[123I]Iodooctyl fenbufen amide as a SPECT tracer for imaging tumors that over-express COX enzymes

Ho Lien Huang, Chun Nan Yeh, Wei Yuan Lee, Ying Cheng Huang, Kang Wei Chang, Kun Ju Lin, Shu Fan Tien, Wen Chin Su, Ching Hsiuan Yang, Jenn Tzong Chen, Wuu Jyh Lin, Shio Shio Fan, Chung Shan Yu*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

14 Scopus citations


This study is concerned with the development of an agent for single photon emission computer tomography (SPECT) for imaging inflammation and tumor progression. [123I]Iodooctyl fenbufen amide ([123I]IOFA) was prepared from the precursor N-octyl-4-oxo-4-(4'-(trimethylstannyl)biphenyl-4-yl)butanamide with a radiochemical yield of 15%, specific activity of 37 GBq/μmol, and radiochemical purity of 95%. Analysis of the binding of [123I]IOFA to COX-1 and COX-2 enzymes by using HPLC and a gel filtration column showed a selectivity ratio of 1:1.3. An assay for the competitive inhibition of substrate transfer showed that IOFA exhibited a comparable IC50 value compared to fenbufen. In the normal rat liver, a lower level and homogeneous pattern of [123I]IOFA radioactivity was observed by SPECT. In contrast, in the rat liver with thioacetamide-induced cholangiocarcinoma, a higher uptake and heterogeneous pattern of [123I]IOFA radioactivity was seen as hot spots in tumor lesions by SPECT imaging. Importantly, elevated COX-1 and COX-2 expressions from immunostaining were found in the bile ducts of tumor rats but not of normal rats. Therefore, [123I]IOFA was found to exhibit the potential for imaging tumors that over-express COX.

Original languageEnglish
Pages (from-to)3355-3365
Number of pages11
Issue number13
StatePublished - 04 2013


  • Imaging
  • Inflammation
  • Nuclear medicine
  • Radiochemistry
  • Tumor


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