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Enhanced anti-microbial effect through cationization of a mono-triazatricyclodecane substituted asymmetric phthalocyanine
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2018-10-06 , DOI: 10.1016/j.jinorgbio.2018.10.001
Huajian Lin , Jincan Chen , Yaxin Zhang , Azeem Ulla , Jianyong Liu , Fan Lin , Longguang Jiang , Mingdong Huang

Antimicrobial photodynamic therapy (aPDT) is an effective way to combat infectious diseases and antibiotic resistance. Photosensitizer is a key factor of aPDT and has triggered extensive research interest. In this study, a new asymmetric Zn(II) phthalocyanine mono-substituted with a triazatricyclodecane moiety (compound 3) and its cationic N-methylated derivative (compound 4) were synthesized. Their photodynamic antimicrobial activities were evaluated using bioluminescent bacterial strains. Compound 3 showed phototoxicity only toward the Gram-positive bacteria, whereas the cationic derivative compound 4 exhibited strong anti-bacterial activity against both Gram-positive and Gram-negative strains. These bacterial species were eradicated (>4.0 logs or 99.99% killing) at appropriate concentrations of compound 4 with 12.7 J/cm2 of red light, demonstrating compound 4 as a potent aPDT agent.



中文翻译:

通过单三氮杂三环癸烷取代的不对称酞菁的阳离子化增强的抗菌作用

抗菌素光动力疗法(aPDT)是对抗传染病和抗生素耐药性的有效方法。光敏剂是aPDT的关键因素,并引起了广泛的研究兴趣。在这项研究中,合成了三氮杂三环癸烷部分(化合物3)单取代的新型不对称Zn(II)酞菁及其阳离子N-甲基化衍生物(化合物4)。使用生物发光细菌菌株评估了它们的光动力学抗菌活性。化合物3仅对革兰氏阳性细菌显示光毒性,而阳离子衍生物化合物4对革兰氏阳性和革兰氏阴性菌株均表现出强大的抗菌活性。这些化合物在适当浓度的化合物4和12.7 J / cm 2的红光下被消灭(> 4.0 log或99.99%的杀灭率),证明化合物4为有效的aPDT试剂。

更新日期:2018-10-06
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