抗微生物光动力治疗(aPDT)为对抗微生物病原体提供了另一种选择,以这种方式,应对日益增长的抗菌素耐药性的挑战。在这种有希望和有效的方法中,阳离子卟啉和相关的大环已经成为aPDT的主要光敏剂(PS)。总的来说,它们的制备是通过用烷基卤化物将基于氮的部分进行N-烷基化,这限制了微调基于卟啉的PS的特征的能力。在这里,据报道,卟啉大环与三苯基鳞单元的缀合产生了一系列用于aPDT的有效的基于阳离子卟啉的PS。卟啉大环和三苯基鳞部分的正电荷的存在显着增强了基于卟啉的PS对革兰氏阳性和革兰氏阴性细菌菌株的光动力活性。此外,细菌光灭活与辐射时间显着减少,超过50%,与5,10,15,20-四(1-甲基吡啶-4-基)卟啉(TMPyP)相比,用作参考,被称为良好的PS。卟啉大环产生单线态氧的能力提高,加上三苯基鳞部分的存在促进的膜相互作用增强,代表了一种开发具有增强光敏活性的卟啉基PS的有希望的方法。
Antimicrobial photodynamic treatment (aPDT) offers an alternative option for combating microbial pathogens, and in this way, addressing the challenges of growing antimicrobial resistance. In this promising and effective approach, cationic porphyrins and related macrocycles have emerged as leading photosensitizers (PS) for aPDT. In general, their preparation occurs via N-alkylation of nitrogen-based moieties with alkyl halides, which limits the ability to fine-tune the features of porphyrin-based PS. Herein, is reported that the conjugation of
porphyrin macrocycles with triphenylphosphonium units created a series of effective cationic
porphyrin-based PS for aPDT. The presence of positive charges at both the porphyrin macrocycle and triphenylphosphonium moieties significantly enhances the photodynamic activity of
porphyrin-based PS against both Gram-positive and Gram-negative bacterial strains. Moreover, bacterial photoinactivation is achieved with a notable reduction in irradiation time, exceeding 50%, compared to 5,10,15,20-tetrakis(1-methylpyridinium-4-yl)
porphyrin (TMPyP), used as the reference and known as good PS. The improved capability of the
porphyrin macrocycle to generate singlet oxygen combined with the enhanced membrane interaction promoted by the presence of triphenylphosphonium moieties represents a promising approach to developing porphyrin-based PS with enhanced photosensitizing activity.