LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
CESAM, Department of Biology, University of Aveiro, 3810-193 Aveiro, Portugal.
Int J Mol Sci. 2023 Feb 15;24(4):3922. doi: 10.3390/ijms24043922.
Antimicrobial photodynamic therapy (aPDT) has been explored as an innovative therapeutic approach because it can be used to inactivate a variety of microbial forms (vegetative forms and spores) without causing significant damage to host tissues, and without the development of resistance to the photosensitization process. This study assesses the photodynamic antifungal/sporicidal activity of tetra- and octasubstituted phthalocyanine (Pc) dyes with ammonium groups. Tetra- and octasubstituted zinc(II) phthalocyanines ( and ) were prepared and tested as photosensitizers (PSs) on conidia. Photoinactivation (PDI) tests were conducted with photosensitizer (PS) concentrations of 20, 40, and 60 µM under white-light exposure at an irradiance of 135 mW·cm, applied during 30 and 60 min (light doses of 243 and 486 J·cm). High PDI efficiency corresponding to the inactivation process until the detection limit was observed for both PSs. The tetrasubstituted PS was the most effective, requiring the lowest concentration and the shortest irradiation time for the complete inactivation of conidia (40 µM, 30 min, 243 J·cm). Complete inactivation was also achieved with PS , but a longer irradiation time and a higher concentration (60 µM, 60 min, 486 J·cm) were necessary. Because of the low concentrations and moderate energy doses required to inactivate resistant biological forms such as fungal conidia, these phthalocyanines can be considered potent antifungal photodynamic drugs.
抗菌光动力疗法 (aPDT) 作为一种创新的治疗方法得到了探索,因为它可以用于灭活各种微生物形式(营养形式和孢子),而不会对宿主组织造成显著损伤,并且不会对光敏化过程产生抗性。本研究评估了具有铵基团的四取代和八取代酞菁(Pc)染料的光动力抗真菌/杀孢子活性。合成了四取代和八取代锌 (II) 酞菁 () 和 ,并将其作为光敏剂 (PS) 对 分生孢子进行了测试。在 135 mW·cm 的辐照度下,用白光照射,进行光灭活 (PDI) 测试,PS 浓度分别为 20、40 和 60 µM,持续 30 和 60 min(光剂量为 243 和 486 J·cm)。两种 PS 都表现出高的 PDI 效率,对应于直至检测极限的失活动力学。四取代 PS 最有效,需要最低浓度和最短的照射时间才能完全灭活分生孢子(40 µM,30 min,243 J·cm)。PS 也能实现完全失活,但需要更长的照射时间和更高的浓度(60 µM,60 min,486 J·cm)。由于需要低浓度和适度的能量剂量来灭活抗性生物形式,如真菌分生孢子,这些酞菁可以被认为是有效的抗真菌光动力药物。