Lacerda Paula S S, Bartolomeu Maria, Gomes Ana T P C, Duarte Ana S, Almeida Adelaide, Faustino Maria A F, Neves Maria G P M S, Barata Joana F B
CESAM, University of Aveiro, 3810-193 Aveiro, Portugal.
LAQV-REQUIMTE and Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
Microorganisms. 2022 Jun 7;10(6):1167. doi: 10.3390/microorganisms10061167.
Corroles possess key photophysical and photochemical properties to be exploited as therapeutic agents in antimicrobial photodynamic therapy (aPDT). Herein, we present for the first time the antimicrobial efficiency of three corrole dimers and of the corresponding precursor against the Gram(+) bacterium Staphylococcus aureus. Additionally, to explore future clinical applications, the cytotoxicity of the most promising derivatives towards Vero cells was evaluated. The aPDT assays performed under white light irradiation (50 mW/cm2; light dose 450 J/cm2) and at a corrole concentration of 15 µM showed that some dimers were able to reduce 99.9999% of S. aureus strain (decrease of 5 log10 CFU/mL) and their photodynamic efficiency was dependent on position, type of linkage, and aggregation behavior. Under the same light conditions, the corrole precursor 1 demonstrated notable photodynamic efficiency, achieving total photoinactivation (>8.0 log10 CFU/mL reduction) after the same period of irradiation (light dose 450 J/cm2). No cytotoxicity was observed when Vero cells were exposed to corrole 1 and dimer 3 for 24 h according to ISO guidelines (ISO 10993-5) for in vitro cytotoxicity of medical devices. The results show that corrole dimers, dependent on their structures, can be considered good photosensitizers to kill Staphylococcus aureus.
咕啉具有关键的光物理和光化学性质，可作为抗菌光动力疗法（aPDT）中的治疗剂加以利用。在此，我们首次展示了三种咕啉二聚体及其相应前体对革兰氏阳性菌金黄色葡萄球菌的抗菌效率。此外，为探索未来的临床应用，还评估了最具潜力的衍生物对Vero细胞的细胞毒性。在白光照射（50 mW/cm2；光剂量450 J/cm2）和咕啉浓度为15 µM的条件下进行的aPDT试验表明，一些二聚体能够减少99.9999%的金黄色葡萄球菌菌株（降低5 log10 CFU/mL），并且它们的光动力效率取决于位置、连接类型和聚集行为。在相同光照条件下，咕啉前体1表现出显著的光动力效率，在相同照射时间（光剂量450 J/cm2）后实现了完全光灭活（>8.0 log10 CFU/mL降低）。根据医疗器械体外细胞毒性的ISO指南（ISO 10993-5），当Vero细胞暴露于咕啉1和二聚体3 24小时时，未观察到细胞毒性。结果表明，咕啉二聚体根据其结构可被视为杀灭金黄色葡萄球菌的良好光敏剂。
