Quorum Sensing and Biofilm Disrupting Potential of Imidazole Derivatives in Chromobacterium violaceum Using Antimicrobial and Drug Discovery Approaches

4区 · 生物学

ArticleOA

作者: Aqlan, Faisal Mohammed ; Al-Bogami, Abdullah Saad ; Wani, Mohmmad Younus ; Ahmad, Aijaz ; Arendse, Madison ; Khan, Shama

Population of drug-resistant bacteria have increased at an alarming rate in the past few decades. The major reason for increasing drug resistance is the lack of new antibiotics and limited drug targets. It has therefore been a vital task to develop new antibiotics with different drug targets. Two such targets are biofilm formation and quorum sensing. Quorum sensing is cell to cell communication used by bacteria that initiates many important survival processes and aids in establishing pathogenesis. Both biofilm and quorum sensing are inter-related processes and play a major role in physiological and pathogenesis processes. In this study, five novel imidazole derivatives (IMA-1-IMA-5) were synthesised and tested for their antibacterial and anti-quorum sensing activities against Chromobacterium violaceum using different in silico and in vitro techniques following the standard protocols. In silico results revealed that all compounds were able to effectively bind to and interact sufficiently with the target protein CviR. CviR is a protein to which autoinducers bind to initiate the quorum sensing process. In silico results also revealed that the compounds generated favourable structural dynamics implying that the compounds would be able to effectively bind to CviR and inhibit quorum sensing. Susceptibility results revealed that IMA-1 is the most active of all the derivatives against both planktonic cells and biofilms. Qualitative and quantitative evaluation of anti-quorum sensing activity at sub-inhibitory concentrations of these compounds also revealed high activity for IMA-1. Down-regulation of most of the quorum sensing genes when cells were treated with the test compounds affirmed the high anti-quorum sensing activities of these compounds. The results from this study are promising and urges on the use of anti-quorum sensing and biofilm disrupting molecules to combat multi-drug resistance problem.

2021-12-15·Science Translational Medicine1区 · 医学

A small molecule targeting ALOX12-ACC1 ameliorates nonalcoholic steatohepatitis in mice and macaques

1区 · 医学

Article

作者: Touyz, Rhian M. ; Cheng, Xu ; Huang, Yong-Ping ; Zhao, Ling-Ping ; Tian, Song ; Li, Hongliang ; Ma, Jun-Peng ; Zhang, Peng ; Yang, Juan ; Xiao, Li ; Cheng, Yanjie ; Xiang, Hui ; Ma, Xinliang ; Wan, Juan ; Zhao, Guang-Nian ; Liao, Rufang ; Wang, Yibin ; Liu, Peter P. ; Cai, Jingjing ; Shen, Li-Jun ; Zhang, Xiao-Jing ; Ji, Yan-Xiao ; She, Zhi-Gang ; Yao, Xinxin ; Wang, Junyong ; Wang, Xi ; Li, Peng-Long ; Yang, Hailong ; Sun, Dating ; Tian, Rui-Feng ; Xu, Qingbo ; Xu, Haibo ; Hu, Man-Li ; Zhang, Xin ; Loomba, Rohit

IMA-1 targets the ALOX12-ACC1 interaction to both prevent and treat NASH without inducing hyperlipidemia.

2020-10-01·Plant Physiology and Biochemistry2区 · 生物学

The arbuscular mycorrhizal fungus Funneliformis mosseae induces changes and increases the concentration of volatile organic compounds in Vitis vinifera cv. Sangiovese leaf tissue

2区 · 生物学

Article

作者: Seeger, Michael ; Fiaschi, Grazia ; D'Onofrio, Claudio ; Carvajal, Marcela ; Velásquez, Alexis ; Giovannetti, Manuela ; Avio, Luciano ; Valenzuela, Miryam

Arbuscular mycorrhizal fungi (AMF) are beneficial obligate symbionts of plant roots. Volatile organic compounds (VOCs) participate in plant communication and defence. The aim of this study was to analyse the effects of the arbuscular mycorrhizal fungus Funneliformis mosseae IMA1 on VOCs in Vitis vinifera cv. Sangiovese leaf tissue. Grapevine plants inoculated with F. mosseae IMA1 were incubated for 23 weeks. VOCs were extracted from leaves and identified using headspace solid-phase microextraction (HS-SPME) coupled to GC-MS. VOCs in leaf tissue were strongly enhanced (85%) by F. mosseae IMA1. The mycorrhizal fungus IMA1 modified the levels of specific VOCs synthesised in different anabolic pathways. An increase in volatiles that have been related to plant defences under pathogen/herbivore attack or linked to water stress, such as (E)-2-hexenal, 3-hexenal, geraniol, benzaldehyde and methyl salicylate, was observed in mycorrhizal plants. In contrast, some C₁₃-norisoprenoids decreased strongly in mycorrhizal plants. The study of the effects of AMF on VOCs in grapevine plants may provide useful information to establish sustainable viticultural practices.

100 项与 IMA-1 相关的药物交易

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