Wang Hongliang, Tang Ganghua, Hu Kongzhen, Huang Tingting, Liang Xiang, Wu Zhifang, Li Sijin
Department of Nuclear Medicine, First Hospital of Shanxi Medical University, Taiyuan, People's Republic of China.
Department of Nuclear Medicine, The First Affiliated Hospital of Sun Yat-Sen University, Guangzhou, People's Republic of China.
BMC Med Imaging. 2016 Jan 12;16:2. doi: 10.1186/s12880-016-0110-7.
The aim of this study was to compare the properties and feasibility of the glucose analog, 2-(18)F-fluoro-2-deoxy-D-glucose ((18)F-FDG), three short (18)F-labeled carboxylic acids, (18)F-fluoroacetate ((18)F-FAC), 2-(18)F-fluoropropionic acid ((18)F-FPA) and 4-((18)F)fluorobenzoic acid ((18)F-FBA), for differentiating tumors from inflammation.
Biodistributions of (18)F-FAC, (18)F-FPA and (18)F-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 (18)F-FDG.
Biodistribution results showed that (18)F-FAC and (18)F-FPA had similar biodistribution profiles and the slow radioactivity clearance from most tissues excluding the in vivo defluorination of (18)F-FAC, and (18)F-FBA demonstrated a lower uptake and fast clearance in most tissues. PET imaging with (18)F-FDG, (18)F-FAC and (18)F-FPA revealed the high uptake in both tumor and inflammatory lesions. The ratios of tumor-to-inflammation were 1.63 ± 0.28 for (18)F-FDG, 1.20 ± 0.38 for (18)F-FAC, and 1.41 ± 0.33 for (18)F-FPA at 60 min postinjection, respectively. While clear tumor images with high contrast between tumor and inflammation lesion were observed in (18)F-FBA/PET with the highest ratio of tumor-to-inflammation (1.98 ± 0.15).
Our data demonstrated (18)F-FBA is a promising PET probe to distinguish tumor from inflammation. But the further modification of (18)F-FBA structure is required to improve its pharmacokinetics.
本研究旨在比较葡萄糖类似物2-(18)F-氟-2-脱氧-D-葡萄糖((18)F-FDG)、三种短链(18)F标记的羧酸,即(18)F-氟乙酸((18)F-FAC)、2-(18)F-氟丙酸((18)F-FPA)和4-((18)F)氟苯甲酸((18)F-FBA)在区分肿瘤与炎症方面的特性和可行性。
测定(18)F-FAC、(18)F-FPA和(18)F-FBA在正常昆明小鼠体内的生物分布,并与(18)F-FDG比较,在单独的荷瘤小鼠模型和炎症小鼠模型上用这些示踪剂进行正电子发射断层扫描(PET)成像。
生物分布结果显示,(18)F-FAC和(18)F-FPA具有相似的生物分布特征,且除(18)F-FAC的体内脱氟外,大多数组织中的放射性清除缓慢,而(18)F-FBA在大多数组织中摄取较低且清除较快。用(18)F-FDG、(18)F-FAC和(18)F-FPA进行PET成像显示肿瘤和炎症病变均有高摄取。注射后60分钟时,(18)F-FDG的肿瘤与炎症比值为1.63±0.28,(18)F-FAC为1.20±0.38,(18)F-FPA为1.41±0.33。而(18)F-FBA/PET中肿瘤与炎症病变之间对比度高,能清晰显示肿瘤图像,肿瘤与炎症比值最高(1.98±0.15)。
我们的数据表明(18)F-FBA是一种有前景的用于区分肿瘤与炎症的PET探针。但需要对(18)F-FBA的结构进行进一步修饰以改善其药代动力学。