Synthesis and preliminary evaluation of 18F-AIF-NOTA-G-TMTP1 for PET imaging on nude mice bearing high-metastatic potential hepatoma cells
10.3760/cma.j.issn.2095-2848.2015.03.004
- VernacularTitle:18F-AlF-NOTA-G-TMTP1的合成及对高转移潜能肝癌细胞荷瘤鼠的显像研究
- Author:
Yesen LI
;
Deliang ZHANG
;
Xianzhong ZHANG
;
Tianxing PENG
;
Wenbo FAN
;
Heping YAN
;
Hua WU
- Publication Type:Journal Article
- Keywords:
Liver neoplasms;
AlF-NOTA-G-TMTP1;
Fluorine radioisotopes;
Chemical synthesis;
Tomography,emission-computed;
Mice,nude
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2015;35(5):351-354
- CountryChina
- Language:Chinese
-
Abstract:
Objective To synthesize 18F-AlF-NOTA-G-TMTP1 and evaluate its potential for PET imaging on nude mice bearing high-metastatic potential hepatoma cells.Methods NOTA-G-TMTP1 was synthesized by the standard Fmoc-solid phase synthetic protocols and radiolabeled with 18F using NOTA-AlF chelation method.The nude mice models bearing low-metastatic potential HCC97L and high-metastatic potential HCCLM3 xenografts were established separately.The tumor-targeting characteristics of 18F-AlF-NOTA-G-TMTP1 were assessed by microPET/CT and biodistribution assay.Results NOTA-G-TMTP1 was labeled with 18F in one step with (25±6)％ labeling yield (n=5).The radiochemical purity of 18F-AlF-NOTA-G-TMTP1 was more than 95％ with a specific activity more than 11.1 GBq/μmol.The octanol/water partition coefficient (logP) for 18F-AlF-NOTA-G-TMTP1 was-3.166±0.022.The tumor to muscle ratios were 1.8± 0.4 and 4.7±0.2 at 35 min post injection for HCC97L and HCCLM3,respectively.The uptake of 18F-AlF-NOTA-G-TMTP1 in HCCLM3 tumor was inhibited (61.4％) by unlabeled G-TMTP1.Conclusion 18F-AlF-NOTA-G-TMTP1 has been successfully synthesized.It shows specific uptake by tumor induced by the high-metastatic potential hepatoma cells.
