In photodynamic therapy (PDT), the level of reactive oxygen species (ROS) produced in the cell directly determines the therapeutic effect. Improvement in ROS concentration can be realized by reducing the glutathione (GSH) level or increasing the amount of photosensitizer. However, excessive amounts photosensitizer may cause side effects. Therefore, the development of photosensitizers that reduce GSH levels through synergistically improving ROS concentration in order to strengthen the efficacy of PDT for tumor is important. We report a nano‐metal–organic framework (Cu^II‐metalated nano‐MOF {CuL‐[AlOH]₂}_n (MOF‐2, H₆L=mesotetrakis(4‐carboxylphenyl)porphyrin)) based on Cu^II as the active center for PDT. This MOF‐2 is readily taken up by breast cancer cells, and high levels of ROS are generated under light irradiation. Meanwhile, intracellular GSH is considerably decreased owing to absorption on MOF‐2; this synergistically increases ROS concentration and accelerates apoptosis, thereby enhancing the effect of PDT. Notably, based on the direct adsorption of GSH, MOF‐2 showed a comparable effect with the commercial antitumor drug camptothecin in a mouse breast cancer model. This work provides strong evidence for MOF‐2 as a promising new PDT candidate and anticancer drug.

中文翻译：

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通过使用以CuII为活性中心的纳米MOF，降低细胞内谷胱甘肽的水平来增强光动力疗法

在光动力疗法（PDT）中，细胞中产生的活性氧（ROS）的水平直接决定了治疗效果。可以通过降低谷胱甘肽（GSH）含量或增加光敏剂的量来实现ROS浓度的提高。但是，过量的光敏剂可能会引起副作用。因此，开发通过协同提高ROS浓度来降低GSH含量以增强PDT对肿瘤的疗效的光敏剂至关重要。我们报告的纳米金属-有机构架（铜^II -metalated纳米MOF {尽头[AlOH] ₂ } _Ñ（MOF-2，H ₆基于Cu L = mesotetrakis（4-羧基苯基）卟啉））^II作为PDT的活跃中心。这种MOF-2容易被乳腺癌细胞吸收，并且在光照射下会产生大量的ROS。同时，由于MOF-2的吸收，细胞内GSH显着降低。这协同增加了ROS浓度并加速了细胞凋亡，从而增强了PDT的作用。值得注意的是，基于GSH的直接吸附，MOF-2在小鼠乳腺癌模型中显示出与商业抗肿瘤药物喜树碱相当的效果。这项工作为MOF-2作为有希望的新型PDT候选药物和抗癌药物提供了有力的证据。