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1. 解放军总医院核医学科
2. 解放军总医院第一附属医院胸心外科
Published:01 November 2011
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[1]张锦明,张晓军,张宝石,刘健,王卉,孙志军,田嘉禾.自动化“点击合成”正电子标记肽类细胞凋亡显像剂~(18)F-Pen-peptide[J].核技术,2011,34(11):845-850.
ZHANG Jinming1 ZHANG Xiaojun1 ZHANG Baoshi2 LIU Jian1 WANG Hui1 SUN Zhijun1 TIAN Jiahe1 1. Automated "click chemistry" synthesis of 18F-Pen-peptide as an apoptosis imaging agent[J]. Nuclear techniques, 2011, 34(11): 845-850.
[1]张锦明,张晓军,张宝石,刘健,王卉,孙志军,田嘉禾.自动化“点击合成”正电子标记肽类细胞凋亡显像剂~(18)F-Pen-peptide[J].核技术,2011,34(11):845-850. DOI:
ZHANG Jinming1 ZHANG Xiaojun1 ZHANG Baoshi2 LIU Jian1 WANG Hui1 SUN Zhijun1 TIAN Jiahe1 1. Automated "click chemistry" synthesis of 18F-Pen-peptide as an apoptosis imaging agent[J]. Nuclear techniques, 2011, 34(11): 845-850. DOI:
采用国产双管PET-MF-2V-IT-1型多功能模块
在第一反应管合成6-氟-18戊炔
将之蒸发到第二反应管
与叠氮短肽前体在亚铜催化下发生点击反应
在室温下生成18F-Pen-peptide
经半制备HPLC纯化
再经固相萃取得到注射18F-Pen-peptide。采用A549肺腺癌细胞测量行化疗前后的细胞摄取。结果显示
6-氟-18戊炔合成效率为51%
6-氟-18戊炔与叠氮前体的反应效率近99%
总的合成效率为(21.0±4.5)%(n=6
未校正)
合成时间为70 min。最终产品的放射性活度14.8–22.2 GBq
放化纯为99%
比活度为870 GBq/μmol。A549细胞摄取实验表明
未化疗的细胞对18F-Pen-peptide摄取为(0.06±0.01)%
细胞凋亡为(1.02±0.31)%。化疗24 h后A549细胞摄取值为(0.86±0.04)%
细胞凋亡为(10.23±2.43)%。18F-Pen-peptide是一个有潜在临床应用价值的正电子肽类细胞凋亡显像剂。
18F-Pen-peptide was synthesized automatically in a PET-MF-IT-1 module using "click chemistry".18F-fluoropentyne was synthesized in reactor No.1 and distilled into reactor No.2
which was pre-loaded with peptide-N3
sodium ascorbate
and CuSO4/TBTA.After reacting at room temperature
the reaction mixture was purified by semi-HPLC
and the fine product 18F-Pen-peptide was collected by solid extraction.The cell uptake of 18F-Pen-peptide in A549 lung adenocarcinoma cells
which were or were not pre-treated with a chemical drug
was determined.The results showed that the yield of 18F-fluoropentyne was 51% from 18F-fluoride(EOS).The yield of 18F-Pen-peptide was nearly 99% from 18F-fluoropentyne.The total synthesis yield was(21.0?4.5)%(n=6
EOS).The radiochemistry purity was over 99%
and the specific activity was 870 GBq/μmol
respectively.It took 70 min for 18F-Pen-peptide starting from 18F-fluoride.After chemotherapy
the A549 cells uptake of 18F-Pen-peptide were(0.86±0.04)%
and the cell apoptosis rate was(10.23±2.43)%.The control A549 cells were(0.06±0.01)%
and the cells apoptosis rate was(1.02±0.31)%.The novel radiotracer 18F-Pen-peptide is a promising candidate for future apoptosis imaging in clinical settings.
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