Synthesis and evaluation of [ 18F]Fluorobutyl ethacrynic amide: A potential PET tracer for studying glutathione transferase

Ho Lien Huang, Chun Nan Yeh, Kang Wei Chang, Jenn Tzong Chen, Kun Ju Lin, Li Wu Chiang, Kee Ching Jeng, Wei Ting Wang, Ken Hong Lim, Caleb Gonshen Chen, Kun I. Lin, Ying Cheng Huang, Wuu Jyh Lin, Tzu Chen Yen, Chung Shan Yu

研究成果: 雜誌貢獻文章同行評審

7 引文 斯高帕斯(Scopus)

摘要

[ 18F]Flurobutyl ethacrynic amide ([ 18F]FBuEA) was prepared from the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)butyl] ethacrynic amide with a radiochemical yield of 3%, a specific activity of 48 GBq/μmol and radiochemical purity of 98%. Chemical conjugation of [ 18F]FBuEA with glutathione (GSH) via a self-coupling reaction and enzymatic conjugation under catalysis of glutathiontransferase alpha (GST-α) and π provided about 41% yields of radiochemical conjugated product [ 18F]FBuEA-GSH, 85% and 5-16%, respectively. The catalytic selectivity of this tracer toward GST-alpha was addressed. Positron emission tomography (PET) imaging of [ 18F]FBuEA in normal rats showed that a homogeneous pattern of radioactivity was distributed in the liver, suggesting a catalytic role of GST. By contrast, PET images of [ 18F]FBuEA in rats with thioacetamide-induced cholangiocarcinoma displayed a heterogeneous pattern of radioactive accumulation with cold spots in tumor lesions. PET imaging with [ 18F]FBuEA could be used for early diagnosis of hepatic tumor with a low GST activity as well as liver function.
原文英語
頁(從 - 到)3998-4003
頁數6
期刊Bioorganic and Medicinal Chemistry Letters
22
發行號12
DOIs
出版狀態已發佈 - 6月 15 2012
對外發佈

ASJC Scopus subject areas

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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