Enhanced anti-microbial effect through cationization of a mono-triazatricyclodecane substituted asymmetric phthalocyanine
Enhanced anti-microbial effect through cationization of a mono-triazatricyclodecane substituted asymmetric phthalocyanine
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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抗菌效果
DOI：
10.1016/j.jinorgbio.2018.10.001
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发表时间：
2018
影响因子：
3.9
通讯作者：
Huang M. D.
中科院分区：
文献类型：
--
作者：
Lin H. J;Chen J. C;Zhang Y. X;Ulla A;Liu J. Y;Lin F;Jiang L. G;Huang M. D.
抗菌光动力疗法（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，引起了广泛的研究兴趣。在本研究中，合成了一种被三氮杂三环癸烷部分单取代的新型不对称Zn(II)酞菁（化合物3）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它们的光动力抗菌活性。化合物3仅对革兰氏阳性菌表现出光毒性，而阳离子衍生物化合物4对革兰氏阳性菌和革兰氏阴性菌均表现出强抗菌活性。在适当浓度的化合物 4 和 12.7J/cm2 红光下，这些细菌物种被根除（>4.0 个对数或 99.99% 杀灭），证明化合物 4 是一种有效的 aPDT 试剂。
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 (compound3) and its cationicN-methylated derivative (compound4) were synthesized. Their photodynamic antimicrobial activities were evaluated using bioluminescent bacterial strains. Compound3showed phototoxicity only toward the Gram-positive bacteria, whereas the cationic derivative compound4exhibited 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 compound4with 12.7 J/cm2of red light, demonstrating compound4as a potent aPDT agent.