Wang Hui, Yu Jin-Ming, Song Xian-Rang, Yang Guo-Ren, Mu Dian-Bin, Zhao Shu-Qiang, Wang Xing-Wu, Wei Ling, Liu Yong-Lei, Song Bao, Fu Zheng, Teng Xue-Peng
Department of Radiation Oncology, Shandong Tumor Hospital, Jinan 250117, China.
Zhonghua Zhong Liu Za Zhi. 2008 May;30(5):343-6.
To investigate the value of 11C-PD153035 as an EGFR imaging agent in C6 tumor-bearing rat.
The tumor-bearing rats were generated by subcutaneous injection of glioma C6 cells. Positron emission tomography/computer tomography (PET/CT) scans started as soon as intravenous injection of 11C-PD153035 (15-20 MBq/0.3 ml) was completed, images were collected continuously. The region of interest (ROI) was used to study the percentage of radioactivity in major organs and implanted tumors in the rats. The accumulation and blocking study in vitro was completed.
There were significant differences in 11C-PD153035 uptake among major organs. The maximum uptake in the organs ranked in the following order: liver > gastrointestinal tract > kidney > lung > brain > muscle. Radioactivity could be also observed in the tumors. The radioactivity ratio (T/NT, target/non-target) peaked (4.15) at 40 - 50 min post injection. The in vitro blocking study showed that 11C-PD153035 uptaken by C6 cells could be blocked by PD153035.
The results of this study show that 11C-PD153035 can be uptaken by EGFR-expressing tumors. 11C-PD153035 has a potential as a bioprobe to yield useful information for both diagnosis and therapy of tumors. However, the high concentration of 11C-PD153035 in the gastrointestinal tract is unfavorably affecting the tumor detection in these organs.
研究11C-PD153035作为表皮生长因子受体(EGFR)显像剂在荷C6肿瘤大鼠中的应用价值。
通过皮下注射胶质瘤C6细胞建立荷瘤大鼠模型。静脉注射11C-PD153035(15 - 20 MBq/0.3 ml)完毕后即刻开始进行正电子发射断层扫描/计算机断层扫描(PET/CT),持续采集图像。采用感兴趣区(ROI)研究大鼠主要器官及植入肿瘤中的放射性百分比。完成体外摄取及阻断研究。
主要器官对11C-PD153035的摄取存在显著差异。各器官的最大摄取量排序如下:肝脏>胃肠道>肾脏>肺>脑>肌肉。肿瘤部位也可观察到放射性。放射性比值(T/NT,靶/非靶)在注射后40 - 50分钟达到峰值(4.15)。体外阻断研究显示,C6细胞摄取的11C-PD153035可被PD153035阻断。
本研究结果表明,11C-PD153035可被表达EGFR的肿瘤摄取。11C-PD153035有潜力作为一种生物探针,为肿瘤的诊断和治疗提供有用信息。然而,胃肠道中11C-PD153035的高浓度对这些器官中的肿瘤检测产生不利影响。