Qu Jiamin, Zhang Yahui, Cai Zhengxu, Tong Bin, Xie Haiyan, Dong Yuping, Shi Jianbing
Beijing Key Laboratory of Construction Tailorable Advanced Functional Materials and Green Applications, School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China.
School of Life Science, Advanced Research Institute of Multidisciplinary Science, Beijing Institute of Technology, Beijing 100081, China.
Nanoscale. 2022 Oct 6;14(38):14064-14072. doi: 10.1039/d2nr02273g.
Developing efficient photosensitizers (PSs) that can generate type I reactive oxygen species (ROS) under illumination is considered an effective way to improve photodynamic therapy (PDT) outcomes due to the hypoxic nature of the tumor environment, but also is very challenging. Herein, a new PS of the multiarylpyrrole (MAP) derivative with a typical donor-acceptor structure was synthesized to efficiently generate type I ROS by using an acceptor-shielding strategy in their aggregated state. The enhanced generation mechanism of type I ROS originated from its ultralong triplet lifetime and the narrow singlet-triplet energy gap of the MAP. More importantly, type I ROS can transform protumoral M2 macrophages (M2) into antitumoral M1 macrophages (M1), which showed synergistic immunotherapy in experiments. Therefore, introducing shielding groups into acceptors provides general guidance for developing efficient PSs in the aggregation state for clinical PDT.
由于肿瘤环境的缺氧特性，开发能够在光照下产生I型活性氧（ROS）的高效光敏剂（PSs）被认为是改善光动力疗法（PDT）效果的有效方法，但这也极具挑战性。在此，合成了一种具有典型供体-受体结构的新型多芳基吡咯（MAP）衍生物PS，通过在其聚集态采用受体屏蔽策略来高效产生I型ROS。I型ROS增强的产生机制源于其超长的三重态寿命和MAP狭窄的单重态-三重态能隙。更重要的是，I型ROS可将促肿瘤的M2巨噬细胞（M2）转化为抗肿瘤的M1巨噬细胞（M1），这在实验中显示出协同免疫治疗效果。因此，在受体中引入屏蔽基团为开发用于临床PDT的聚集态高效PSs提供了通用指导。
