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一种新型次氯酸响应型光敏剂的合成及其抗肿瘤活性

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光动力疗法(photodynamic therapy,PDT)是通过光激发敏剂产生活性氧(ROS)从而引起的肿瘤细胞凋亡或坏死,是一种非侵入式的肿瘤治疗方法.本研究基于酚噻嗪结构,设计并合成了一种新型次氯酸(HClO/ClO-)响应的光敏剂PTZPPy.使用NMR及HR-MS(ESI)对其结构进行了表征,使用紫外吸收光谱、荧光光谱等方法表征了其光物理性质,使用CCK8 法评价了其体外抗肿瘤活性.结果表明:PTZPPy自身不发出荧光,与ClO-响应后发出黄色荧光,PTZPPy具有良好的ROS产生能力和良好的抗肿瘤活性.
Synthesis and Anticancer Activity of A Novel Hypochlorite Responsive Photosensitizer
Photodynamic therapy(PDT)is a non-invasive tumor treatment modality,which produces reactive oxygen species(ROS)through light-activated sensitizers inducing tumor cells apoptosis or nec-rosis.In this study,a novel hypochlorite(HClO/ClO-)responsive photo-sensitizer PTZPPy was de-signed and synthesized based on the structure of phenthiazine.The structure of PTZPPy was confirmed by NMR and HR-MS(ESI),and the photophysical properties of PTZPPy were characterized by UV absorption and fluorescence spectroscopy.The anti-tumor activity of PTZPPy in vitro was evaluated by CCK8 method.The results demonstrated that PTZPPy emits no fluorescence,but emitted yellow fluo-rescence after being exposed to ClO-PTZPPy exhibited considerable ROS generation efficiency and good anti-tumor activity.

phenthiazinephotosensitizerreactive oxygen specieshypochlorous acidantitumor activity

赵勇强、袁家英、匡思颖、吴仕萍、张宁峰、黄统辉

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徐州医科大学 江苏省新药研究与临床药学重点实验室,江苏 徐州 221000

酚噻嗪 光敏剂 活性氧 次氯酸 抗肿瘤活性

江苏省大学生创新创业计划训练项目2023年江苏省研究生科研与实践创新计划

202110313028ZKYCX23-2938

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(3)
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