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首页> 外文期刊>RSC Advances >Self-organized environment-sensitive inulin-doxorubicin conjugate with a selective cytotoxic effect towards cancer cells
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Self-organized environment-sensitive inulin-doxorubicin conjugate with a selective cytotoxic effect towards cancer cells

机译：自组织环境敏感的inulin-doxorubicin缀合物，具有对癌细胞的选择性细胞毒性作用

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摘要

An inulin-based random copolymer bearing high dose doxorubicin (18.45% on a weight basis), INU-EDA-P, C-DOXO, was prepared by coupling doxorubicin with inulin though a citraconylamide bridge used as a pH sensitive spacer. A further conjugation with pentynoic acid via an amidic bond led to the hydrophobization of the copolymer which allows the acquisition of a self-assembling ability at low concentration (0.33 mg mL(-1)) combining both Pi-Pi stacking and London interactions. Drug release studies were carried out at different pH demonstrating a remarkable pH dependency, where the maximum release rate was observed at pH mimicking cancer tissue and lysosomal environments. Besides, by measuring zeta-potential variations as a function of the pH, INU-EDA-P, C-DOXO proved capable of undergoing charge reversal at acidic pH, changing its physicochemical and biological behavior. In vitro tests with cancer (MDA-MB 231) and normal (HB-2) breast cells were carried out to verify the conjugate aptitude to follow different routes to enter cells depending on the microenvironment. This finding was supported by quantitative up-take studies, which revealed that INU-EDA-P, C-DOXO released doxorubicin before entering cancer cells, as the entire copolymer diffused across normal cell membranes without relevant modifications.
机译：含有高剂量的无规共聚物的菊毛蛋白基随机共聚物（18.45％），通过用菊粉与inulin偶联，inu-EDA-P，C-DOXO通过用作pH敏感间隔物的柠檬酰胺桥来制备。通过酰胺键与酰胺键的进一步缀合LED允许共聚物的疏水化，其允许以低浓度（0.33mg ml（-1））的自组装能力，组合PI-PI堆叠和伦敦相互作用。在不同的pH下进行药物释放研究证明了显着的pH依赖性，其中在pH模拟癌组织和溶酶体环境下观察到最大释放速率。此外，通过测量作为pH，INU-EDA-P，C-DOXO的函数的Zeta潜在的变化，证明能够在酸性pH下进行充电反转，改变其物理化学和生物学行为。进行癌症（MDA-MB 231）和正常（HB-2）乳腺细胞的体外试验，以验证缀合物是否遵循不同途径，根据微环境进入细胞。通过定量上升研究支持该发现，揭示了Inu-EDA-P，C-Doxo在进入癌细胞之前释放了多柔比星，因为整个共聚物在不相关的修饰的情况下扩散到正常细胞膜上。

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  • 来源
    《RSC Advances》 |2015年第41期|共10页
  • 作者

    Mauro N.; Campora S.; Scialabba C.; Adamo G.; Licciardi M.; Ghersi G.; Giammona G.;

  • 作者单位

    Univ Palermo Lab Biocompatible Polymers Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90123 Palermo Italy;

    Univ Palermo Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90128 Palermo Italy;

    Univ Palermo Lab Biocompatible Polymers Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90123 Palermo Italy;

    Univ Palermo Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90128 Palermo Italy;

    Univ Palermo Lab Biocompatible Polymers Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90123 Palermo Italy;

    Univ Palermo Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90128 Palermo Italy;

    Univ Palermo Lab Biocompatible Polymers Dept Sci &

    Tecnol Biol Chim &

    Farmaceut STEBICEF I-90123 Palermo Italy;

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  • 正文语种 eng
  • 中图分类 化学;
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