单-[123I]碘金丝桃素单羧酸作为坏死亲和显像剂的合成及初步评价
Synthesis and preliminary evaluation of mono-[123I]iodohypericin monocarboxylic acid as a necrosis avid imaging agent.
作者信息
Fonge Humphrey, Jin Lixin, Wang Huaijun, Ni Yicheng, Bormans Guy, Verbruggen Alfons
机构信息
Laboratory of Radiopharmacy, Faculty of Pharmaceutical Sciences, K.U. Leuven, BE-3000 Leuven, Belgium.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):4001-5. doi: 10.1016/j.bmcl.2007.04.083. Epub 2007 Apr 30.
Hypericin monocarboxylic acid was synthesized in an overall yield of 25% in four steps and radiolabelled with iodine-123 in good yield (>75%). The resulting mono-[(123)I]iodohypericin monocarboxylic acid was evaluated in normal mice and in rats with ethanol induced liver necrosis. In this model, tracer concentration in necrotic liver tissue was 14 times higher than in the viable liver tissue as quantified by autoradiography at 24h post injection. The results indicate the feasibility of visualization of necrotic tissue with the novel tracer.
金丝桃素单羧酸经四步合成，总产率为25%，并以良好的产率（>75%）用碘 - 123进行放射性标记。所得的单 - [(123)I]碘代金丝桃素单羧酸在正常小鼠和乙醇诱导的肝坏死大鼠中进行了评估。在该模型中，注射后24小时通过放射自显影定量显示，坏死肝组织中的示踪剂浓度比存活肝组织高14倍。结果表明，使用这种新型示踪剂可视化坏死组织是可行的。
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