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Study of the Mechanism of the Antimicrobial Activity of Novel Water Soluble Ammonium Quaternary Benzanthrone on Model Membranes.
The Journal of Membrane Biology ( IF 2.4 ) Pub Date : 2020-05-11 , DOI: 10.1007/s00232-020-00121-6
Asya Tsanova 1 , Vishnya Stoyanova 1 , Albena Jordanova 1 , Ivo Grabchev 1
Affiliation  

The increasing resistance of many pathogens to most of the common antimicrobials requires the development of new substances with more effective antimicrobial properties. In the present work, we investigated the mechanism of the antimicrobial activity of novel water soluble ammonium quaternary benzanthrone (Compound B) on model membranes, composed of dipalmitoylphosphatidylcholine, 1-palmitoyl-2-oleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, 1-palmitoyl-2-oleoylphosphatidylglycerol, and dipalmitoylphosphatidylethanolamine (DPPE). The lipids were chosen to represent a model of a bacterial membrane. The changes in surface pressure of the model membranes, before and after the addition of Compound B, were studied by the Langmuir's monolayer method, and the compressional modulus for each monolayer was determined. In addition, the surface morphology of the lipid monolayers before and after injection of Compound B was monitored by Brewster Angle Microscopy. The results showed that Compound B penetrated all the monolayers studied. The most noticeable effects were found with the negatively charged phosphatidylglycerols and with DPPE leading to the conclusion that the electrostatic interactions between the compound and the lipid head groups and the possible formation of hydrogen bonds between the amino group of the ethanolamine and the keto groups in the structure of Compound B are of great importance. In addition, the penetration ability of the benzoquinone with all phospholipids studied was stable even at higher values of the surface pressure, i.e. thicker monolayers, due to the hydrophobic interaction, which plays also an important role for the antimicrobial activity of Compound B.

中文翻译:

新型水溶性季铵盐对模型膜抗菌活性机理的研究。

许多病原体对大多数常见抗菌剂的耐药性不断增加,需要开发具有更有效抗菌特性的新物质。在目前的工作中,我们研究了新型水溶性季铵苯蒽酮(化合物 B)对模型膜的抗菌活性机制,模型膜由二棕榈酰磷脂酰胆碱、1-棕榈酰-2-油酰磷脂酰胆碱、二棕榈酰磷脂酰甘油、2-棕榈酰磷脂酰磷脂酰、2-棕榈酰磷脂酰胆碱组成。和二棕榈酰磷脂酰乙醇胺(DPPE)。选择脂质来代表细菌膜的模型。通过朗缪尔单层法研究模型膜在加入化合物 B 之前和之后的表面压力变化,并确定每个单层的压缩模量。此外,通过布鲁斯特角显微镜监测注射化合物B之前和之后的脂质单层的表面形态。结果表明化合物B渗透了所有研究的单层。最显着的影响是带负电荷的磷脂酰甘油和 DPPE 导致的结论是化合物和脂质头基之间的静电相互作用以及乙醇胺的氨基和酮基之间可能形成的氢键化合物 B 的结构非常重要。此外,苯醌对所有研究的磷脂的渗透能力即使在较高的表面压力值下也是稳定的,即较厚的单层,由于疏水相互作用,
更新日期:2020-05-11
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