[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

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

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
JournalBiomaterials
Volume34
Issue number13
DOIs
Publication statusPublished - Apr 1 2013
Externally publishedYes

Fingerprint

Photons
Amides
Tomography
Rats
Tumors
Enzymes
Imaging techniques
Radioactivity
Liver
Neoplasms
Thioacetamide
Cholangiocarcinoma
Bile Ducts
Ducts
Inhibitory Concentration 50
Gel Chromatography
Assays
Gels
High Pressure Liquid Chromatography
Inflammation

Keywords

  • Imaging
  • Inflammation
  • Nuclear medicine
  • Radiochemistry
  • Tumor

ASJC Scopus subject areas

  • Bioengineering
  • Ceramics and Composites
  • Biophysics
  • Biomaterials
  • Mechanics of Materials

Cite this

[123I]Iodooctyl fenbufen amide as a SPECT tracer for imaging tumors that over-express COX enzymes. / Huang, Ho Lien; Yeh, Chun Nan; Lee, Wei Yuan; Huang, Ying Cheng; Chang, Kang Wei; Lin, Kun Ju; Tien, Shu Fan; Su, Wen Chin; Yang, Ching Hsiuan; Chen, Jenn Tzong; Lin, Wuu Jyh; Fan, Shio Shio; Yu, Chung Shan.

In: Biomaterials, Vol. 34, No. 13, 01.04.2013, p. 3355-3365.

Research output: Contribution to journalArticle

Huang, HL, Yeh, CN, Lee, WY, Huang, YC, Chang, KW, Lin, KJ, Tien, SF, Su, WC, Yang, CH, Chen, JT, Lin, WJ, Fan, SS & Yu, CS 2013, '[123I]Iodooctyl fenbufen amide as a SPECT tracer for imaging tumors that over-express COX enzymes', Biomaterials, vol. 34, no. 13, pp. 3355-3365. https://doi.org/10.1016/j.biomaterials.2013.01.050
Huang, Ho Lien ; Yeh, Chun Nan ; Lee, Wei Yuan ; Huang, Ying Cheng ; Chang, Kang Wei ; Lin, Kun Ju ; Tien, Shu Fan ; Su, Wen Chin ; Yang, Ching Hsiuan ; Chen, Jenn Tzong ; Lin, Wuu Jyh ; Fan, Shio Shio ; Yu, Chung Shan. / [123I]Iodooctyl fenbufen amide as a SPECT tracer for imaging tumors that over-express COX enzymes. In: Biomaterials. 2013 ; Vol. 34, No. 13. pp. 3355-3365.
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AU - Yeh, Chun Nan

AU - Lee, Wei Yuan

AU - Huang, Ying Cheng

AU - Chang, Kang Wei

AU - Lin, Kun Ju

AU - Tien, Shu Fan

AU - Su, Wen Chin

AU - Yang, Ching Hsiuan

AU - Chen, Jenn Tzong

AU - Lin, Wuu Jyh

AU - Fan, Shio Shio

AU - Yu, Chung Shan

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