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Rationale of 5-125I-Iodo-4'-Thio-2'-Deoxyuridine as a Potential Iodinated Proliferation Marker

Jun Toyohara, MS1, Akio Hayashi, PhD1, Mikiko Sato, MS1, Hiromichi Tanaka, PhD2, Kazuhiro Haraguchi, PhD2, Yuichi Yoshimura, PhD2, Yoshiharu Yonekura, MD, PhD3 and Yasuhisa Fujibayashi, PhD, DMedSci3

1 Research and Development Division, Research Center, Nihon Medi-Physics Company, Limited, Chiba, Japan
2 School of Pharmaceutical Science, Showa University, Tokyo, Japan
3 Biomedical Imaging Research Center, Fukui Medical University, Fukui, Japan



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  		FIGURE 1. Synthetic pathway for preparation of radiolabeled ITdU and ITAU by destannylation.

 


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  		FIGURE 2. Time-dependent incorporation of radioactivity into Lewis lung carcinoma cells. (A) Radioactivity of acid-soluble small molecule, DNA, RNA, and protein fractions is shown. (B) Time-dependent percentage of radioactivity distribution in each fraction of Lewis lung carcinoma. Data are expressed as mean ± SD for 3 experiments.

 


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  		FIGURE 3. Uptake of iodonucleosides, expressed as organ-to-blood ratio of radioactivity. Animals were killed at 18 h after injection. Data are expressed as mean ± SD for 3 experiments. Iodonucleosides showed higher uptake in proliferation organs (femur, spleen, intestine, and thymus) than in nonproliferating organs (muscle, liver, and lung). Statistical significance between 125I-IUdR uptake and 125I-ITdU uptake was observed in intestine and thymus (P < 0.05; Student t test).

 




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