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莱涅佐利德和万科米辛与一种小型合成的2 - 默卡普托索衍生物的抗微生物协同作用:解决MRSA的挑战

Marilena Muraglia¹, Brigida Immacolata Pia Schiavone¹, Antonio Rosato¹

¹Dipartimento di Farmacia-Scienze del Farmaco, Università Degli Studi di Bari "A. Moro", Campus Universitario E. Quagliarello Via Orabona 4, 70125 Bari, Italy.

Molecules (Basel, Switzerland)

|September 9, 2023

概括

一种新的化合物BTZ2e显示出对抗MRSA和MRSE等耐药细菌的前景. 它与现有的抗生素Linezolid和Vancomycin协同作用,抑制浮游生物和生物膜细菌的生长.

科学领域:

微生物学微生物学
药用化学医学化学
抗微生物耐药性抗微生物耐药性

背景情况:

甲素耐药黄金葡萄球菌 (MRSA) 构成重大威胁,原因是持续性感染和具有挑战性的细菌病,由生物膜形成加剧.
现有的抗生素往往对MRSA和MRSE进行斗争,需要新的治疗策略.
开发新的抗菌剂对于克服抗菌素耐药性至关重要.

研究的目的:

为了研究一种新型的2-mercaptobenzothiazole衍生物BTZ2e与Linezolid (LNZ) 和Vancomycin (VAN) 结合的体外协同活性.
评估BTZ2e对临床MRSA,MRSE和对照菌株的浮游生物和生物膜培养的疗效.
确定BTZ2e作为对抗多药耐药细菌的辅助疗法的潜力.

主要方法:

用微稀释试验来评估浮游生物细菌细胞的易感性.
使用XTT减小试验来评估代谢活性和生物膜形成的抑制.
确定BTZ2e针对各种葡萄球菌菌株的最小生物膜抑制度 (MBIC50) 值.

主要成果:

在测试的菌株中,BTZ2e显著抑制了生物膜的形成.
在BTZ2e检测中,MBIC50值在16μg/mL到256μg/mL之间,针对不同的MRSA和MRSE单独体.
观察到BTZ2e与LNZ和VAN结合的协同效应 (FICI ≤0.5) 对浮游生物和静态细菌.
最有效的协同效应组合是浮游生物细胞的LNZ + BTZ2e和状细胞的VAN + BTZ2e.

结论:

BTZ2e具有强大的抗菌活性,并有效抑制生物膜的形成.
该化合物在与Linezolid和Vancomycin等已知抗生素相结合时显示出显著的协同效应.
BTZ2e代表了一种有前途的辅助治疗剂,用于治疗由MRSA和MRSE等多耐药菌株引起的感染.

关键词:

在FICI中,FICI是FICI,FICI是FICI.在MRSA和MRSE中,黄金葡萄球菌黄金葡萄球菌在XTT测试中进行测试.抗生物膜是一种抗生物膜.抗生素耐药性抗生素耐药性班佐提亚 (benzothiazole) 是一种一种小分子分子小分子有协同作用的协同作用.

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