Tuning Organelle Specificity and Photodynamic Therapy Efficiency by Molecular Function Design
Tuning Organelle Specificity and Photodynamic Therapy Efficiency by Molecular Function Design
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DOI：
10.1021/acsnano.9b04430
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发表时间：
2019-10-01
期刊：
影响因子：
17.1
通讯作者：
Tang, Ben Zhong
中科院分区：
文献类型：
--
作者：
Liu, Zhiyang;Zou, Hang;Tang, Ben Zhong
高效有机光敏剂（PS）因其在光动力疗法（PDT）中的良好应用而备受关注。然而，关于其分子设计的指导方针却很少报道。在这项工作中，基于三苯胺-氮杂芴酮核设计并合成了一系列PS。系统地研究了它们的结构-性能-应用关系。阳离子化是通过靶向线粒体来提高 PSs 的 PDT 效率的有效策略。从分子分散态到聚集态，由于分子内运动的限制和系间窜越的增强，具有聚集诱导发射（AIE）的PS的荧光和活性氧生成效率增加。与靶向脂滴的非离子化 PS 相比，阳离子化线粒体靶向 PS 显示出更高的 PDT 效率。 PDT与放射治疗相结合可以进一步增强AIE PS杀死癌细胞的能力。这些结果应该会激发设计和合成具有更好的 PDT 效率和性能的 AIE PS 的研究热情。
Efficient organic photosensitizers (PSs) have attracted much attention because of their promising applications in photodynamic therapy (PDT). However, guidelines on their molecular design are rarely reported. In this work, a series of PSs are designed and synthesized based on a triphenylamine-azafluorenone core. Their structure-property-application relationships are systematically studied. Cationization is an effective strategy to enhance the PDT efficiency of PSs by targeting mitochondria. From the molecularly dispersed state to the aggregate state, the fluorescence and the reactive oxygen species generation efficiency of PSs with aggregation-induced emission (AIE) increase due to the restriction of the intramolecular motions and enhancement of intersystem crossing. Cationized mitochondrion-targeting PSs show higher PDT efficiency than that of nonionized ones targeting lipid droplets. The ability of AIE PSs to kill cancer cells can be further enhanced by combination of PDT with radiotherapy. Such results should trigger research enthusiasm for designing and synthesizing AIE PSs with better PDT efficiency and properties.