正电子发射型计算机断层显像剂^(18)F-FEA-Erlotinib与^(11)C-Erlotinib在HCC827荷瘤小鼠中的显像效果对比研究  

Comparative imaging study of two positron emission computed tomography tracers of ^(18)F-FEA-Erlotinib and ^(11)C-Erlotinib in HCC827 tumor-bearing nude mice

作　　者：黄顺[1,2] 韩彦江[2] 胡孔珍[2] 陈莉 孙朋辉[2] 吴湖炳 王全师[2] 赵肃清[1] 郑希[1] 

机构地区：[1]广东工业大学轻工化工学院,广州510006 [2]南方医科大学南方医院正电子发射型计算机断层中心,广州510515

出　　处：《中国临床药理学杂志》2018年第5期535-538,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家自然科学基金资助项目(81701729);广东省科技计划基金资助项目(2014A020212175);广东省医学科研基金资助项目(A2015525)

摘　　要：目的通过对比[~18F]氟乙基-埃罗替尼与[~11C]埃罗替尼在HCC827荷瘤鼠中的正电子发射型计算机断层(PET)显像,评价新PET显像剂~18F-FEAErlotinib的应用潜力。方法经一步亲核取代反应制得~18F-FEA-Erlotinib,而~11C-Erlotinib经[~11C]碘代甲烷(~11CH_3I)甲基化反应合成;先由~18F-FEAErlotinib在HCC827荷瘤鼠中进行1 h Micro-PET动态显像,探索其体内生物分布并确定最佳显像时间;然后分别进行~18F-FEA-Erlotinib与~11C-Erlotinib的1h静态显像,并勾画感兴趣区域(ROI),测定每克组织百分注射剂量率(%ID/g),进行半定量分析。结果经动态显像结果确定1 h为最佳显像时间。1 h静态显像中,~18F-FEA-Erlotinib图像中,肿瘤边界清晰,分辨率、对比度高。1 h静态显像半定量研究发现,~18F-FEA-Erlotinib显像中,肿瘤/脑、肿瘤/肺、肿瘤/骨骼、肿瘤/肌肉的比值分别为5.87±1.21,2.97±0.58,3.33±0.60,3.80±0.72;~11C-Erlotinib显像中,肿瘤/脑、肿瘤/肺、肿瘤/骨骼、肿瘤/肌肉的比值分别为5.48±1.45,1.10±0.34,2.63±0.54,2.10±0.63。结论~18F-FEA-Erlotinib显像肿瘤摄取高,靶/非靶比值较~11C-Erlotinib显像更高,显像清晰,具有较好应用潜力。Objective To evaluate the imaging study of two positron emission computed tomography （PET） tracers of is F - fluoroethyl （FEA） - Erlotinib and 11C - Erlotinib in HCC827 tumor - bearing nude mice. Methods The 18F- FEA- Erlotinib and 11C- Erlotinib were synthe- sized by nucleophile substitution reactions. The dynamic micro - PET/CT imaging of 18F - FEA - Erlotinib for 1 h was performed in HCC827 tumor -bearing mice to evaluate the in vivo biological distribution and determine the best imaging time. Static scan of lS F - FEA - Erlotinib and 11C - Erlotinib were performed after 1 h injection. The regions of interest （ROIs） were sketched and the semi -quantitative analysis was conduc- ted by the percentage activity of injection dose per gram of tissue （ % ID/g） . Results Dynamic micro - PET/CT imaging analysis revealed that the best static imaging time was 1 h. The resolution and con- trast were good and the tumor boundaries were clear in the 18F - FEA -Erlotinib static images. In the semi - quantitative analysis, the ratios of tumor/brain, tumor/lung, tumor/bone and tumor/muscle ratios were 5.87 ± 1.21, 2.97±0. 58, 3.33± 0. 60 and 3. 80± 0. 72 respectively for 18F - FEA - Erlotinib. Meanwhile, the ratios of the same tissues were 5.48 ±1.45, 1.10 ±0. 34, 2. 63 ± 0. 54 and 2. 10 ± 0. 63 respectively for n C -Erlotinib. The resolution of 18F- FEA- Erlotinib imaging was better than 1JC -Erlotinib images. Conclusion The uptake of 18F - FEA - Erlotinib in HCC827 tumor was visual obviously. The image resolution and the target/non- target ratio of 18F- FEA- Erlotinib was higher than 11C -Erlotinib.

关 键 词：非小细胞肺癌 HCC827细胞 [18F]氟乙基-埃罗替尼 [11C]埃罗替尼 正电子发射型计算机断层显像 

分 类 号：R97[医药卫生—药品]