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Dual Acid-Responsive Micelle-Forming Anticancer Polymers as New Anticancer Therapeutics

机译：双酸响应胶束形成抗癌聚合物作为新的抗癌药物。

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摘要

Cinnamaldehyde, a major active compound of cinnamon, is known to induce apoptotic cell death in numerous human cancer cells. Here, dual acid-responsive polymeric micelle-forming cinnamaldehyde prodrugs, poly[(3-phenyl-prop-2-ene-1,1-diyl)bis(oxy)bis(ethane-2,1-diyl)diacrylate]-co-4,4'(trimethylene dipiperidine)-co-poly(ethylene glycol), termed PCAE copolymers, are reported. PCAE is designed to incorporate cinnamaldehyde via acid-cleavable acetal linkages in its pH-sensitive hydrophobic backbone and self assemble to form stable micelles which can encapsulate camptothecin (CPT). PCAE self assembles to form micelles which release CPT and cinnamaldehyde in pH-dependent manners. PCAE micelles induce apoptotic cell death through the generation of intracellular reactive oxygen species (ROS) and exert synergistic anticancer effects with a payload of CPT in vitro and in vivo model of SW620 human colon tumor-bearing mice. It is anticipated that dual acid-sensitive micelle-forming PCAE with intrinsic anticancer activities has enormous potential as novel anticancer therapeutics.
机译：肉桂醛是肉桂的主要活性化合物，已知可在许多人类癌细胞中诱导凋亡性细胞死亡。在这里，双酸响应聚合物胶束形成肉桂醛前药，聚[（3-苯基-丙-2-烯-1,1-二基）双（氧基）双（乙烷-2,1-二基）二丙烯酸酯] -co报道了称为PCAE共聚物的-4，4′（三亚甲基二哌啶）-共聚（乙二醇）。 PCAE旨在通过酸可裂解的缩醛键将肉桂醛掺入其对pH敏感的疏水性骨架中，并自组装形成稳定的胶束，该胶束可以封装喜树碱（CPT）。 PCAE自组装形成胶束，以依赖pH的方式释放CPT和肉桂醛。 PCAE胶束通过细胞内活性氧（ROS）的产生诱导凋亡细胞死亡，并在SW620人结肠癌荷瘤小鼠的体内和体外模型中与CPT的有效载荷一起发挥协同抗癌作用。预期具有固有抗癌活性的双酸敏感性胶束形成PCAE作为新型抗癌治疗剂具有巨大潜力。

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  • 来源
    《Advanced Functional Materials》 |2013年第40期|5091-5097|共7页
  • 作者

    Byungkuk Kim; Eunsun Lee; Yerang Kim; Sanga Park; Gilson Khang; Dongwon Lee;

  • 作者单位

    Department of BIN Fusion Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

    Department of BIN Fusion Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

    Department of BIN Fusion Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

    Department of BIN Fusion Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

    Polymer Fusion Research Center Department of Polymer-Nano Science and Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

    Polymer Fusion Research Center Department of Polymer-Nano Science and Technology Chonbuk National University Jeonju, Chonbuk, 561-756, Korea;

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