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Synthesis of Folate Receptor-targeted Photosensitize for Photodynamic Therapy

机译：叶酸受体靶向光敏剂的合成用于光动力疗法

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摘要

A series of amphiphilic benzylidene cycloalkanes ketone photosensitizers C1-C4 with or without folate receptor-targeted agent were designed and synthesized. Their photophysical properties and in vitro photodynamic therapy (PDT) effects were studied. The results showed that all compounds exhibited appropriate lipid-water partition coefficients and high reactive oxygen yields. The introduction of the folate receptor-targeted agent had no obvious influence on the basic photophysical & photochemical properties of C2 and C4 compared to those of their corresponding prototype compounds (Cl and C3). In vitro studies were carried out using MCF-7 cells (FR+), Hela cells (FR+) and A549 cells (FR-), which represented different levels of folate receptor (FR) expression. All of C1-C4 showed low dark toxicity and superior PDT effects compared with the clinical drug PSD-007 (a mixture of porphyrins). What's more, folate receptor-targeted photosensitizers (C2 and C4) achieved higher accumulation and more excellent PDT effects in MCF-7 cells (FR+) and Hela cells (FR+) than photosensitizers (Cl and C3) without folate receptor-targeted agent and PSD-007. The photo-cytotoxicity of these photosensitizers showed no obvious differences in A549 cells (FR-).
机译：设计并合成了一系列带有或不带有叶酸受体靶向剂的两亲亚苄基环烷烃酮类光敏剂C1-C4。研究了它们的光物理性质和体外光动力疗法（PDT）的作用。结果表明，所有化合物均表现出适当的脂质-水分配系数和高活性氧产率。与相应的原型化合物（C1和C3）相比，叶酸受体靶向剂的引入对C2和C4的基本光物理和光化学特性没有明显的影响。使用代表不同水平叶酸受体（FR）表达的MCF-7细胞（FR +），Hela细胞（FR +）和A549细胞（FR-）进行了体外研究。与临床药物PSD-007（卟啉的混合物）相比，所有C1-C4均显示出低的暗毒性和优异的PDT效果。而且，与没有叶酸受体靶向剂和PSD的光敏剂（C1和C3）相比，以叶酸受体靶向的光敏剂（C2和C4）在MCF-7细胞（FR +）和Hela细胞（FR +）中具有更高的积累和更出色的PDT效果。 -007。这些光敏剂的光细胞毒性显示A549细胞（FR-）没有明显差异。

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  • 来源
    《Optics in health care and biomedical optics VI》|2014年|92680O.1-92680O.7|共7页
  • 会议地点 Beijing(CN)
  • 作者

    Yanyan Fang; Xiaopu Wang; Qianli Zou; Yuxia Zhao; Feipeng Wu;

  • 作者单位

    Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China,University of Chinese Academy of Sciences, Beijing 100049, China;

    Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China,University of Chinese Academy of Sciences, Beijing 100049, China;

    Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China;

    Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China;

    Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China;

  • 会议组织
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    Folate receptor-targeted agent; photosensitizer; photodynamic therapy;

    机译：叶酸受体靶向药物；光敏剂光动力疗法;

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