Novel <sup>99m</sup>Tc-Labeled Glucose Derivative for Single Photon Emission Computed Tomography: A Promising Tumor Imaging Agent
作者:Xuran Zhang、Qing Ruan、Xiaojiang Duan、Qianqian Gan、Xiaoqing Song、Sian Fang、Xiao Lin、Jin Du、Junbo Zhang
DOI:10.1021/acs.molpharmaceut.8b00415
日期:2018.8.6
cells in vitro, suggesting the mechanism of 99mTc-CN5DG into tumor cells was related to glucose transporters. Biodistribution studies in mice bearing A549 xenografts showed 99mTc-CN5DG had a high tumor uptake and high tumor-to-background ratios. SPECT/CT images further supported its ability for tumor imaging. As a cheap, conveniently made and widely available probe, 99mTc-CN5DG would become a potential
本研究合成了具有异腈基团的d-葡萄糖胺衍生物(CN5DG),选择与99m Tc配位制备99m Tc-CN5DG。可以容易地获得99m Tc-CN5DG,其放射化学纯度高(> 95%),并且在体外尿液中具有很好的体外稳定性和代谢稳定性。放射性示踪剂在体外对S180和A549肿瘤细胞中的葡萄糖和胰岛素给药呈阳性反应,表明99m Tc-CN5DG进入肿瘤细胞的机制与葡萄糖转运蛋白有关。在带有A549异种移植物的小鼠中的生物分布研究显示99mTc-CN5DG具有较高的肿瘤吸收率和较高的肿瘤与背景比率。SPECT / CT图像进一步支持了其对肿瘤成像的能力。99m Tc-CN5DG作为一种便宜,易于制造且广泛使用的探针,将成为潜在的“工作之马”,并成为99m Tc标记的放射性药物用于肿瘤检测的突破。