At 0.5 h, 2 h and 4 h post-injection, the mice were
sacrificed by neck dislocation. The tumor, other organs of
interest and blood were collected, weighed and measured for
radioactivity. The results were expressed as the percent up-
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standard deviation. The
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SPECT imaging studies
A dual-head SPECT (Skylight; Philips, Milpitas, CA, USA),
with a low-energy parallel-hole collimator (diameter 3.5 mm),
was used for SPECT imaging studies. 0.1 mL of 99mTcN-3b
(18.5 MBq) was injected intravenously through a tail vein into
mice (18–22 g) bearing S180 tumor. Static images were
obtained using 128 × 128 matrices at 4 h after injection.
Conclusion
In summary, two novel functionalized glucose dithiocarba-
mates (3a and 3b) were successfully synthesized via a “click
chemistry” route and their 99mTcN complexes were prepared
with high yields through a ligand-exchange reaction. They
were hydrophilic and stable in vitro. The preliminary in vivo
studies showed that both complexes were accumulated in the
tumor with good retention. Especially for 99mTcN-3b, the bio-
distribution and SPECT imaging studies in mice bearing
S180 tumor showed that it had appreciable tumor uptake
and a high tumor/muscle ratio. In the present case, it may be
of great interest to further investigate 99mTcN-3b as a poten-
tial radiotracer for tumor imaging.
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Conflict of interest
The author(s) confirm that this article content has no con-
flicts of interest.
23 R. Pasqualini, A. Duatti, E. Bellande, V. Comazzi, V. Brucato,
This journal is © The Royal Society of Chemistry 2016
Med. Chem. Commun., 2016, 7, 1381–1386 | 1385