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Ferrocenyl chalcone derivatives as possible antimicrobial agents.
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2020-01-28 , DOI: 10.1038/s41429-020-0280-y
Elecia J Henry 1, 2 , Susan J Bird 1 , Pauline Gowland 1 , Michael Collins 3 , John P Cassella 4
Affiliation  

The swift spread of infections caused by drug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA), has quickly become a worldwide concern as infections spread from healthcare settings to the wider community. While ferrocenyl chalcones, which are chalcone derivatives with antimicrobial activity, have gained attention from researchers, further study is needed to assess their cytotoxicity. Ten newly developed chalcones, in which ring A was replaced with a ferrocenyl moiety and ring B contained increasing alkyl chain lengths from 1 to 10 carbons, were assessed. Using twofold broth microdilution, the minimum inhibitory concentration (MIC) of five of the ten compounds were lower against Gram-positive organisms (MICs from 0.008 mg ml-1 to 0.063 mg ml-1) than Gram-negative organisms (MICs = 0.125 mg ml-1). These novel ferrocenyl chalcone compounds were effective against three types of clinically isolated drug-resistant S. aureus, including an MRSA, and against other non-resistant clinically isolated and laboratory-adapted Gram-positive bacteria. The same compounds inhibited growth in non-resistant bacteria by potentially obstructing cellular respiration in Gram-positive bacteria. Images obtained through scanning electron microscopy revealed fully lysed bacterial cells once exposed to a selected compound that showed activity. The results indicate that these newly developed compounds could be important antimicrobial agents in the treatment of infections from clinically resistant bacteria.

中文翻译:

二茂铁基查耳酮衍生物可能是抗微生物剂。

由于耐药菌引起的感染的迅速传播,例如耐甲氧西林金黄色葡萄球菌(MRSA),已迅速引起全世界关注,因为感染已从医疗机构传播到更广泛的社区。尽管二茂铁基查耳酮是具有抗菌活性的查尔酮衍生物,已引起研究人员的注意,但仍需要进一步研究以评估其细胞毒性。评估了十个新开发的查耳酮,其中的A环被二茂铁基部分取代,B环的烷基链长度从1个碳增加到10个碳。使用双重肉汤微量稀释法,十种化合物中的五种对革兰氏阳性菌(MIC从0.008 mg ml-1到0.063 mg ml-1)的最低抑菌浓度(MIC)低于革兰氏阴性菌(MICs = 0.125 mg ml-1)。这些新颖的二茂铁基查耳酮化合物可有效对抗三种类型的临床分离的耐药金黄色葡萄球菌(包括MRSA)和其他非耐药的临床分离且实验室适应的革兰氏阳性细菌。相同的化合物通过潜在地阻碍革兰氏阳性菌的细胞呼吸来抑制非耐药菌的生长。通过扫描电子显微镜获得的图像显示,一旦暴露于具有活性的选定化合物,细菌细胞就会完全裂解。结果表明,这些新开发的化合物在治疗临床耐药细菌感染中可能是重要的抗菌剂。并针对其他非耐药临床分离和实验室适应的革兰氏阳性细菌。相同的化合物通过潜在地阻碍革兰氏阳性菌的细胞呼吸来抑制非耐药菌的生长。通过扫描电子显微镜获得的图像显示,一旦暴露于具有活性的选定化合物,细菌细胞就会完全裂解。结果表明,这些新开发的化合物在治疗临床耐药细菌感染中可能是重要的抗菌剂。并针对其他非耐药临床分离和实验室适应的革兰氏阳性细菌。相同的化合物通过潜在地阻碍革兰氏阳性菌的细胞呼吸来抑制非耐药菌的生长。通过扫描电子显微镜获得的图像显示,一旦暴露于具有活性的选定化合物,细菌细胞就会完全裂解。结果表明,这些新开发的化合物在治疗临床耐药细菌感染中可能是重要的抗菌剂。通过扫描电子显微镜获得的图像显示,一旦暴露于具有活性的选定化合物,细菌细胞就会完全裂解。结果表明,这些新开发的化合物在治疗临床耐药细菌感染中可能是重要的抗菌剂。通过扫描电子显微镜获得的图像显示,一旦暴露于具有活性的选定化合物,细菌细胞就会完全裂解。结果表明,这些新开发的化合物在治疗临床耐药细菌感染中可能是重要的抗菌剂。
更新日期:2020-01-28
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