Synthesis and biological evaluation of a <sup>99m</sup>Tc-labeled glucose derivative for tumor imaging

Abstract

<p indent="0mm">The development of novel tumor-imaging agents for single-photon-emission-computed tomography (SPECT) with good performance, simple preparation and low price is a hot topic in the field of radiopharmaceutical research. ^99mTc is the most widely used SPECT nuclide in clinic. In order to develop a novel ^99mTc-labeled tumor radiopharmaceuticals, in this study, a glucose derivative (CN6DG) containing isonitriles was synthesized and it was radiolabeled with ^99mTc to obtain the ^99mTc-CN6DG complex with high radiochemical purity (&gt;95%). The complex is hydrophilic (log<italic>D</italic>=−2.52±0.33) and has good stability <italic>in vitro </italic>and<italic> in vivo</italic>. <italic>In vitro</italic> cell-uptake assay showed that tumor cells uptake of the complex was related to glucose transporters. In S180 tumor-bearing mice <sc>2 h</sc> after injection, the tumor-uptake value was 0.75±0.12 %ID/g and the tumor/muscle, tumor/blood ratios were 4.41 and 18.75, respectively. In A549 tumor-bearing mice after <sc>2 h</sc> of post-injection, the tumor-uptake value was 2.62±0.23 %ID/g, which was higher than that of ^99mTc-CN5DG (1.48±0.23 %ID/g). Its tumor/blood (52.4 <italic>vs</italic>. 49.33) ratios and tumor/muscle ratios (6.89 <italic>vs</italic>. 24.67) were as good as that of ^99mTc-CN5DG. The SPECT/CT imaging results in S180 and A549 tumor-bearing mice showed that it had significant tumor uptakes, indicating that it is a promising tumor-imaging agent.