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氟芳基-2,2'-联二萘酚化合物对多药耐药性的生物学见解。

Biological Insights of Fluoroaryl-2,2'-Bichalcophene Compounds on Multi-Drug Resistant .

机构信息

Botany Department, Faculty of Science, Mansoura University, Elgomhouria St., Mansoura 35516, Egypt.

Chemistry Department, Faculty of Science, Mansoura University, Elgomhouria St., Mansoura 35516, Egypt.

出版信息

Molecules. 2020 Dec 30;26(1):139. doi: 10.3390/molecules26010139.

Abstract

Resistance of bacteria to multiple antibiotics is a significant health problem; hence, to continually respond to this challenge, different antibacterial agents must be constantly discovered. In this work, fluoroaryl-2,2'-bichalcophene derivatives were chemically synthesized and their biological activities were evaluated against (). The impact of the investigated bichalcophene derivatives was studied on the ultrastructural level via scanning electron microscopy (SEM), molecular level via sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) method and on the biofilm inhibition via the electrochemical biosensors. Arylbichalcophenes' antibacterial activity against was affected by the presence and location of fluorine atoms. The fluorobithiophene derivative displayed the best minimum inhibitory concentration (MIC) value of 16 µM among the tested fluoroarylbichalcophenes. Over a period of seven days, did not develop any resistance against the tested fluoroarylbichalcophenes at higher concentrations. The impact of fluoroarylbichalcophenes was strong on protein pattern showing high degrees of polymorphism. SEM micrographs of cells treated with fluoroarylbichalcophenes displayed smaller cell-sizes, fewer numbers, arranged in a linear form and some of them were damaged when compared to the untreated cells. The bioelectrochemical measurements demonstrated the strong sensitivity of cells to the tested fluoroarylbichalcophenes and an antibiofilm agent. Eventually, these fluoroarylbichalcophene compounds especially the could be recommended as effective antibacterial agents.

摘要

细菌对多种抗生素的耐药性是一个重大的健康问题;因此,为了不断应对这一挑战,必须不断发现新的抗菌剂。在这项工作中,我们合成了氟芳基-2,2'-双查尔酮衍生物,并评估了它们对()的生物活性。通过扫描电子显微镜(SEM)研究了所研究的双查尔酮衍生物在超微结构水平上的影响,通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳(SDS-PAGE)方法研究了分子水平上的影响,通过电化学生物传感器研究了生物膜抑制作用。芳基双查尔酮对()的抗菌活性受氟原子的存在和位置影响。在所测试的氟芳基双查尔酮中,氟代联噻吩衍生物 显示出最佳的最小抑菌浓度(MIC)值为 16 μM。在七天的时间内,()在较高浓度下对测试的氟芳基双查尔酮没有产生任何耐药性。氟芳基双查尔酮对()蛋白图谱的影响很大,表现出高度的多态性。用氟芳基双查尔酮处理的细胞的 SEM 显微照片显示,与未处理的细胞相比,细胞尺寸更小,数量更少,呈线性排列,有些细胞受损。生物电化学测量表明,测试的氟芳基双查尔酮对 细胞具有很强的敏感性,是一种抗生物膜剂。最终,这些氟芳基双查尔酮化合物,尤其是 ,可被推荐为有效的抗菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/710c/7795799/7744ab0c9d26/molecules-26-00139-g001.jpg

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