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首页> 外文期刊>The Journal of Antibiotics: An International Journal >In vitro antibacterial activity of MGDG-palmitoyl from Oscillatoria acuminata NTAPC05 against extended-spectrum beta-lactamase producers
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In vitro antibacterial activity of MGDG-palmitoyl from Oscillatoria acuminata NTAPC05 against extended-spectrum beta-lactamase producers

机译：来自散射型β-内酰胺酶生产商的振荡症acuminata ntapc05的Mgdg-palmitoyl的体外抗菌活性

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摘要

Extended-spectrum beta-lactamase (ESBL)-producing bacteria pose a big challenge in clinical practices, warranting a new therapeutic strategy. In this study, methanol extract of the marine cyanobacterium Oscillatoria acuminata NTAPC05 was fractionated under bioassay guidance and the fractions were tested against three well-characterized ESBL-producing bacteria Escherichia coli U655, Stenotrophomonas maltophilia B929 and Enterobacter asburiae B938. Out of the four HPLC fractions, fraction 2 showed bactericidal activity against all the three ESBL producers much more efficiently (MIC 100 mu g m1(-1)) than the fourth-generation cephalosporin (MIC >125 mu g m1(-1)). The active fraction was subjected to time-kill test at concentrations of 1/2 x MIC, 1 x MIC and 2 x MIC, and the results substantiated the bactericidal property of the fraction against the ESBL producers. Spectral analysis revealed monogalactosyldiacylglycerol containing a palmitoyl (MGDG-palmitoyl), being reported for the first time, as the active fraction, and its bactericidal property against ESBL producers was determined. The active fraction appears to damage the bacterial membrane leading to lysis of the cell, as revealed in confocal laser scanning microscopy (CLSM) analysis, that was confirmed in scanning electron microscopic analysis. Cytotoxicity assay revealed the 0. acuminata compound to be safe to a normal cell line HEK293 (human embryonic kidney cell). The in silico analysis of MGDG-palmitoyl revealed two successive H-bonding interactions with Leu198 of TEM1 beta-lactamase. Taken together, the MGDG-palmitoyl from 0. acuminata NTAPC05 offers potential to develop analogs as a therapeutic for bacteremia caused by ESBL producers.
机译：扩展光谱β-内酰胺酶（ESBL） - 发霉的细菌在临床实践中提出了大量挑战，需要进行新的治疗策略。在该研究中，在生物测定的引导下分馏出海洋角质瘤弧菌aciminata的甲醇提取物，并且对三种特征的ESBL-产生的细菌大肠杆菌U655，Stenotophomonas麦芽蛋白B929和肠杆菌才B938进行了馏分。在四个HPLC级分中，比第四代头孢菌素（MIC>125μgm1（-1））更有效地（Mic 100 mu g m1（-1））更有效地显示杀菌活性。在1/2×MIC，1×MIC和2×MIC的浓度下进行活性级分的时间杀死试验，结果证实了对ESBL生产者的级分的杀菌性能。光谱分析显示含有棕榈酰基（Mgdg-Palmityoy1）的单母酸二酰基甘油首次报道，作为活性级分，测定对ESBL生产者的杀菌性质。活性分数似乎损害了导致细胞裂解的细菌膜，如在扫描电子显微镜分析中确认的相辅相激光扫描显微镜（CLSM）分析中所示。细胞毒性测定显示出0.煤尘化合物对正常的细胞系HEK293（人胚胎肾细胞）是安全的。 MGDG-PalmItoyl的硅分析揭示了与TEM1β-内酰胺酶的Leu198连续的两个连续的H键合相互作用。从0. acuminata ntapc05的mgdg-palmitoyl一起占用，提供了潜在的威斯伯国生产者造成的菌血症的疗效。

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