Synthesis and biodistribution of a new (99m) Tc-oxo complex with deoxyglucose dithiocarbamate for tumor imaging.

Abstract

The deoxyglucose dithiocarbamate (DGDTC) was radiolabeled with (99m) Tc(V)-glucoheptonate (GH), for the potential use as radiopharmaceuticals for tumor imaging. For labeling, (99m) TcO-DGDTC was prepared by ligand-exchange reaction with (99m) Tc-GH. The radiochemical purity of the (99m) TcO-DGDTC complex was over 90% by thin-layer chromatography and high-performance liquid chromatography, without any notable decomposition at room temperature over a period of 6 h. Its partition coefficient indicated that it was a hydrophilic complex. The ligand-exchange reaction occured at neutral condition and under 100 °C for 15 min to achieve high radiochemical purity. In vitro cell studies showed there was an increase in the uptake of (99m) TcO-DGDTC as a function of incubation time and the cellular uptake of (99m) TcO-DGDTC was possibly mediated by way of a d-glucose mechanism. The biodistribution of (99m) TcO-DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with good uptake and excellent retention. As compared with other reported (99m) Tc radiolabeled glucose derivatives, (99m) TcO-DGDTC showed the highest tumor uptake and good tumor/muscle ratios. The tumor/muscle ratio of (99m) TcO-DGDTC uptake was higher than that of [(18) F] FDG uptake. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in tumor sites, suggesting (99m) TcO-DGDTC would be a promising candidate for tumor imaging.

• Authors: Xiao Lin, Zhonghui Jin, Jialei Ren, Yan Pang, Weifang Zhang, Jinfeng Huo, Xuebin Wang, Junbo Zhang, Yanyan Zhang
• Journal: Chemical biology & drug design (Chem Biol Drug Des) Vol. 79 Issue 3 Pg. 239-45 (Mar 2012) ISSN: 1747-0285 [Electronic] England
• PMID: 22136603 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2011 John Wiley & Sons A/S.

Chemical References

• Carbamates
• Coordination Complexes
• Organotechnetium Compounds
• Radiopharmaceuticals
• deoxyglucose dithiocarbamate
• Fluorodeoxyglucose F18
• Deoxyglucose

Topics

• Animals
• Carbamates (chemistry)
• Cell Line, Tumor
• Coordination Complexes (chemical synthesis, chemistry, pharmacokinetics)
• Deoxyglucose (analogs & derivatives, chemistry)
• Fluorodeoxyglucose F18 (chemistry, pharmacokinetics)
• Mice
• Mice, Nude
• Neoplasms (diagnostic imaging)
• Organotechnetium Compounds (chemistry)
• Radiopharmaceuticals (chemical synthesis, chemistry, pharmacokinetics)
• Tissue Distribution
• Tomography, Emission-Computed, Single-Photon