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姜辣素作为抗 QS 分子的兴起:LuxR 介导的生物发光传奇中的最黑暗篇章。

The rise of gingerol as anti-QS molecule: Darkest episode in the LuxR-mediated bioluminescence saga.

机构信息

Department of Microbiology & Biotechnology, University School of Sciences, Gujarat University, Ahmedabad 380009, Gujarat, India.

Department of Biochemistry & Forensic Science, University School of Sciences, Gujarat University, Ahmedabad 380009, Gujarat, India.

出版信息

Bioorg Chem. 2020 Jun;99:103823. doi: 10.1016/j.bioorg.2020.103823. Epub 2020 Apr 8.

Abstract

The phenomenon of bioluminescence is the most widely investigated model of quorum sensing (QS) that occurs in various strains of Vibrio. Of lately, most of the virulence exhibited by other microbes is also attributed by similar quorum sensing pathways. Any leap towards blocking of such mechanisms is the need of the hour which is hypothesized to be achieved by interfering with normal QS interactions between ligands and their receptors. Gingerol, a pungent oil easily available from ginger is a structural analog of N-acylhomoserine lactone (AHL), which is an actual signalling ligand of QS-receptor LuxR responsible for initiating a cascade of reactions leading to bioluminescence. In-silico study suggested the antagonistic binding of gingerol to LuxR by hydrogen bonding and hydrophobic interactions which should, in theory, reduce bioluminescence. This was corroborated experimentally by rigorous image analysis of luminescence using hue, saturation and luminescence (HSL) values. Hence, we conclude gingerol as a potent QS-inhibitor for LuxR that may also inhibit the other members of AHL-receptor family.

摘要

生物发光现象是群体感应(QS)的最广泛研究模型,它发生在各种弧菌菌株中。最近,其他微生物表现出的大多数毒性也归因于类似的群体感应途径。任何阻止这种机制的进展都是当前的需要,人们假设通过干扰配体和它们的受体之间的正常 QS 相互作用来实现这一目标。姜辣素是一种辛辣的油,很容易从生姜中获得,它是 N-酰基高丝氨酸内酯(AHL)的结构类似物,AHL 是负责引发一系列反应导致生物发光的 QS 受体 LuxR 的实际信号配体。计算机模拟研究表明,姜辣素通过氢键和疏水相互作用与 LuxR 拮抗结合,这应该会在理论上减少生物发光。这通过使用色调、饱和度和亮度(HSL)值对发光进行严格的图像分析得到了实验证实。因此,我们得出结论,姜辣素是 LuxR 的一种有效的 QS 抑制剂,也可能抑制 AHL 受体家族的其他成员。

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