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首页> 外文期刊>RSC Advances >Benzocyclohexane oxide derivatives and neolignans from Piper betle inhibit efflux-related resistance in Staphylococcus aureus
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Benzocyclohexane oxide derivatives and neolignans from Piper betle inhibit efflux-related resistance in Staphylococcus aureus

机译：苯并氯己烷氧化物衍生物和来自吹笛剂浸渍剂的新血碳抑制金黄色葡萄球菌中的流出相关性

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摘要

This research seeks to address the problem of methicillin-resistant Staphylococcus aureus (MRSA) by discovering synergistic antibacterial natural substances from traditional Chinese herbs using antibacterial bioassays. Six compounds, including three neolignans (-)-acuminatin (1), (-)-denudatin B (2), puberulin D (3), and three benzocyclohexane oxide derivatives ferrudiol (4), ellipeiopsol B (5) and zeylenol (6), were isolated and purified by silica gel and reverse-phase silica gel column chromatography, and the chemical structures were determined through NMR spectroscopy, MS, together with CD and calculated CD spectroscopic methods. Synergistic activity was determined using strain SA1199B, a strain that overexpresses the major S. aureus multidrug transporter, NorA. Compounds 1-6 showed synergistic activity combined with norfloxacin against SA1199B, with FICI values of 0.13, 0.25, 0.25, 0.52, 0.08 and 0.27 respectively. The synergistic effects of the benzocyclohexane oxide derivatives with norfloxacin were further demonstrated through strain growth kinetics experiments. In the mechanistic experiment, the compounds showed significant accumulation and/or inhibition effects for EtBr efflux in SA1199B. These active compounds showed no toxicity to HEK293T cells at a concentration of 100 mu M in the cytotoxicity evaluation experiments. Combined with efflux pump inhibitors, classic antibiotics that are substrates for efflux pumps may yet play a role in the therapy of drug-resistant bacteria where a lower dose could result in improved safety.
机译：该研究旨在通过使用抗菌生物测量法发现来自中草药的协同抗菌天然物质来解决耐素抗性葡萄球菌（MRSA）的问题。六种化合物，包括三种新核素（ - ） - 磷酸（1），（ - ） - Denudatin B（2），蒲吩蛋白D（3）和三个苯并苯二甲酸氧化物衍生物Ferrudiol（4），Ellipeolb（5）和Zeylenol（6 ）通过硅胶和反相硅胶柱色谱分离和纯化，并通过NMR光谱，MS与CD和计算的CD光谱法测定化学结构。使用菌株SA1199B测定协同活性，该菌株过表现出主要的S.UUREUS Multidrug Transporter，Nora。化合物1-6显示了与SA1199B相对于诺氟沙星联合的协同活性，FICI值分别为0.13,0.25,0.25,0.52,0.08和0.27。通过菌株生长动力学实验进一步证明了苯并辛己烷氧化物衍生物与诺氟沙星的协同效应。在机械实验中，化合物对SA1199B的EtBR Efflux显示出显着的积累和/或抑制作用。这些活性化合物在细胞毒性评估实验中以100μm的浓度为HEK293T细胞没有毒性。结合流水泵抑制剂，作为流出泵的底物的经典抗生素可能在耐药细菌的治疗中起作用，其中较低剂量可能导致安全性改善。

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  • 来源
    《RSC Advances》 |2016年第49期|共8页
  • 作者

    Sun Zhong-Lin; He Jian-Ming; Wang Shuang-Ying; Ma Ru; Khondkar Proma; Kaatz Glenn W.; Gibbons Simon; Mu Qing;

  • 作者单位

    Fudan Univ Sch Pharm Shanghai 201203 Peoples R China;

    Fudan Univ Sch Pharm Shanghai 201203 Peoples R China;

    Fudan Univ Sch Pharm Shanghai 201203 Peoples R China;

    Fudan Univ Sch Pharm Shanghai 201203 Peoples R China;

    UCL Sch Pharm Res Dept Pharmaceut &

    Biol Chem London WC1N 1AX England;

    Wayne State Univ John D Dingell Dept Vet Affairs Med Ctr Detroit MI 48201 USA;

    UCL Sch Pharm Res Dept Pharmaceut &

    Biol Chem London WC1N 1AX England;

    Fudan Univ Sch Pharm Shanghai 201203 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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