The Institute For Advanced Studies, Wuhan University, Luojiashan, Wuhan, 430072, China.
Key Laboratory of Biomedical Polymers-Ministry of Education, College of Chemistry and Molecular Sciences, Wuhan University, Luojiashan, Wuhan, 430072, China.
Angew Chem Int Ed Engl. 2019 Oct 1;58(40):14213-14218. doi: 10.1002/anie.201909020. Epub 2019 Aug 16.
Covalent organic frameworks (COFs) with 2D π-conjugation were designed and synthesized as molecular photosensitizers for efficient photodynamic therapy. Two molecules, 5',5''''-(1,4-phenylene)bis(([1,1':3',1''-terphenyl]-4,4''-dicarbaldehyde)) (L-3C) and 4,4',4''-(1,4-phenylene)bis(([2,2':6',2''-terpyridine]-5,5''-dicarbaldehyde)) (L-3N), inactive to generating reactive oxygen species (ROS), were linked to form two COFs, COF-808 and COF-909, respectively, exhibiting excellent ROS production efficiency. The high permanent porosity of these COFs (surface areas 2270 and 2610 m g ) promoted diffusion of both oxygen and release of ROS in cells. This, combined with the excellent photostability and biocompatibility, led to excellent PDT performance. In vitro, over 80 % of tumor cells were killed after PDT treatment using COF-909 at the concentration of 50 μg mL for 150 s. In vivo, drastic reduction of tumor size was observed (from 9 mm to less than 1 mm) after 10 day treatment.
具有二维π共轭的共价有机骨架（COFs）被设计并合成作为分子光动力治疗的光敏剂。两个分子，5'，5''''-（1,4-亚苯基）双（[[1,1':3',1''-三联苯]-4,4''-二醛]）（L-3C）和 4,4'，4''-（1,4-亚苯基）双（[[2,2':6',2''-三联吡啶]-5,5''-二醛]）（L-3N），不具有生成活性氧物种（ROS）的能力，分别连接形成两个 COFs，COF-808 和 COF-909，表现出优异的 ROS 生成效率。这些 COFs 的高永久孔隙率（表面积分别为 2270 和 2610 m g ）促进了氧气的扩散和 ROS 在细胞中的释放。这与优异的光稳定性和生物相容性相结合，导致了优异的 PDT 性能。在体外，在用 COF-909 在 50 μg mL 的浓度下处理 150 s 后，超过 80％的肿瘤细胞在 PDT 治疗后被杀死。在体内，在用 COF-909 治疗 10 天后，观察到肿瘤大小急剧减小（从 9 mm 减少到小于 1 mm）。
