Automatic synthesis of N-succinimidyl 4-18F-fluorobenzoate and its utility for 18F labeled C2A donain of synaptotagmin I
10.3760/cma.j.issn.0253-9780.2010.06.015
- VernacularTitle:N-琥珀酰亚胺4-18F-氟苯甲酸酯的全自动化合成及用于突触结合蛋白C2A-GST的标记
- Author:
Yan-jie, HOU
;
Biao, LIU
;
Zi-zheng, WANG
;
Xu-dang, XU
;
Shao-hua, LI
;
Wei, TIAN
;
Feng, WANG
- Publication Type:Journal Article
- Keywords:
Succinimides;
Benzoates;
Fluorine radioisotopes;
Chemical synthesis;
Isotope labeling;
Glutathione transferases;
Apoptosis;
Radionuclide imaging
- From:Chinese Journal of Nuclear Medicine
2010;30(6):414-418
- CountryChina
- Language:Chinese
-
Abstract:
Objective To develop and optimize a module for the automatic production of N-succinimidyl-4-[18F] fluorobenzoate (18F-SFB) that is used for further 18F labelling C2A domain of Synaptotagmin Ⅰ . The conjugated compound was applied for detecting the tumor apoptosis in rabbit model after chemotherapy. Methods GE TRACERlab and TRACERlab FXF-N modules were modified and programmed to automatically produce 18 F-SFB which was further analyzed by high performance liquid chromatography (HPLC).C2A-glutathione S transferase (GST) was conjugated with 18F-SFB (18F-FB-C2A-GST) and subsequently purified by HPLC. Two rabbits grafted with VX2 lung cancer were first treated with chemotherapy and then,37 MBq of 18F-FB-C2A-GST was administered via the auricular vein. Serial PET/CT imagings were performed at 0.5, 1 and 2 h post-injection respectively. Tumor apoptosis was examined by pathological study. Results The TRACERlab FXFoG and TRACERlab FXF-N modules were successfully adapted to synthesize18F-SFB, with the radiochenmical yield (76.41 ±4.00)% (n = 10), the corrected yield (45.43 ±5.90 ) % and the radiochemical purity about 95%. The whole procedure for labeling 18 F-SFB was about 87 min.From PET/CT imagings, significant uptake was found in the tumor after chemotherapy, but no obvious up-take was found in heart, lungs and liver. HE staining demonstrated large number of apoptotic bodies within the tumor tissues. Conclusions 18 F-SFB can be automatically synthesized. 18F-FB-C2A-GST might be useful for the detection of apoptosis in tumor after chemotherapy.
