Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging
Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging
复制标题
用于肿瘤成像的新型 99mTc-oxo 复合物与脱氧葡萄糖二硫代氨基甲酸酯的合成和生物分布
DOI：
10.1111/j.1747-0285.2011.01280.x
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发表时间：
2012-03-01
影响因子：
3
通讯作者：
Zhang, Yanyan
中科院分区：
文献类型：
--
作者：
Lin, Xiao;Jin, Zhonghui;Zhang, Yanyan
The deoxyglucose dithiocarbamate (DGDTC) was radiolabeled with 99mTc(V)-glucoheptonate (GH), for the potential use as radiopharmaceuticals for tumor imaging. For labeling, 99mTcO-DGDTC was prepared by ligand-exchange reaction with 99mTc-GH. The radiochemical purity of the 99mTcO-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 degrees C for 15 min to achieve high radiochemical purity. In vitro cell studies showed there was an increase in the uptake of 99mTcO-DGDTC as a function of incubation time and the cellular uptake of 99mTcO-DGDTC was possibly mediated by way of a d-glucose mechanism. The biodistribution of 99mTcO-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 99mTc radiolabeled glucose derivatives, 99mTcO-DGDTC showed the highest tumor uptake and good tumor/muscle ratios. The tumor/muscle ratio of 99mTcO-DGDTC uptake was higher than that of [18F] FDG uptake. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in tumor sites, suggesting 99mTcO-DGDTC would be a promising candidate for tumor imaging.
