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

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. KCI Citation Count: 9