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http://dx.doi.org/10.5012/bkcs.2008.29.10.2023

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

Kim, Sang-Wook (Radiation Research Division for Industry & Environment, Korea Atomic Energy Research Institute)
Park, Jeong-Hoon (Radiation Research Division for Industry & Environment, Korea Atomic Energy Research Institute)
Yang, Seung-Dae (Radiation Research Division for Industry & Environment, Korea Atomic Energy Research Institute)
Hur, Min-Goo (Radiation Research Division for Industry & Environment, Korea Atomic Energy Research Institute)
Choi, Chang-Woon (Department of Nuclear Medicine, Korea Institute of Radiological and Medical Sciences)
Yu, Kook-Hyun (Department of Chemistry, Dongguk University)
Publication Information
Abstract
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.
Keywords
Hypericin; 2-[123I]iodohypericin; 2-[124I]iodohypericin; Protein kinase C; Glioma
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