Department of Chemical Biology and Bioimaging, Faculty of Chemistry, Wrocław University of Science and Technology, Wyb. Wyspiańskiego 27, 50-370, Wrocław, Poland.
Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wyb. Wyspiańskiego 27, 50-370, Wrocław, Poland.
Sci Rep. 2022 Mar 29;12(1):5319. doi: 10.1038/s41598-022-09210-z.
Due to market and legislative expectations, there is a constant need to explore new potential antimicrobial agents for functional perfumery. In this study, we evaluated the antimicrobial activity of 53 low molecular oximes and the corresponding carbonyl compounds against Escherichia coli, Enterococcus hirae, Pseudomonas aeruginosa, Bacillus cereus, Staphylococcus aureus, Aspergillus brasiliensis, Legionella pneumophila and Candida albicans. The most potent compound was α-isomethylionone oxime, which exhibited a minimum inhibitory concentration (MIC) of 18.75 µg/mL against E. hirae. The evaluation of the MICs for bacterial and fungal strains was performed for selected compounds, for example, the MIC of 2-phenylpropionaldehyde, cis-jasmone oxime, and trans-cinnamaldehyde measured against A. brasiliensis was 37.50 µg/mL. ADME-Tox (Absorption, Distribution, Metabolism, Excretion, and Toxicity) and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays were performed to assess the cytotoxicity of tested compounds. ADME-Tox indicated the safety and promising properties of selected compounds, which enables their usage as nontoxic supporting antibacterial agents. The results of the in vitro MTS assay were consistent with the ADME-Tox results. None of the compounds tested was toxic to Human Embryonic Kidney 293T (HEK293T) cells, with all cell viabilities exceeding 85%.
由于市场和立法方面的期望，我们不断需要探索新的潜在抗菌剂，以应用于功能性香水。在这项研究中，我们评估了 53 种低分子肟类化合物及其相应羰基化合物对大肠杆菌、屎肠球菌、铜绿假单胞菌、蜡状芽孢杆菌、金黄色葡萄球菌、巴西曲霉、嗜肺军团菌和白色念珠菌的抗菌活性。最有效的化合物是α-异甲基紫罗兰酮肟，其对屎肠球菌的最小抑菌浓度（MIC）为 18.75 µg/mL。针对选定的化合物，我们评估了细菌和真菌菌株的 MIC 值，例如，2-苯基丙醛、顺式茉莉酮肟和反式肉桂醛对巴西曲霉的 MIC 值为 37.50 µg/mL。我们还进行了吸收、分布、代谢、排泄和毒性（ADME-Tox）和 3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲氧基苯基)-2-(4-磺苯基)-2H-四唑（MTS）细胞活力测定，以评估测试化合物的细胞毒性。ADME-Tox 表明选定化合物具有安全性和良好的特性，使其可作为非毒性的支持抗菌剂使用。体外 MTS 测定的结果与 ADME-Tox 的结果一致。在测试的化合物中，没有一种对人胚肾 293T（HEK293T）细胞有毒性，所有细胞活力均超过 85%。
