| 叔丁氧羰基二肽胺磷酸对碘苯酚酯的生物性质研究 |
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| 引用本文： | 何佳恒,蹇源,蒋树斌,王关全,刘国平.叔丁氧羰基二肽胺磷酸对碘苯酚酯的生物性质研究[J].化学研究与应用,2009,21(5). |
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| 作者姓名： | 何佳恒 蹇源 蒋树斌 王关全 刘国平 |
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| 作者单位： | 中国工程物理研究院核物理与化学研究所,四川,绵阳,621900 |
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| 基金项目： | 中国工程物理研究院核物理与化学研究所创新基金 |
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| 摘 要： | 采用细胞结合实验对配合物叔丁氧羰基二肽胺磷酸对碘(131I)苯酚酯的体外生物活性进行了评价,结果表明标记抗原保持了原来的亲和力,在标记等操作过程中未受到明显损伤;对配合物进行了稳定性、亲脂性、急性毒性的考察,结果显示配合物的结构和性能比较稳定,三天后的脱碘率为12%左右、是亲脂性的、毒性低;成功建立了VX2肝癌单发肿瘤动物模型,得到了配合物在正常小鼠和肿瘤大白兔体内的分布结果.
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| 关 键 词： | 二肽 生物活性 |
The study on biological activity of p-BocGly-Tyr-NH(CH_2)_2 NH-PO(ONH_4)-O-PhI |
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| HE Jia-heng,JIAN Yuan,JIANG Shu-bin,WANG Guan-quan,LIU Guo-ping.The study on biological activity of p-BocGly-Tyr-NH(CH_2)_2 NH-PO(ONH_4)-O-PhI[J].Chemical Research and Application,2009,21(5). |
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| Authors: | HE Jia-heng JIAN Yuan JIANG Shu-bin WANG Guan-quan LIU Guo-ping |
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| Institution: | Institute of Nuclear Physics and Chemistry;China Academy of Engineering Physics;Mianyang 621900;China |
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| Abstract: | Using cell coalescent method,the biological activity in vitro of the labelled compounds(di-peptidep-Boc-Gly-Tyr-NH(CH2)2 NH-PO(ONH4)-O-PhI]) was evaluated in this work.The results showed that the primary appetency was kept and not damaged obviously during labelling.Results on judgement of their stability,lipophilicity and toxicity demonstrated lower toxicity,higher lipophilicity and lower Iodium disassociation percentage(<12% after 72h);furthermore,a tumour-bearing animal model,was establishd successfully,... |
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| Keywords: | 131I |
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