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    邵堃

    • 教授     博士生导师   硕士生导师
    • 性别:女
    • 毕业院校:复旦大学
    • 学位:博士
    • 所在单位:化工学院
    • 办公地点:大连理工大学西校区化工实验楼 E532
    • 联系方式:shaok@dlut.edu.cn
    • 电子邮箱:shaok@dlut.edu.cn

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    An APN-activated NIR photosensitizer for cancer photodynamic therapy and fluorescence imaging

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    论文类型:期刊论文

    发表时间:2021-04-12

    发表刊物:BIOMATERIALS

    卷号:253

    ISSN号:0142-9612

    关键字:Aminopeptidase N; Enzyme-activated photosensitizer; PDT; NIR fluorescence imaging

    摘要:Photodynamic therapy has been developed as a prospective cancer treatment in recent years. Nevertheless, conventional photosensitizers suffer from lacking recognition and specificity to tumors, which causing severe side effects to normal tissues, while the enzyme-activated photosensitizers are capable of solving these conundrums due to high selectivity towards tumors. APN (Aminopeptidase N, APN/CD13), a tumor marker, has become a crucial targeting substance owing to its highly expressed on the cell membrane surface in various tumors, which has become a key point in the research of anti-tumor drug and fluorescence probe. Based on it, herein an APN-activated near-infrared (NIR) photosensitizer (APN-CyI) for tumor imaging and photodynamic therapy has been firstly developed and successfully applied in vitro and in vivo. Studies showed that APN-CyI could be activated by APN in tumor cells, hydrolyzed to fluorescent CyI-OH, which specifically located in mitochondria in cancer cells and exhibited a high singlet oxygen yield under NIR irradiation, and efficiently induced cancer cell apoptosis. Dramatically, the in vivo assays on Balb/c mice showed that APN-CyI could achieve NIR fluorescence imaging (lambda(em) = 717 nm) for endogenous APN in tumors and possessed an efficient tumor suppression effect under NIR irradiation.