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首页> 外文期刊>Biomaterials Science >Theranostic supramolecular polymers formed by the self-assembly of a metal-chelating prodrug
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Theranostic supramolecular polymers formed by the self-assembly of a metal-chelating prodrug

机译：由金属螯合前药的自组装形成的治疗超分子聚合物

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摘要

Therapeutic constructs with imaging modalities hold great promise for improving the treatment efficacy for cancer and many other diseases. We report here the design and synthesis of a self-assembling prodrug (SAPD) by the direct linkage of camptothecin (CPT), an anticancer drug, to a metal-chelating agent, DOTA. We found that under physiological conditions the DOTA-conjugated CPT prodrug can self-assemble into tubular supramolecular polymers (SPs) with a length of several micrometers. Our studies also suggest that the resultant assemblies were stable in biological environments and exhibited a fast drug release rate in the presence of intracellular glutathione. Furthermore, the SAPD exhibited remarkable in vitro efficacy against various cancer cell lines and effectively inhibited the growth of tumor spheroids. We believe that the design and optimization of self-assembling theranostic conjugates could provide a robust yet simple platform for the development of new imaging-guided drug delivery systems.
机译：具有成像方式的治疗构建能够对提高癌症和许多其他疾病的治疗疗效具有巨大的希望。我们在此报告了通过Camptothecin（CPT），抗癌药物直接连接到金属螯合剂，DotA的自组装前药（SAPD）的设计和合成。我们发现，在生理条件下，DotA缀合的CPT前药可以自组装成具有几微米的长度的管状超分子聚合物（SPS）。我们的研究还表明，所得组件在生物环境中稳定，并在细胞内谷胱甘肽存在下表现出快速的药物释放速率。此外，SAPD对各种癌细胞系具有显着的体外功效，并有效地抑制肿瘤球状体的生长。我们认为，自组装Heranostic缀合物的设计和优化可以为新的成像引导药物输送系统的开发提供强大而简单的平台。

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  • 来源
    《Biomaterials Science》 |2021年第2期|共8页
  • 作者

    Su Hao; Cui Yonggang; Wang Feihu; Zhang Weijie; Zhang Chunli; Wang Rongfu; Cui Honggang;

  • 作者单位

    Johns Hopkins Univ Dept Chem &

    Biomol Engn 3400 North Charles St Baltimore MD 21218 USA;

    Peking Univ Dept Nucl Med Hosp 1 8 Xishiku St Beijing 100034 Peoples R China;

    Johns Hopkins Univ Dept Chem &

    Biomol Engn 3400 North Charles St Baltimore MD 21218 USA;

    Johns Hopkins Univ Dept Chem &

    Biomol Engn 3400 North Charles St Baltimore MD 21218 USA;

    Peking Univ Dept Nucl Med Hosp 1 8 Xishiku St Beijing 100034 Peoples R China;

    Peking Univ Dept Nucl Med Hosp 1 8 Xishiku St Beijing 100034 Peoples R China;

    Johns Hopkins Univ Dept Chem &

    Biomol Engn 3400 North Charles St Baltimore MD 21218 USA;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 分子生物学;
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