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新型天然洞灵感的两动物作为膜向抗菌剂对抗抗甲素耐药黄金葡萄球菌 (MRSA)

Ruige Yang¹, Zihan Xue², Xinhui Li²

¹Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, School of Pharmaceutical Science, Hengyang Medical School, University of South China, Hengyang, 421001, Hunan Province, China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, Henan Province, China.

European journal of medicinal chemistry

|May 1, 2024

概括

开发了新型的洞两动物来对抗抗生素耐药的细菌. 化合物6aa对抗抗甲素耐药黄金葡萄球菌 (MRSA) 具有强烈活性,并具有低毒性的快速杀死细菌.

科学领域:

药用化学医学化学
抗微生物药物发现发现
分子药理学分子药理学

背景情况:

甲素耐药黄金葡萄球菌 (MRSA) 由于其多药耐药性而构成重大威胁.
迫切需要新型抗菌剂来克服MRSA感染.

研究的目的:

设计和合成新型的洞两生物作为潜在的抗MRSA剂.
评估这些化合物对MRSA的体外和体内疗效.

主要方法:

由抗微生物 (AMP) 启发的 Osthole 两性动物 (6a-6ad) 的合成.
抗菌试验用于确定针对S. aureus和MRSA分离物的最小抑制度 (MIC).
评估细菌杀死动力学,耐药性潜力,毒性,膜选择性和等离子体稳定性.
涉及细菌膜相互作用,活性氧物种 (ROS) 生成和细胞组件泄漏的机制研究.
在动物模型中的体内疗效研究和对益炎性细胞因子 (TNF-α,IL-6) 的分析.

主要成果:

洞两6aa证明了S. aureus和10个临床MRSA分离物的强烈抑制 (MIC:1-2μg/mL),与万科米相似.
化合物6aa表现出快速杀死细菌,低毒性,良好的膜选择性和血稳定性,没有易于发展的耐药性.
机械学研究显示,通过与酸糖醇 (PG) 结合而破坏膜,导致ROS增加,DNA/蛋白质泄漏和细菌死亡.
在体内研究表明,6aa具有优越的抗MRSA疗效,与万科米辛相比,并减少MRSA诱导的TNF-α和IL-6.

结论:

洞两6aa是对抗MRSA感染的有希望的候选者.
它的机制涉及细菌膜的破坏和炎症反应的调制.
进一步开发6aa可能会导致对抗MRSA感染的有效治疗方法.

关键词:

具有抗菌活性,具有抗菌活性.细菌耐药性的细菌耐药性膜准机制的机制甲基西林耐药的金黄色葡萄球菌 (Staphylococcus aureus) 是一种东洞灵感的两动物有毒性有毒性

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