a School of Pharmacy , China Pharmaceutical University , Nanjing , China.
Expert Opin Ther Pat. 2018 Dec;28(12):849-865. doi: 10.1080/13543776.2018.1541174. Epub 2018 Oct 31.
: Quorum sensing (QS) is a cell density-dependent phenomenon in which specific pathways are activated after autoinducers (AIs) outside the microorganism reach a threshold concentration. QS creates a positive feedback loop that induces a cascade of gene expression and causes biofilm formation, virulence and sporulation. QS signals are diverse, acyl-homoserine lactone (AHL), AI peptide (AIP) and AI-2 are three major categories of QS signals. QS inhibitors (QSIs) can disrupt or prevent the formation of biofilm and reduce virulence while exerting less selective pressure on the bacteria, suggesting that QSIs are potential alternatives for antibiotics. : This review summarized the pertinent patents on QS inhibition available from 2014 to 2018. The authors analyze these patents and provided an overview of them and their potential applications. : The main strategy for QS inhibition is to use the analogues of various QS signals to block downstream signal transducers. The inactivation of signal molecules or the stimulation of the immune response is also attractive strategies to inhibit QS. However, additional clinical trials are needed to assess their efficacy in mammals. In sum, QS inhibition can reduce the virulence of bacteria without affecting their growth or killing them and the reduced pressure may minimize the increasingly resistance.
群体感应(QS)是一种细胞密度依赖性现象,即在微生物体外的自诱导剂(AIs)达到阈值浓度后,特定途径被激活。QS 会产生正反馈回路,诱导基因表达级联反应,并导致生物膜形成、毒力和孢子形成。QS 信号多种多样,酰基高丝氨酸内酯(AHL)、AI 肽(AIP)和 AI-2 是三种主要的 QS 信号类别。QS 抑制剂(QSIs)可以破坏或阻止生物膜的形成并降低毒力,同时对细菌的选择性压力较小,这表明 QSIs 是抗生素的潜在替代品。
本综述总结了 2014 年至 2018 年有关 QS 抑制的相关专利。作者分析了这些专利,并对它们及其潜在应用进行了概述。
QS 抑制的主要策略是使用各种 QS 信号的类似物来阻断下游信号转导器。信号分子的失活或免疫反应的刺激也是抑制 QS 的诱人策略。然而,需要进行更多的临床试验来评估它们在哺乳动物中的疗效。总之,QS 抑制可以降低细菌的毒力,而不影响其生长或杀死它们,并且减少的压力可能最小化日益增加的耐药性。