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Synthesis and Biodistribution of a New 99m Tc‐oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging
Author(s) -
Lin Xiao,
Jin Zhonghui,
Ren Jialei,
Pang Yan,
Zhang Weifang,
Huo Jinfeng,
Wang Xuebin,
Zhang Junbo,
Zhang Yanyan
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01280.x
Subject(s) - biodistribution , chemistry , single photon emission computed tomography , ligand (biochemistry) , radiochemistry , technetium 99m , dithiocarbamate , positron emission tomography , in vitro , nuclear medicine , biochemistry , scintigraphy , receptor , organic chemistry , medicine
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.