Institute for Nanotechnology Innovation, Rhodes University, Makhanda 6140, South Africa.
Institute for Nanotechnology Innovation, Rhodes University, Makhanda 6140, South Africa.
Photodiagnosis Photodyn Ther. 2022 Jun;38:102863. doi: 10.1016/j.pdpdt.2022.102863. Epub 2022 Apr 14.
New tetrasubstituted zinc (II) and indium (III) phthalocyanines bearing dimethylamino chalcone group (complexes 3 and 4) as well as their quaternized analogs (3a and 4a) have been assessed for their photodynamic therapy (PDT) of cancer as well as photodynamic antimicrobial chemotherapy activities against biofilms and planktonic cultures of pathogenic bacteria of Staphylococcus aureus and Escherichia coli. Compared to the non-quaternized phthalocyanines 3 and 4, the cationic phthalocyanines 3a and 4a exhibit a higher photodynamic inactivation against the planktonic cells with log reduction values above 9 at a concentration of 1.25 µM. This was attributed to the positive charge which enhances cellular uptake. More interestingly, 3a and 4a show a higher photodynamic inactivation (less than 3% of S. aureus survived) on their biofilm counterparts thanks to their stronger affinity to these cells. 3a and 4a Pcs also exhibited interesting PDT activity against MCF-7 cancer cells giving IC values of 17.9 and 7.4 μM, respectively following 15 min irradiation. The obtained results in this work show that the positively charged phthalocyanines 3a and 4a are potential antibacterial photosensitizers that show some selectivity toward the Gram-positive and Gram-negative bacteria as well as MCF-7 breasts cancer cells.
新型四取代锌(II)和铟(III)酞菁，带有二甲氨基查耳酮基团（化合物 3 和 4）及其季铵化类似物（3a 和 4a），已被评估用于癌症的光动力疗法（PDT）以及针对金黄色葡萄球菌和大肠杆菌等病原菌浮游生物和生物膜的光动力抗菌化疗活性。与非季铵化酞菁 3 和 4 相比，阳离子酞菁 3a 和 4a 在 1.25 μM 浓度下对浮游细胞的光动力灭活具有更高的对数减少值，超过 9。这归因于增强细胞摄取的正电荷。更有趣的是，3a 和 4a 对其生物膜对应物表现出更高的光动力灭活（不到 3%的金黄色葡萄球菌存活），这要归功于它们对这些细胞更强的亲和力。3a 和 4a Pcs 对 MCF-7 癌细胞也表现出有趣的 PDT 活性，在 15 分钟照射后，IC 值分别为 17.9 和 7.4 μM。本工作中的结果表明，带正电荷的酞菁 3a 和 4a 是潜在的抗菌光敏剂，对革兰氏阳性和革兰氏阴性细菌以及 MCF-7 乳腺癌细胞具有一定的选择性。
