关键词: bacterial resistance to antibiotics bioactive compounds clinical trial quorum sensing

Mesh : Quorum Sensing / drug effects Plants, Medicinal / chemistry Anti-Bacterial Agents / pharmacology chemistry Humans Bacteria / drug effects metabolism Clinical Trials as Topic Phytochemicals / pharmacology chemistry Flavonoids / pharmacology chemistry Plant Extracts / pharmacology chemistry

来  源:   DOI:10.3390/molecules27051484   PDF(Pubmed)

Abstract:
Bacterial strains have developed an ability to resist antibiotics via numerous mechanisms. Recently, researchers conducted several studies to identify natural bioactive compounds, particularly secondary metabolites of medicinal plants, such as terpenoids, flavonoids, and phenolic acids, as antibacterial agents. These molecules exert several mechanisms of action at different structural, cellular, and molecular levels, which could make them candidates or lead compounds for developing natural antibiotics. Research findings revealed that these bioactive compounds can inhibit the synthesis of DNA and proteins, block oxidative respiration, increase membrane permeability, and decrease membrane integrity. Furthermore, recent investigations showed that some bacterial strains resist these different mechanisms of antibacterial agents. Researchers demonstrated that this resistance to antibiotics is linked to a microbial cell-to-cell communication system called quorum sensing (QS). Consequently, inhibition of QS or quorum quenching is a promising strategy to not only overcome the resistance problems but also to treat infections. In this respect, various bioactive molecules, including terpenoids, flavonoids, and phenolic acids, exhibit numerous anti-QS mechanisms via the inhibition of auto-inducer releases, sequestration of QS-mediated molecules, and deregulation of QS gene expression. However, clinical applications of these molecules have not been fully covered, which limits their use against infectious diseases. Accordingly, the aim of the present work was to discuss the role of the QS system in bacteria and its involvement in virulence and resistance to antibiotics. In addition, the present review summarizes the most recent and relevant literature pertaining to the anti-quorum sensing of secondary metabolites and its relationship to antibacterial activity.
摘要:
细菌菌株已经发展出通过多种机制抵抗抗生素的能力。最近,研究人员进行了几项研究,以确定天然生物活性化合物,特别是药用植物的次生代谢产物,比如萜类化合物,黄酮类化合物,和酚酸,作为抗菌剂。这些分子在不同的结构上发挥几种作用机制,细胞,和分子水平,这可能使它们成为开发天然抗生素的候选化合物或先导化合物。研究发现,这些生物活性化合物可以抑制DNA和蛋白质的合成,阻断氧化呼吸,增加膜的渗透性,并降低膜的完整性。此外,最近的调查表明,一些细菌菌株抵抗这些不同机制的抗菌剂。研究人员证明,这种对抗生素的耐药性与称为群体感应(QS)的微生物细胞间通讯系统有关。因此,抑制QS或群体猝灭是不仅克服耐药性问题而且治疗感染的有前途的策略。在这方面,各种生物活性分子,包括萜类化合物,黄酮类化合物,和酚酸,通过抑制自动诱导物释放表现出许多抗QS机制,QS介导的分子的螯合,以及QS基因表达的失调。然而,这些分子的临床应用尚未完全涵盖,这限制了它们对传染病的使用。因此,本工作的目的是讨论QS系统在细菌中的作用及其在毒力和抗生素耐药性中的作用。此外,本综述总结了有关次级代谢产物的抗群体感应及其与抗菌活性的关系的最新和相关文献。
公众号