基于吡哆醇的季铵盐新衍生物对革兰氏阳性/阴性细菌的体外杀菌活性研究

M. Agafonova, Elizaveta D. Kobylinskaia, E. S. Bulatova, Alina S. Biktimirova, S. Sapozhnikov, N. Shtyrlin, Y. Shtyrlin
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摘要

背景:预防和成功治疗传染病(包括医院感染)是现代医疗保健最重要的任务之一。要解决这一问题,有效的防腐剂和消毒剂并不多。季铵盐是目前最有前途的消毒剂之一,但由于微生物对这些化合物产生抗药性,其使用受到了限制。用不同性质的取代基修饰季铵盐是解决这一问题的可行方法。目的:本研究对两种基于吡哆醇的原始季铵盐化合物与苯扎氯铵进行了杀菌活性比较分析。材料和方法:研究了 0.1%和 0.2%基于吡哆醇的原始季铵化合物水溶液对两种常见病原体的杀菌活性:金黄色葡萄球菌和大肠杆菌。抗菌活性数据是通过标准体外测试(金属表面杀菌活性测试,接触时间为 1、5 和 15 分钟)获得的。除标准条件外,还在蛋白质负载条件下(在表面上添加 BSA 溶液)研究了抗菌功效。结果:对于所研究的化合物,RF(减少因子-微生物的减少量 lgCFU)平均≥ 3。以蛋白质负荷的形式使模型条件复杂化会导致效率降低 1-3 个数量级。我们还观察到一个有趣的现象,即金黄色葡萄球菌和大肠杆菌的特异性逆转与暴露时间有关。结论:研究结果表明,所研究的化合物具有很高的活性(与该领域使用的商用化合物的有效性标准 RF≥3 相对应)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro study of the bactericidal activity for new derivatives of quaternary ammonium salts based on pyridoxine against gram-positive/gram-negative bacteria
Background: preventive care and successful treatment of infectious diseases (including hospital-acquired infections) are among the most important tasks of modern healthcare. There are not many effective antiseptics and disinfectants to solve this problem. Quaternary ammonium salts are currently one of the promising classes of disinfectants but their use is limited by the ability of microorganisms to develop resistance to these compounds. Modification of QAS with substituents of various natures is a possible way to solve this problem. Aims: in this work a bactericidal activity comparative analysis for two original quaternary ammonium compounds based on pyridoxine was carried out in comparison with benzalkonium chloride. Materials and methods: the bactericidal activity of 0.1% and 0.2% aqueous solutions of original QACs based on pyridoxine were studied against two widespread pathogens: S. aureus and E. coli. Antibacterial activity data were obtained using a standard in vitro test (bactericidal activity test on a metal surface, exposure time 1, 5 and 15 minutes). In addition to standard conditions, antibacterial efficacy was also studied under protein loading conditions (adding BSA solution to the surface). Results: for the studied compounds the RF (reduction factor - reduction lgCFU of microorganisms) was on average ≥ 3. Complicating the model conditions in the form of protein load led to a decrease in efficiency by 1-3 orders. We have also observed an interesting effect of exposure time-dependent specificity reversal to the S. aureus and E. coli. Conclusions: The obtained results showed high activity of the studied compounds (corresponding to the effectiveness criterion RF≥3 for commercial compounds used in this field).
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