Equisetin as potential quorum sensing inhibitor of Pseudomonas aeruginosa

Zhang, Mengmeng; Wang, Mengjia; Zhu, X. D.; Yu, Wengong; Gong, Qianhong

doi:10.1007/s10529-018-2527-2

Cited by 30 publications

(21 citation statements)

References 15 publications

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“…The tetramic acid scaffold is an important structure which has been found in terrestrial and marine organisms [25]. In addition to cladodionen, similar structures have been found in QSIs, such as tenuazonic acid [26] and equisetin [27]. Tenuazonic acid inhibits QS of C. violaceum CV017 without interfering with bacterial vitality [26].…”

Section: Discussionmentioning

confidence: 97%

“…Tenuazonic acid inhibits QS of C. violaceum CV017 without interfering with bacterial vitality [26]. Equisetin inhibits three QS systems of P. aeruginosa; it has the strongest inhibitory effect on the PQS system [27]. The anti-QS activity of the other compounds with similar skeletons to cladodionen, and other cladosporiumins, should be explored.…”

Section: Discussionmentioning

confidence: 99%

“…The effect of cladodionen on the mRNA expression of QS-related genes in P. aeruginosa PAO1 was detected as described previously [27]. RNA was isolated with a bacteria RNA isolation kit (Nobelab Biotechnologies, Beijing, China).…”

Section: Real-time Rt-pcrmentioning

confidence: 99%

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Cladodionen Is a Potential Quorum Sensing Inhibitor Against Pseudomonas aeruginosa

Wang

Zhao

et al. 2020

Marine Drugs

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Pseudomonas aeruginosa is an opportunistic pathogen using virulence factors and biofilm regulated by quorum sensing (QS) systems to infect patients and protect itself from environmental stress and antibiotics. Interfering with QS systems is a novel approach to combat P. aeruginosa infections without killing the bacteria, meaning that it is much harder for bacteria to develop drug resistance. A marine fungus Cladosporium sp. Z148 with anti-QS activity was obtained from Jiaozhou Bay, China. Cladodionen, a novel QS inhibitor, was isolated from the extracts of this fungus. Cladodionen had a better inhibitory effect than pyocyanin on the production of elastase and rhamnolipid. It also inhibited biofilm formation and motilities. The mRNA expressions of QS-related genes, including receptor proteins (lasR, rhlR and pqsR), autoinducer synthases (lasI, rhlI and pqsA) and virulence factors (lasB and rhlA) were down-regulated by cladodionen. Molecular docking analysis showed that cladodionen had better binding affinity to LasR and PqsR than natural ligands. Moreover, the binding affinity of cladodionen to LasR was higher than to PqsR. Cladodionen exhibits potential as a QS inhibitor against P. aeruginosa, and its structure–activity relationships should be further studied to illustrate the mode of action, optimize its structure and improve anti-QS activity.

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Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 99%

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Cladodionen Is a Potential Quorum Sensing Inhibitor Against Pseudomonas aeruginosa

Wang

Zhao

et al. 2020

Marine Drugs

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“…Biological Evaluation A QSI screening model (las system model: QSIS-lasI 36) ) was used to evaluate the inhibitory activity of newly synthesized compounds against P. aeruginosa. This screening model is based on the sucrose lethal gene sacB being activated after self-expressed or externally added signal molecules bind to the LasR protein expressed by the P. aeruginosa las system.…”

Section: Resultsmentioning

confidence: 99%

“…28) L Bacterial Strains and Media Bacterial strains are provided by Ocean University of China. 36) Unless otherwise stated, strains were grown in LB medium.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel L-Homoserine Lactone Analogs as Quorum Sensing Inhibitors of <i>Pseudomonas aeruginosa</i>

Liu

Gong

Luo

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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In this study, we synthesized four series of novel L-homoserine lactone analogs and evaluated their in vitro quorum sensing (QS) inhibitory activity against two biomonitor strains, Chromobacterium violaceum CV026 and Pseudomonas aeruginosa PAO1. Studies of the structure-activity relationships of the set of Lhomoserine lactone analogs indicated that phenylurea-containing N-dithiocarbamated homoserine lactones are more potent than (Z)-4-bromo-5-(bromomethylene)-2(5H)-furanone (C30), a positive control for biofilm formation. In particular, compared with C30, QS inhibitor 11f significantly reduced the production of virulence factors (pyocyanin, elastase and rhamnolipid), swarming motility, the formation of biofilm and the mRNA level of QS-related genes regulated by the QS system of PAO1. These results reveal 11f as a potential lead compound for developing novel antibacterial quorum sensing inhibitors.

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Unveiling the potential of marine compounds as quorum sensing inhibitors targeting Pseudomonas aeruginosa's LasI: A computational study using molecular docking and molecular dynamics

Singothu,

Begum,

Maddi

et al. 2023

J of Cellular Biochemistry

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Antimicrobial resistance (AMR) poses a significant threat to global public health, with multidrug‐resistant Pseudomonas aeruginosa being a leading cause of mortality, accounting for 18%–61% of deaths annually. The quorum sensing (QS) systems of P. aeruginosa, particularly the LasI‐LasR system, play a crucial role in promoting biofilm formation and expression of virulent genes, which contribute to the development of AMR. This study focuses on LasI, the mediator of biofilm formation for identifying its inhibitors from a marine compound database comprising of 32 000 compounds using molecular docking and molecular simulation techniques. The virtual screening and docking experiments demonstrated that the top 10 compounds exhibited favorable docking scores of <−7.19 kcal/mol compared to the reported inhibitor 3,5,7‐Trihydroxyflavone with a docking score of −3.098 kcal/mol. Additionally, molecular mechanics/Poisson‐Boltzmann generalized born surface area (MM‐GBSA) analyses were conducted to assess these compounds' suitability for further investigation. Out of 10 compounds, five compounds demonstrated high MM‐GBSA binding energy (<−35.33 kcal/mol) and were taken up for molecular dynamics simulations to evaluate the stability of the protein‐ligand complex over a 100 ns period. Based on root mean square deviation, root mean square fluctuation, radius of gyration, and hydrogen bond interactions analysis, three marine compounds, namely MC‐2 (CMNPD13419) and MC‐3 (CMNPD1068), exhibited consistent stability throughout the simulation. Therefore, these compounds show potential as promising LasI inhibitors and warrant further validation through in vitro and in vivo experiments. By exploring the inhibitory effects of these marine compounds on P. aeruginosa's QS system, this research aims to contribute to the development of novel strategies to combat AMR.

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Equisetin as potential quorum sensing inhibitor of Pseudomonas aeruginosa

Abstract: Equisetin proved its potential as an inhibitor against P. aeruginosa QS system and might also serve as precursor compound in development of novel therapeutics for infectious diseases by optimal design of structures.

Cited by 30 publications

References 15 publications

Cladodionen Is a Potential Quorum Sensing Inhibitor Against Pseudomonas aeruginosa

Cladodionen Is a Potential Quorum Sensing Inhibitor Against Pseudomonas aeruginosa

Synthesis and Biological Evaluation of Novel L-Homoserine Lactone Analogs as Quorum Sensing Inhibitors of <i>Pseudomonas aeruginosa</i>

Unveiling the potential of marine compounds as quorum sensing inhibitors targeting Pseudomonas aeruginosa's LasI: A computational study using molecular docking and molecular dynamics

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