JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2020
·Vol. 326
·期 1
·575-581
·
IF 1.137
Cai Fei,Yan Heng,Fan Wenbin,Li Shihong,Xu Jianfeng,Wang Zheng,Tang Xiaobin
A mild HPLC method for the quality control of [ 18 F]sodium fluoride solution for injection was developed. The method used anion exchange column for separation, UV and online radio-detectors for fluoride content and fluorine-18 determination. A mixture of 100 mM sodium acetate and 25 mM sodium chloride was chosen as mobile phase. The method was validated for system suitability, specificity, fluoride concentration and radiochemical purity determination with good linearity, accuracy and precision. The good robustness of the system was also verified, enabling routine analysis of fluoride content and radiochemical purity of the [ 18 F]sodium fluoride product.
研究领域:
药学
·
核医学
✓ 已验证
DOI
高影响因子
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2017
·Vol. 312
·期 3
·599-607
·
IF 1.282
Liu Guiqing,Wang Wei,Lin Jianguo,Li Ke,Lv Gaochao,Zhao Xueyu,Wang Shanshan,Luo Shineng,Qiu Ling
16α- 18 F-fluoroestradiol ( 18 F-FES) has been developed as a promising positron emission tomography (PET) imaging agent for targeting estrogen receptor positive (ER + ) breast cancer in the clinical trial. However, the radiosynthesis of 18 F-FES often requires two steps and tough experimental conditions. Therefore, a new estradiol derivative ( 18 F-AmBF 3 -ES) was prepared by an efficient one-step 18 F-radiolabeling method. The tracer was obtained in high yield (~65%) and excellent radiochemical purity (>98%) within 30 min. The uptake rate of 18 F-AmBF 3 -ES in ER + cells was about 3.5% at 30 min. The results suggested that the tracer may be a potential PET imaging agent for ER + breast cancer.
研究领域:
医学影像学
·
肿瘤学
·
核化学
✓ 已验证
DOI
高影响因子
RSC Advances
·
2021
·Vol. 11
·期 31
·18738-18747
·
IF 3.361
Dingyao Gao,Yinxing Miao,Siqin Ye,Chunmei Lu,Gaochao Lv,Ke Li,Chunjing Yu,Jianguo Lin,Ling Qiu
The expression level of γ-glutamyltranspeptidase (GGT) in some malignant tumors is often abnormally high, while its expression is low in normal tissues. Therefore, GGT is considered as a key biomarker for cancer diagnosis. Several GGT-targeting fluorescence probes have been designed and prepared, but their clinical applications are limited due to their shallow tissue penetration. Considering the advantages of positron emission tomography (PET) such as high sensitivity and deep tissue penetration, we designed a novel PET imaging probe for targeted monitoring of the expression of GGT in living subjects, ([18F]γ-Glu-Cys-PPG(CBT)-AmBF3)2, hereinafter referred to as ([18F]GCPA)2. The non-radioactive probe (GCPA)2 was synthesized successfully and [18F]fluorinated rapidly via the isotope exchange method. The radiotracer ([18F]GCPA)2 could be obtained within 0.5 h with the radiochemical purity over 98% and the molar activity of 10.64 ± 0.89 GBq μmol−1. It showed significant difference in cellular uptake between GGT-positive HCT116 cells and GGT-negative L929 cells (2.90 ± 0.12% vs. 1.44 ± 0.15% at 4 h, respectively). In vivo PET imaging showed that ([18F]GCPA)2 could quickly reach the maximum uptake in tumor (4.66 ± 0.79% ID g−1) within 5 min and the tumor-to-muscle uptake ratio was higher than 2.25 ± 0.08 within 30 min. Moreover, the maximum tumor uptake of the control group co-injected with the non-radioactive probe (GCPA)2 or pre-treated with the inhibitor GGsTop decreased to 3.29 ± 0.24% ID g−1 and 2.78 ± 0.32% ID g−1 at 10 min, respectively. In vitro and in vivo results demonstrate that ([18F]GCPA)2 is a potential PET probe for sensitively and specifically detecting the expression level of GGT.
研究领域:
医学影像学
·
肿瘤学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
MOLECULAR DIVERSITY
·
2025
·
IF 3.8
Miao Wenjun,Yang Meixian,Peng Zhiping,Xia Zhu,Zhang Xiaoyang,Chen Yi,Jia Jianhua
Cyclooxygenase-2 (COX-2) plays vital roles in promoting angiogenesis, tissue invasion, and resistance to apoptosis, so it has become an attractive biomarker for imaging and therapy of cancer. Numerous radio-tracers for detection of COX-2 in vivo have been reported, but no one has been successfully applied in clinic. In this study, the radiosynthesis and evaluation of [ 18 F] 6 , containing a 1,5-diarylpyrrole structure, as a radiotracer for imaging of COX-2 is described. [ 18 F] 6 was prepared within 90 min synthesis time with radiochemical yields (RCYs) of 2–6% (n = 7, decay corrected) from [ 18 F]fluoride by a one-step 18 F-trifluoromethylation reaction. After purification by high performance liquid chromatography (HPLC), its radiochemical purity (RCP) was higher than 98%, and the molar activity was 156–210 MBq/mmol. The stability of [ 18 F] 6 was determined by incubation in saline and fetal bovine serum (FBS) in vitro, showing excellent stability in 4 h. The specific binding of [ 18 F] 6 was evaluated using MCF-7 cells (COX-2 positive cells) in vitro, where the radiotracer uptake was blocked in the presence of Celecoxib (a commonly used COX-2 inhibitor). However, no tumor accumulation of [ 18 F] 6 could be observed by micro-PET/CT studies on MCF-7 tumor-bearing mice in vivo. This may be due to the insufficient molar activity of [ 18 F] 6, or inadequate expression of COX-2 in MCF-7. In conclusion, optimizations of radiosynthesis and evaluations of specific binding in suitable model are further still needed to verify the potential of [ 18 F] 6 as a COX-2 imaging agent.
研究领域:
分子影像学
·
核医学
·
药物化学
·
肿瘤学
·
放射化学
✓ 已验证
DOI
PubMed
高影响因子
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