Effects 4-(1-adamantyl)-phenoxy-3-(n-benzyl, n-dimethylamino)-2-propanol chloride on the strains of Pseudomonas Spp.

D. Dudikova, S. Voychuk, N. Vrynchanu
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Abstract

Pseudomonas aeruginosa is one of the main pathogens of nosocomial infections. High resistance of P. aeruginosa to modern antimicrobial agents leads to the decrease in the effectiveness of antibiotic chemotherapy and the need to search for new active compounds. Adamantane derivatives with a wide range of biological activity can be considered as a promising class of substances with an antimicrobial effect. Aim. In the present study, our purpose was to examine susceptibility and ultrastructural alterations of P. aeruginosa cells under the influence of 4-(1-adamantyl)-phenoxy-3-(N-benzyl, N-dimethylamino)-2-propanol chloride (compound KVM-97). Materials and methods. The antimicrobial activity assay of tested compound against bacteria of genus Pseudomonas was determined by serial dilution test in broth. Bacterial cells were exposed to the 0.5 MIC and 2.0 MIC of the KVM-97 for 1, 3, 6 and 24 h. Ultrastructure of intact and treated P. aeruginosa cells was examined by transmission electron microscopy after contrasting by uranyl acetate and lead citrate. Results. It was shown, that compound KVM-97 inhibited Pseudomonas spp growth at concentration 2.5 μg/ml. Examination of P. aeruginosa ultrastructure using electron microscopy showed that the cell and cytoplasmic membrane were damaged in the presence of KVM-97 (invaginations, ruptures) with followed disorganization of cell contents, lysis and cell death. These changes are dose-dependent, they are registered after 1 hour of exposure with the compound and intensified with the time of incubation. Conclusions. A study carried out with KVM-97 has shown that the compound possesses significant inhibitory activity against tested bacterial strains. The detected ultrastructural alterations of P. aeruginosa suggest the possible mechanism of action of 4-(1-adamantyl)-phenoxy-3-(N-benzyl, N-dimethylamino)-2-propanol chloride due to its influence on the membrane apparat in bacterial cell
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4-(1-金刚烷基)-苯氧基-3-(n-苄基,n-二甲氨基)-2-丙醇氯对假单胞菌的影响。
铜绿假单胞菌是医院感染的主要病原菌之一。铜绿假单胞菌对现代抗菌药物的高耐药性导致抗生素化疗效果下降,需要寻找新的活性化合物。金刚烷衍生物具有广泛的生物活性,是一类很有前途的抗菌物质。的目标。在本研究中,我们的目的是研究4-(1-金刚烷基)-苯氧基-3-(n -苄基,n -二甲氨基)-2-丙醇氯(化合物km -97)对铜绿假单胞菌细胞的易感性和超微结构的改变。材料和方法。采用连续稀释法测定所试化合物对肉汤中假单胞菌的抑菌活性。将细菌细胞分别置于0.5 MIC和2.0 MIC的KVM-97中1、3、6和24 h,通过乙酸铀酰和柠檬酸铅对比,透射电镜观察完整细胞和处理后P. aeruginosa细胞的超微结构。结果。结果表明,复方km -97在浓度为2.5 μg/ml时对假单胞菌的生长有抑制作用。电镜观察铜绿假单胞菌的超微结构,发现KVM-97的存在使细胞和细胞质膜受到损伤(内陷、破裂),细胞内容物解体、溶解和死亡。这些变化是剂量依赖性的,它们在与化合物接触1小时后被记录下来,并随着孵育时间的延长而增强。结论。用KVM-97进行的一项研究表明,该化合物对所测试的细菌菌株具有显著的抑制活性。铜绿假单胞菌的超微结构变化提示4-(1-金刚烷基)-苯氧基-3-(n -苄基,n -二甲氨基)-2-丙醇氯可能通过影响细菌细胞的膜装置而起作用
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