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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 10
BKCSDE 29(10)
October 20, 2008 

Synthesis and in vitro/vivo Evaluation of Iodine-123/124 Labelled Hypericin Derivatives
Sang Wook Kim, Jeong Hoon Park, Seung Dae Yang*, Min Goo Hur, Chang Woon Choi, Kook Hyun Yu*,
Hypericin, 2-[123I]iodohypericin, 2-[124I]iodohypericin, Protein kinase C, Glioma
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-[123I/124I]iodohypericin and the results of a corresponding biological evaluation. In all glioma cell lines, 2-[123I]iodohypericin uptake was increased in a time dependant manner and an accumulation of 2-[124I]iodohypericin was observed in C6 glioma bearing nude mouse. These results suggest that radioiodine labelled hypericin can visualize a PKC overexpressed malignant glioma.
2023 - 2025
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