[11C]Choline as a PET biomarker for assessment of prostate cancer tumor models

Qi Huang Zheng, Thomas A. Gardner, Sudhanshu Raikwar, Chinghai Kao, K. Lee Stone, Tanya D. Martinez, Bruce H. Mock, Xiangshu Fei, Ji Quan Wang, Gary D. Hutchins

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Abstract

[11C]Choline has been evaluated as a positron emission tomography (PET) biomarker for assessment of established human prostate cancer tumor models. [11C]Choline was prepared by the reaction of [ 11C]methyl triflate with 2-dimethylaminoethanol (DMAE) and isolated and purified by solid-phase extraction (SPE) method in 60-85% yield based on [11C]CO2, 15-20min overall synthesis time from end of bombardment (EOB), 95-99% radiochemical purity and specific activity >0.8Ci/μmol at end of synthesis (EOS). The biodistribution of [ 11C]choline was determined at 30min post iv injection in prostate cancer tumor models C4-2, PC-3, CWR22rv, and LNCaP tumor-bearing athymic mice. The results showed the accumulation of [11C]choline in these tumors was 1.0% dose/g in C4-2 mouse, 0.4% dose/g in PC-3 mice, 3.2% dose/g in CWR22rv mice, and 1.4% dose/g in LNCaP mice; the ratios of tumor/muscle (T/M) and tumor/blood (T/B) were 2.3 (T/M, C4-2), 1.4 (T/M, PC-3), 2.5 (T/M, CWR22rv), 1.2 (T/M, LNCaP) and 2.6 (T/B, C4-2), 2.6 (T/B, PC-3), 7.8 (T/B, CWR22rv), 3.2 (T/B, LNCaP), respectively. The micro-PET imaging of [11C]choline in prostate cancer tumor models was acquired from a C4-2, PC-3, CWR22rv, or LNCaP implanted mouse at 30min post iv injection of 1mCi of the tracer using a dedicated high resolution (<3mm full-width at half-maximum) small FOV (field-of-view) PET imaging system, IndyPET-II scanner, developed in our laboratory, which showed the accumulation of [11C]choline in C4-2, PC-3, CWR22rv, or LNCaP tumor implanted in a nude athymic mouse. The initial dynamic micro-PET imaging data indicated the average T/M ratios were approximately 3.0 (C4-2), 2.1 (PC-3), 3.5 (CWR22rv), and 3.3 (LNCaP), respectively, which showed the tumor accumulation of [11C]choline in all four tumor models is high. These results suggest that there are significant differences in [11C]choline accumulation between these different tumor types, and these differences might offer some useful measure of tumor biological process.

Original languageEnglish (US)
Pages (from-to)2887-2893
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number11
DOIs
StatePublished - Jun 1 2004

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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