Sun Zhiyuan, Zhou Shaona, Qiu Haixia, Gu Ying, Zhao Yuxia
Technical Institute of Physics and Chemistry, Chinese Academy of Sciences Beijing 100190 P. R. China
University of Chinese Academy of Sciences Beijing 100049 P. R. China.
RSC Adv. 2018 May 9;8(31):17073-17078. doi: 10.1039/c8ra02557f.
A series of novel water-soluble photosensitizers (PSs; M1-M5) based on 3-cinnamoylcoumarin derivatives, incorporating carboxylic acid salt (M1, M2), pyridine salt (M3, M4) and quaternary ammonium salt (M5) groups, were designed and synthesized. Their photophysical and photochemical properties and antimicrobial photodynamic inactivation (PDI) were investigated. M2, modified with two carboxylic acid salts, was unstable in phosphate-buffered saline (PBS). The four other PSs all showed higher binding/uptake to methicillin-resistant (MRSA), and compared with the clinical drug methylene blue (MB), except for M1 to . Furthermore, the three cationic PSs (M3-M5) exhibited equivalent antibacterial PDI efficacies against MRSA and compared with MB. The antifungal efficacies of M4 and M5 to were both significantly higher than that of MB, especially for M5, indicating that the quaternary ammonium-salt-modified coumarin derivative has substantial potential for antifungal PDI.
设计并合成了一系列基于3-肉桂酰香豆素衍生物的新型水溶性光敏剂（PSs；M1-M5），其包含羧酸盐（M1、M2）、吡啶盐（M3、M4）和季铵盐（M5）基团。研究了它们的光物理和光化学性质以及抗菌光动力灭活（PDI）。用两种羧酸盐修饰的M2在磷酸盐缓冲盐水（PBS）中不稳定。其他四种PSs对耐甲氧西林金黄色葡萄球菌（MRSA）均表现出更高的结合/摄取能力，并且与临床药物亚甲蓝（MB）相比，除了M1……此外，三种阳离子PSs（M3-M5）对MRSA表现出与MB相当的抗菌PDI效果。M4和M5对……的抗真菌效果均显著高于MB，尤其是M5，表明季铵盐修饰的香豆素衍生物在抗真菌PDI方面具有巨大潜力。
