A single-dose toxicity study on non-radioactive iodinated hypericin for a targeted anticancer therapy in mice

Jun-jie LI; Yi-cheng NI; Marlein Miranda CONA; Yuan-bo FENG; Feng CHEN; Guo-zhi ZHANG; Xue-bin FU; Uwe HIMMELREICH; Raymond OYEN; Alfons VERBRUGGEN

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A single-dose toxicity study on non-radioactive iodinated hypericin for a targeted anticancer therapy in mice

机译：非放射性碘化金丝桃素对小鼠靶向抗癌治疗的单剂量毒性研究

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Aim: Hypericin (Hyp) and its radio-derivatives have been investigated in animal models with ischemic heart diseases and malignancies for diagnostic and therapeutic purposes.Before radioiodinated Hyp (123I-Hyp or 131I-Hyp) can be considered as a clinically useful drug,vigorous evaluations on its chemotoxicity are necessary.In the present study,we examined the toxicity of a single dose of non-radioactive 127I-Hyp in normal mice for 24 h and 14 d.Methods: Studies were performed on 132 normal mice.127I-Hyp at a clinically relevant dose of 0.1 mg/kg body weight and a 100-times higher dose of 10 mg/kg was intravenously injected into 40 mice.The safety aspects of clinical manifestations,serological biochemistry,and histopathology were assessed.In another 72 mice,127I-Hyp was administered intravenously at assumed values to bracket the value of LD50.The rest 20 mice were used in the control groups.Results: At 24 h and 14 d following the injection of 127I-Hyp at either 0.1 or 10 mg/kg,all mice tolerated well without mortality or any observable treatment-related symptoms.No significant differences were found in blood biochemical parameters between the test and control groups.All organs presented normal appearances upon histopathological inspection.The value of LD50 of 127I-Hyp in mice through intravenous injection was 20.26 mg/kg,with the 95％ confidence interval between 18.90 and 21.55 mg/kg.Conclusion: The current study reveals a broad safety range of 127I-Hyp,which not only supports the use of 123I-Hyp or 131I-Hyp in the necrosis targeting theragnostic strategy,but also serves as a valuable reference for exploring other possible applications for iodinated Hyp.

机译：目的：在缺血性心脏病和诊断和治疗目的的动物模型中研究过胰蛋白酶对其嗜毒性的剧烈评估是必要的。在本研究中，我们检查了24小时和14d的正常小鼠单剂量非放射性127i-hyp中的毒性：在132正常小鼠上进行研究.127i-临床相关剂量为0.1mg / kg体重和100倍的剂量10mg / kg的剂量静脉注射到40只小鼠中。评估临床表现，血清生物化学和组织病理学的安全方面。另外72在假定的值处静脉内施用127i-hyp，以括在LD50的值。在对照组中使用其余20只小鼠。结果：在0.1或10mg的127i-hyp后24小时和14d。 / kg，所有小鼠t没有死亡或任何可观察的治疗相关症状的糖类良好。在试验和对照组之间存在显着的差异。在测试和对照组之间存在显着差异。所有器官在组织病理学检查时呈现正常的外观。通过静脉注射术直播127i-hyp的LD50的值。为20.26 mg / kg，置信区间为18.90和21.55 mg / kg。结论：目前的研究显示了127i-hyp的广泛安全范围，这不仅支持123i-hyp或131i-hyp的使用针对治疗策略的坏死，但也是探索碘化百下可能的其他可能应用的有价值的参考。

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《中国药理学报：英文版》 |2012年第12期|1549-1556|共8页
作者
Jun-jie LI; Yi-cheng NI; Marlein Miranda CONA; Yuan-bo FENG; Feng CHEN; Guo-zhi ZHANG; Xue-bin FU; Uwe HIMMELREICH; Raymond OYEN; Alfons VERBRUGGEN;
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Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Molecular Small Animal Imaging Centre(MoSAIC), Faculty of medicine, KU Leuven, Belgium;

Theragnostic Laboratory, Department of Imaging and Pathology, Biomedical Sciences Group, KU Leuven, Belgium;

Faculty of Pharmaceutical Sciences, KU Leuven, Belgium;

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A single-dose toxicity study on non-radioactive iodinated hypericin for a targeted anticancer therapy in mice

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