Xie Wen-Hui, Zhang Bin, Wang Li-Hua, Liu Ci-Yi, Chang Cheng, Lei Bei, Wu Yi-Wei
1 Department of Nuclear Medicine, The First Affiliated Hospital of Soochow University. Suzhou , Jiangsu, P.R. China .
Cancer Biother Radiopharm. 2015 Apr;30(3):117-24. doi: 10.1089/cbr.2014.1765. Epub 2015 Feb 25.
To investigate the biodistribution and single-photon emission computed tomography (SPECT) imaging of (99m)Tc-labeled arginine-glutamic acid-threonine (RET) and arginine-glutamic acid-glycine (REG) in nude mice bearing human lung cancer xenografts.
RET and REG were labeled directly with (99m)Tc and their binding efficiency to tumor cells was measured in human nonsmall cell lung cancer H1299 cells. After intravenously injecting (99m)Tc-RET and (99m)Tc-REG into normal mice and nude mice bearing human lung cancer xenografts, their biodistribution was measured at different postinjection times, and percentages of injected dose per gram tissue (% ID/g) of organs of interest were calculated. The mice bearing H1299 lung cancer xenografts were scanned by SPECT at different times following the (99m)Tc-RET or (99m)Tc-REG injection.
The radiochemical purity of (99m)Tc-RET and (99m)Tc-REG was 93.15%±2.02% and 92.90%±2.86%, respectively. The binding rate of (99m)Tc-RET and (99m)Tc-REG to H1299 cells was 3.56%±0.37% and 2.32%±0.31%, respectively. The uptake of (99m)Tc-RET and (99m)Tc-REG in tumor was 4.96±1.05% ID/g at 4 hours postinjection and 1.95±0.73% ID/g at 2 hours postinjection, respectively. Tumors in nude mice could be best imaged at 4.5-6 hours postinjection of (99m)Tc-RET.
(99m)Tc-RET has a higher binding rate to H1299 cells than (99m)Tc-REG and might be used as a potential lung cancer imaging agent.
研究（99m）Tc标记的精氨酸-谷氨酸-苏氨酸（RET）和精氨酸-谷氨酸-甘氨酸（REG）在人肺癌异种移植裸鼠中的生物分布及单光子发射计算机断层扫描（SPECT）成像。
RET和REG直接用（99m）Tc标记，并在人非小细胞肺癌H1299细胞中测定它们与肿瘤细胞的结合效率。将（99m）Tc-RET和（99m）Tc-REG静脉注射到正常小鼠和人肺癌异种移植裸鼠体内后，在注射后不同时间测量其生物分布，并计算感兴趣器官每克组织的注射剂量百分比（%ID/g）。在注射（99m）Tc-RET或（99m）Tc-REG后的不同时间，对荷H1299肺癌异种移植瘤的小鼠进行SPECT扫描。
（99m）Tc-RET和（99m）Tc-REG的放射化学纯度分别为93.15%±2.02%和92.90%±2.86%。（99m）Tc-RET和（99m）Tc-REG与H1299细胞的结合率分别为3.56%±0.37%和2.32%±0.31%。注射后4小时，（99m）Tc-RET和（99m）Tc-REG在肿瘤中的摄取量分别为4.96±1.05%ID/g和1.95±0.73%ID/g；注射后2小时，（99m）Tc-REG在肿瘤中的摄取量为1.95±0.73%ID/g。注射（99m）Tc-RET后4.5 - 6小时，裸鼠体内的肿瘤成像效果最佳。
（99m）Tc-RET与H1299细胞的结合率高于（99m）Tc-REG，可能用作潜在的肺癌显像剂。
