在Enterococcus faecalis和Staphylococcus aureus中拦截了Epoxide环到定数感应系统的拦截
Mohammed Y Refai1, Ahmed M Elazzazy1, Said E Desouky2,3
1Department of Biological Science, College of Science, University of Jeddah, Jeddah, Saudi Arabia.
AMB Express
|November 9, 2023
概括
带有环氧组的定数感知抑制剂 (QSI) 显示出作为抗抗生素耐药细菌的抗病毒剂的前景,如MRSA和VRE. 这些化合物通过干扰重要的信号通路来有效地解除病原体的作用.
科学领域:
- 微生物学 微生物学
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
背景情况:
- 抗生素耐药性对全球健康构成重大威胁,需要新的治疗策略.
- 质量感应抑制剂 (QSI) 提供了一种通过解除病原体而不是杀死它们的抗病毒性方法.
- 阳性细菌利用循环介导的定量体感应 (QS) 系统,如agr和fsr,这对于毒性至关重要.
研究的目的:
- 研究环氧组在QSI的抗病毒活性中的作用.
- 为了评估已知的天然环氧化物化合物的疗效作为QSIs对抗格兰阳性细菌QS系统.
- 探索结构-活性关系 (SAR) 和含有环氧化物化合物的in silico相互作用.
主要方法:
- 对Epoxide化合物的QSI活性进行选,以对抗ag和fsr QS系统.
- 对含有环氧化物的分子进行in silico分析和SAR研究.
- 测试自然环氧化物化合物,如Cerulenin和Fosfomycin的QSI特性.
主要成果:
- 两种环氧化物化合物,安布酸和赛内拉,被确定为农业和FSR QS系统的强有力的抑制剂.
- 大多数经过测试的含有环氧化物的抗生素在亚致死度下显示与QSI活性发生相关干扰.
- 环氧化物部分似乎参与了这些QSI的作用机制.
结论:
- 含有环氧化物的化合物,包括天然抗生素,可以作为有效的QSIs对抗阳性细菌.
- 这一发现支持以环氧化物为基础的QSI的发展,作为对抗抗生素耐药性感染的可行策略.
- 质量测试剂代表了传统抗生素化疗的有希望的替代品或辅助剂.
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