Wang Yue, Zhu Jingjing, Song Xiaoqing, Wang Xuebin, Yang Jigang, Zhang Junbo
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
Department of Nuclear Medicine, Beijing Friendship Hospital of Capital Medical University, Beijing, China.
Bioorg Med Chem Lett. 2014 Aug 15;24(16):3882-5. doi: 10.1016/j.bmcl.2014.06.051. Epub 2014 Jun 25.
The 2-[(3-carboxy-1-oxopropyl)amino]-2-deoxy-D-glucose (CPADG) was synthesized and radiolabeled with (99m)TcO4(-) to obtain the (99m)Tc-CPADG complex in high yield. It was stable over 6 h in saline at room temperature and in serum at 37 °C. The partition coefficient and electrophoresis results indicated that the complex was hydrophilic and cationic. In vitro cell studies showed there was an increase in the uptake of (99m)Tc-CPADG as a function of incubation time and (99m)Tc-CPADG was possibly transported via the glucose transporters. The biodistribution of (99m)Tc-CPADG in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 1.91 and 5.05 at 4h post-injection. Single photon emission computed tomography (SPECT) image studies showed there was an obvious accumulation in tumor sites, suggesting (99m)Tc-CPADG would be a promising candidate for tumor imaging.
合成了2-[(3-羧基-1-氧代丙基)氨基]-2-脱氧-D-葡萄糖(CPADG)，并用(99m)TcO4(-)进行放射性标记，以高收率获得(99m)Tc-CPADG络合物。它在室温下的盐溶液中以及在37℃的血清中6小时内稳定。分配系数和电泳结果表明该络合物具有亲水性且带正电荷。体外细胞研究表明，(99m)Tc-CPADG的摄取量随孵育时间增加，并且(99m)Tc-CPADG可能通过葡萄糖转运蛋白进行转运。(99m)Tc-CPADG在荷S 180肿瘤小鼠体内的生物分布表明，该络合物在肿瘤中高摄取并良好滞留。肿瘤/血液和肿瘤/肌肉比值随时间增加，注射后4小时达到1.91和5.05。单光子发射计算机断层扫描(SPECT)图像研究表明肿瘤部位有明显积聚，提示(99m)Tc-CPADG有望成为肿瘤显像剂。
