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Meeting ReportMolecular Targeting Probes - Radioactive and Nonradioactive

Synthesis and evaluation of fluorine-18 labeled ipomeanol as a CYP4B1 expression imaging probe

Byung Seok Moon, Su Jin Jang, Tae Sup Lee, Byung Chul Lee, Joo Hyun Kang and Sang Eun Kim
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1571;
Byung Seok Moon
1Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seoul, Republic of Korea
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Su Jin Jang
2Molecular Imaging Research Center, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea
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Tae Sup Lee
2Molecular Imaging Research Center, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea
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Byung Chul Lee
1Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seoul, Republic of Korea
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Joo Hyun Kang
2Molecular Imaging Research Center, Korea Institute of Radiological and Medical Sciences, Seoul, Republic of Korea
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Sang Eun Kim
1Department of Nuclear Medicine, Seoul National University Bundang Hospital, Seoul National University College of Medicine, Seoul, Republic of Korea
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Abstract

1571

Objectives 4-Ipomeanol (1-(3-furyl)-4-hydroxy-1-pentanone, 4-IPO) is naturally occurring pulmonary toxin. The major metabolic pathway of 4-IPO by cytochrome P450 enzymes involves furan ring opening leading to the formation of unsaturated α,β-aldehyde/ketone of dialdehyde reactive metabolite. Among of cytochrome P450 isozyme, CYP4B1, efficiently converts the prodrug, 4-IPO, to the alkylating metabolite which was highly reactive and binding covanently with tissues immediately at its site of formation. The present study is the development of F-18 labeled 4-IPO which has efficient targeting of CYP4B1 gene transfected cells.

Methods The target compound, 5-fluoro-4-hydroxy-1-furan-3-yl-1-pentanone (F-4-IPO), was synthesized in twelve steps from 3-furaldehyde. [18F]F-4-IPO was synthesized from mesylate precursor through three-consecutive steps - displacement of [18F]fluoride, reduction and acidic-deprotection. C6-CYP4B1 cells were established using plasmid transfection. Evaluation of CYP4B1 expression level was confirmed by RT-PCR and MTT assay. Biodistribution study of [18F]F-4-IPO was investigated in normal rats. The cellular uptake of [18F]F-4-IPO and [3H]-4-IPO was performed in parental and CYP4B1-transfected cells and compared.

Results The radiochemical yield of [18F]F-4-IPO was 20-35% with >95% of radiochemical purity. [18F]F-4-IPO showed over 96% stability until 120 min in human serum. Biodistribution of [18F]F-4-IPO in normal rats showed similar uptake patterns to [3H]-4-IPO. The cellular uptake ratios of [18F]F-4-IPO and [3H]-4-IPO in C6-CYP4B1 cells increased up to about 1.8 times at 30 min for [18F]F-4-IPO and 2.3 times at 360 min for [3H]-4-IPO higher than that of parental cells.

Conclusions Our results show that [18F]F-4-IPO is an excellent analog of 4-IPO, and deserves further studies to evaluate its utility for PET imaging of CYP4B1 transfected cancer cells

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Journal of Nuclear Medicine
Vol. 53, Issue supplement 1
May 2012
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Synthesis and evaluation of fluorine-18 labeled ipomeanol as a CYP4B1 expression imaging probe
Byung Seok Moon, Su Jin Jang, Tae Sup Lee, Byung Chul Lee, Joo Hyun Kang, Sang Eun Kim
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1571;

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Synthesis and evaluation of fluorine-18 labeled ipomeanol as a CYP4B1 expression imaging probe
Byung Seok Moon, Su Jin Jang, Tae Sup Lee, Byung Chul Lee, Joo Hyun Kang, Sang Eun Kim
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1571;
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