Editorial: Pathoblockers and antivirulence agents of plant-origin for the management of multidrug resistant pathogens

Bonvicini, Francesca; Mandrone, Manuela; Cosa, Sekelwa

doi:10.3389/fmicb.2023.1201495

Cited by 1 publication

(1 citation statement)

References 7 publications

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“…Such 'pathoblockers' are expected to compromise the ability of the pathogen to damage the host, by exerting their effect on nonessential targets such as bacterial quorum sensing (QS) (7), stress-response machinery (8), metal homeostasis (9,10), etc. The next-generation antibacterials preferably should be attacking such hitherto unexplored/underexplored targets in pathogenic bacteria (11)(12)(13).…”

Section: Introductionmentioning

confidence: 99%

Identification of anti-pathogenic activity among in silico predicted small-molecule inhibitors of Pseudomonas aeruginosa LasR or nitric oxide reductase (NOR)

Gajera,

Henriksen,

Cox

et al. 2023

dti

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Introduction: Antibiotic-resistant Pseudomonas aeruginosa strains cause considerable morbidity and mortality globally. Identification of novel targets in this notorious pathogen is urgently warranted to facilitate discovery of new anti-pathogenic agents against it. This study attempted to identify small-molecule inhibitors of two important proteins LasR and nitric oxide reductase (NOR) in P. aeruginosa. ‘Las’ system can be said to be the ‘master’ regulator of quorum sensing in P. aeruginosa, whose receptor protein is LasR. Similarly, NOR is crucial to detoxification of reactive nitrogen species. Methods: In silico identification of potential LasR or NOR inhibitors was attempted through a virtual screening platform AtomNet® to obtain a final subset of <100 top scoring compounds. These compounds were evaluated for their in vivo anti-pathogenic activity by challenging the model host Caenorhabditis elegans with P. aeruginosa in the presence or absence of test compounds. Survival of the worm population in 24-well assay plates was monitored over a period of 5 days microscopically. Results: Of the 96 predicted LasR inhibitors, 11 exhibited anti-Pseudomonas activity (23%-96% inhibition of bacterial virulence as per third-day end-point) at 25-50 µg/mL. Of the 85 predicted NOR inhibitors, 8 exhibited anti-Pseudomonas activity (40%-85% inhibition of bacterial virulence as per second-day end-point) at 25-50 µg/mL. Conclusion: Further investigation on molecular mode of action of compounds found active in this study is warranted. Virtual screening can be said to be a useful tool in narrowing down the list of compounds requiring actual wet-lab screening, saving considerable time and efforts for drug discovery.

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Section: Introductionmentioning

confidence: 99%

Identification of anti-pathogenic activity among in silico predicted small-molecule inhibitors of Pseudomonas aeruginosa LasR or nitric oxide reductase (NOR)

Gajera,

Henriksen,

Cox

et al. 2023

dti

View full text Add to dashboard Cite

show abstract

Editorial: Pathoblockers and antivirulence agents of plant-origin for the management of multidrug resistant pathogens

Abstract: April CITATIONBonvicini F, Mandrone M and Cosa S ( ) Editorial: Pathoblockers and antivirulence agents of plant-origin for the management of multidrug resistant pathogens.

Cited by 1 publication

References 7 publications

Identification of anti-pathogenic activity among in silico predicted small-molecule inhibitors of Pseudomonas aeruginosa LasR or nitric oxide reductase (NOR)

Identification of anti-pathogenic activity among in silico predicted small-molecule inhibitors of Pseudomonas aeruginosa LasR or nitric oxide reductase (NOR)

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