• Title/Summary/Keyword: 2-[124I]iodohypericin

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Synthesis and in vitro/vivo Evaluation of Iodine-123/124 Labelled Hypericin Derivatives

  • Kim, Sang-Wook;Park, Jeong-Hoon;Yang, Seung-Dae;Hur, Min-Goo;Choi, Chang-Woon;Yu, Kook-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.29 no.10
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    • pp.2023-2025
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    • 2008
  • To evaluate the potential of radioiodine labelled hypericin as a malignant glioma imaging agent, U-251 MG, U-373 MG, C6 glioma and fibroblast were treated with a I-123 labelled hypericin derivative and C6 glioma transplanted nude mouse were injected with a I-124 labelled hypericin derivative for a micro PET imaging. 2- Iodohypericin was prepared as a reference compound. In this paper, we describe the syntheses of 2- iodohypericin and 2-[$^{123}I/^{124}I$]iodohypericin and the results of a corresponding biological evaluation. In all glioma cell lines, 2-[$^{123}I$]iodohypericin uptake was increased in a time dependant manner and an accumulation of 2-[$^{124}I$]iodohypericin was observed in C6 glioma bearing nude mouse. These results suggest that radioiodine labelled hypericin can visualize a PKC overexpressed malignant glioma.