Comparison of three ¹⁸F-labeled carboxylic acids with ¹⁸F-FDG of the differentiation tumor from inflammation in model mice.
Comparison of three ¹⁸F-labeled carboxylic acids with ¹⁸F-FDG of the differentiation tumor from inflammation in model mice.
复制标题
三种F-18标记羧酸与F-18-FDG对模型小鼠肿瘤与炎症分化的比较
DOI：
10.1186/s12880-016-0110-7
复制
发表时间：
2016-01-12
影响因子：
2.7
通讯作者：
Li S
中科院分区：
文献类型：
--
作者：
Wang H;Tang G;Hu K;Huang T;Liang X;Wu Z;Li S
本研究的目的是比较葡萄糖类似物 2-18F-氟-2-脱氧-D-葡萄糖 (18F-FDG)、三种短 18F 标记的羧酸、18F-氟乙酸酯 (18F-FAC)、2-18F-氟丙酸 (18F-FPA) 和 4-(18F) 氟苯甲酸 (18F-FBA) 的特性和可行性，区分肿瘤和炎症。在正常昆明小鼠上测定 18F-FAC、 18F-FPA 和 18F-FBA 的生物分布，并在单独的荷瘤小鼠模型和炎症小鼠模型上使用这些示踪剂进行正电子发射断层扫描（PET）成像，并与 18F-FDG 进行比较。生物分布结果表明， 18F-FAC 和 18F-FPA 具有相似的生物分布特征，并且从大多数组织中缓慢的放射性清除（排除 18F-FAC 的体内脱氟作用），而 18F-FBA 在大多数组织中表现出较低的摄取和快速的清除。 18F-FDG、18F-FAC 和 18F-FPA 的 PET 成像显示肿瘤和炎症病变中的高摄取。注射后 60 分钟，肿瘤与炎症的比率分别为 18F-FDG 为 1.63±0.28、18F-FAC 为 1.20±0.38、18F-FPA 为 1.41±0.33。而18F-FBA/PET可观察到清晰的肿瘤图像，肿瘤与炎症病灶之间对比度高，肿瘤与炎症的比率最高（1.98±0.15）。我们的数据表明 18F-FBA 是一种很有前景的 PET 探针，可用于区分肿瘤和炎症。但需要对18F-FBA结构进行进一步修饰以改善其药代动力学。
The aim of this study was to compare the properties and feasibility of the glucose analog, 2-18F-fluoro-2-deoxy-D-glucose (18F-FDG), three short 18F-labeled carboxylic acids, 18F-fluoroacetate (18F-FAC), 2-18F-fluoropropionic acid (18F-FPA) and 4-(18F)fluorobenzoic acid (18F-FBA), for differentiating tumors from inflammation. Biodistributions of 18F-FAC, 18F-FPA and 18F-FBA were determined on normal Kunming mice, and positron emission tomography (PET) imaging with these tracers were performed on the separate tumor-bearing mice model and inflammation mice model in comparison with 18F-FDG. Biodistribution results showed that 18F-FAC and 18F-FPA had similar biodistribution profiles and the slow radioactivity clearance from most tissues excluding the in vivo defluorination of 18F-FAC, and 18F-FBA demonstrated a lower uptake and fast clearance in most tissues. PET imaging with 18F-FDG, 18F-FAC and 18F-FPA revealed the high uptake in both tumor and inflammatory lesions. The ratios of tumor-to-inflammation were 1.63 ± 0.28 for 18F-FDG, 1.20 ± 0.38 for 18F-FAC, and 1.41 ± 0.33 for 18F-FPA at 60 min postinjection, respectively. While clear tumor images with high contrast between tumor and inflammation lesion were observed in 18F-FBA/PET with the highest ratio of tumor-to-inflammation (1.98 ± 0.15). Our data demonstrated 18F-FBA is a promising PET probe to distinguish tumor from inflammation. But the further modification of 18F-FBA structure is required to improve its pharmacokinetics.