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化学进展 2018, Vol. 30 Issue (9): 1403-1414 DOI: 10.7536/PC171245 前一篇   后一篇

• 综述 •

可激活抗癌光敏剂

郑秉得, 赵园园, 李洪才, 郑碧远, 柯美荣, 黄剑东*   

  1. 福州大学化学学院 能源与环境光催化国家重点实验室 福建省肿瘤转移药物干预重点实验室 福州 350108
  • 收稿日期:2017-12-29 修回日期:2018-05-03 出版日期:2018-09-15 发布日期:2018-06-28
  • 通讯作者: 黄剑东 E-mail:jdhuang@fzu.edu.cn
  • 基金资助:
    国家自然科学基金项目（No.21473033，U1705282）资助
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Activatable Photodynamic Anticancer Photosensitizers

Bingde Zheng, Yuanyuan Zhao, Hongcai Li, Biyuan Zheng, Meirong Ke, Jiandong Huang*   

  1. College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou 350108, China
  • Received:2017-12-29 Revised:2018-05-03 Online:2018-09-15 Published:2018-06-28
  • Supported by:
    The work was supported by the National Natural Science Foundation of China(No.21473033, U1705282).
光动力治疗（Photodynamic therapy，PDT）是利用光敏剂在光照下促使分子氧转为具有细胞毒性的活性氧，从而达到破坏靶细胞和靶组织效应的一种治疗手段。可激活光敏剂（Activatable photosensitizers，aPSs）是指事先屏蔽了光敏效应的光敏剂，只在特定因素下，如与肿瘤相关的特异性酶、酸性pH、核酸等的激活下，光敏剂转为激活状态，从而发挥诊断或者治疗的作用。可激活光敏剂由于具有更高的选择性而备受瞩目，成为医用光敏剂领域的研究前沿热点。本文将总结和分析近年来可激活抗癌光敏剂的研究现状和构效关系，以期为后续的相关研究提供参考。
关键词： 可激活光敏剂, 癌症, 光动力治疗
Photodynamic therapy(PDT) is a cancer therapeutic modality that utilizes photosensitizers(PSs) and molecular oxygen upon irradiation with light to generate cytotoxic reactive oxygen species leading to damage of the target tissues and cells. Activatable photosensitizers(aPSs)that are inactivated initially, can only be activated by tumor-associated stimuli, such as tumor-associated specific enzymes, acidic pH, nucleic acid, to achieve targeting diagnosis and treatment. The aPSs have become a hot spot in the field of medical photosensitizers because of its higher selectivity. In this paper, we will summarize the recent development of aPSs, and analyze their structure-activity relationships, expecting to provide a reference for the future studies.
Contents
1 Introduction
2 pH-activatable photosensitizers
3 Enzyme-activatable photosensitizers
3.1 Cathepsin-activatable photosensitizers
3.2 Urokinase type plasminogenactivator(uPA)-activatable photosensitizers
3.3 Fibroblast activation protein-α(FAPα)-activatable photosensitizers
3.4 Matrix metalloproteinase(MMP)-activatable photosensitizers
3.5 Hyaluronidase-activatable photosensitizers
3.6 Other enzyme-activatable photosensitizers
4 Nucleic acid-activatable photosensitizers
5 Other activatable photosensitizers
6 Perspective
Key words: activatable photosensitizer, cancer, photodynamic therapy

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可激活抗癌光敏剂