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首页> 外文期刊>Chemistry: A European journal >A Bio-Chemosynthetic Approach to Superparamagnetic Iron Oxide-Ansamitocin Conjugates for Use in Magnetic Drug Targeting
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A Bio-Chemosynthetic Approach to Superparamagnetic Iron Oxide-Ansamitocin Conjugates for Use in Magnetic Drug Targeting

机译：用于磁性药物靶向的超顺磁性氧化铁 - 氧化胺缀合物的生物化学合成方法

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摘要

A combination of mutasynthesis using a mutant strain of A. pretiosum blocked in the biosynthesis of amino-hydroxybenzoic acid (AHBA) and semisynthesis relying on a Stille cross-coupling step provided access to new ansamitocin derivatives of which one was attached by a thermolabile linker to nanostructured iron oxide particles. When exposed to an oscillating electromagnetic field the resulting iron oxide/ansamitocin conjugate 19 heats up in an aqueous suspension and the ansamitocin derivative 16 is released by means of a retro-Diels-Alder reaction. It exerts strong antiproliferative activity (IC_(50)= 4.8 ngmg~(-1)) in mouse fibroblasts. These new types of conjugates have the potential for combating cancer through hyperthermia and chemotherapy using an electromagnetic external trigger.
机译：使用A的突变株的突变体菌株在氨基 - 羟基苯甲酸（AHBA）的生物合成中，依赖于STILLE联偶联步骤的半合成菌株的组合提供了进入新的αamitocin衍生物，其由热电子连接器连接 纳米结构氧化铁颗粒。 当暴露于振荡电磁场时，所得氧化铁/氨基酰缀合物19在含水悬浮液中加热，并且通过复古酰胺 - Alder反应释放释放anamitocin衍生蛋白16。 在小鼠成纤维细胞中施加强烈的抗增殖活性（IC_（50）= 4.8 ngmg〜（-1））。 这些新型的缀合物具有使用电磁外部触发通过热疗和化疗来调用癌症的可能性。

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  • 来源
    《Chemistry: A European journal》 |2017年第10期|共6页
  • 作者

    Liang-Liang Wang; Asha Balakrishnan; Nadja-Carola Bigall; David Candito; Jan Frederick Miethe; Katja Seidel; Yu Xie; Michael Ott; Andreas Kirschning;

  • 作者单位

    Institut für Organische Chemie und Biomolekulares Wirkstoffzentrum (BMWZ) Leibniz Universit?t Hannover Schneiderberg 1B 30167 Hannover (Germany);

    Department of Gastroenterology Hepatology and Endocrinology Hannover Medical School (MHH) TWINCORE Center for Experimental and Clinical Infection Research Feodor-Lynen-Str. 7 30625 Hannover (Germany);

    Institut für Physikalische Chemie und Elektrochemie Leibniz Universit?t Hannover Callinstr. 3A 30167 Hannover (Germany);

    Institut für Organische Chemie und Biomolekulares Wirkstoffzentrum (BMWZ) Leibniz Universit?t Hannover Schneiderberg 1B 30167 Hannover (Germany);

    Institut für Physikalische Chemie und Elektrochemie Leibniz Universit?t Hannover Callinstr. 3A 30167 Hannover (Germany);

    Institut für Organische Chemie und Biomolekulares Wirkstoffzentrum (BMWZ) Leibniz Universit?t Hannover Schneiderberg 1B 30167 Hannover (Germany);

    Department of Gastroenterology Hepatology and Endocrinology Hannover Medical School (MHH) TWINCORE Center for Experimental and Clinical Infection Research Feodor-Lynen-Str. 7 30625 Hannover (Germany);

    Department of Gastroenterology Hepatology and Endocrinology Hannover Medical School (MHH) TWINCORE Center for Experimental and Clinical Infection Research Feodor-Lynen-Str. 7 30625 Hannover (Germany);

    Institut für Organische Chemie und Biomolekulares Wirkstoffzentrum (BMWZ) Leibniz Universit?t Hannover Schneiderberg 1B 30167 Hannover (Germany);

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 应用化学;
  • 关键词

    ansamitocin; chemotherapy; Diels-Alder reaction; nanoparticles; drug delivery; hyperthermia;

    机译：Ansamitocin;化疗;Diels-Alder反应;纳米粒子;药物递送;热疗;

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