阳离子甾体抗生素CSA - 13、CSA - 131、CSA - 138、CSA - 142和CSA - 192对耐碳青霉烯类抗生素的活性
Activities of the Cationic Steroid Antibiotics CSA-13, CSA-131, CSA-138, CSA-142, and CSA-192 Against Carbapenem-resistant .
作者信息
Bozkurt Güzel Çağla, Avci Nevin Meltem, Savage Paul
机构信息
İstanbul University, Faculty of Pharmacy, Department of Pharmaceutical Microbiology, İstanbul, Turkey.
Brigham Young University, Department of Chemistry and Biochemistry, Provo, Utah, USA.
出版信息
Turk J Pharm Sci. 2020 Feb;17(1):63-67. doi: 10.4274/tjps.galenos.2018.26566. Epub 2020 Feb 19.
OBJECTIVES
is an important opportunistic pathogen that is difficult to treat because of the antibiotic resistance that has developed in recent years. Increasing carbapenem resistance has led to a rise in hospital infections caused by this bacterium. As a result, researchers have begun to search for new molecules. Ceragenins are the general name for membrane-acting cationic steroid antimicrobial molecules that have activity similar to that of antimicrobial peptides. In this study, we investigated the activities of the cationic steroid antibiotics (CSAs) CSA-13, CSA-131, CSA-138, CSA-142, CSA-192, and colistin on carbapenem-resistant (CRPA).
MATERIALS AND METHODS
Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined by broth dilution method.
RESULTS
The MIC (μg/mL) values of CSA-13, CSA-131, CSA-138, CSA-142, CSA-192, colistin, and meropenem were 8, 4, 8, 16, 32, 1, and 16, respectively. The MBC values were equal to or twice the MIC values.
CONCLUSION
CSA-131 and CSA-138 appear to be good candidates for CRPA treatment. However, the lack of stability, efficacy, and pharmacokinetic properties of CSA requires further research in the future and .
目的
是一种重要的机会性病原体，由于近年来产生的抗生素耐药性，难以治疗。碳青霉烯类耐药性的增加导致了由这种细菌引起的医院感染的上升。因此，研究人员开始寻找新的分子。西拉菌素是一类膜活性阳离子甾体抗菌分子的统称，其活性与抗菌肽相似。在本研究中，我们研究了阳离子甾体抗生素（CSA）CSA-13、CSA-131、CSA-138、CSA-142、CSA-192和黏菌素对耐碳青霉烯类肺炎克雷伯菌（CRPA）的活性。
材料与方法
采用肉汤稀释法测定最低抑菌浓度（MIC）和最低杀菌浓度（MBC）。
结果
CSA-13、CSA-131、CSA-138、CSA-142、CSA-192、黏菌素和美罗培南的MIC（μg/mL）值分别为8、4、8、16、32、1和16。MBC值等于或为MIC值的两倍。
结论
CSA-131和CSA-138似乎是治疗CRPA的良好候选药物。然而，CSA缺乏稳定性、疗效和药代动力学特性，未来需要进一步研究。
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