pyocyanin

Hemipyocyanine (528-71-2) is the virulence factor of Gram-negative, aerobic rod bacterium Pseudomonas aeruginosa. Hemipyocyanine is an α-Amylase inhibitor.

Hexyl gallate (Gallic acid hexyl ester), an alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum (IC50: 0.11 mM).

2-heptyl-3-hydroxy-4(1H)-Quinolone (Pseudomonas Quinolone Signal) is a quorum-sensing signalling molecule produced by Pseudomonas aeruginosa in response to increased cell density. It increases the expression of the lasB gene in P. aeruginosa, the secretion of the metabolites pyocyanin and the lectin PA-IL, as well as increasing biofilm production in P. aeruginosa populations. It also reduces the iron content of the P. aeruginosa growth medium when used at a concentration of 40 μM and acts as an iron chelator in iron sulphate solutions.

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively, and it reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM[1].

Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.

RhlR antagonist 1 is a highly effective antagonist of the RhlR protein, showing an IC50 value of 26 μM. It exhibits selective antagonistic activity against RhlR, with minimal effect on LasR and PqsR. RhlR antagonist 1 strongly inhibits biofilm formation in both static and dynamic environments and reduces the production of virulence factors, such as rhamnolipid and pyocyanin, in P. aeruginosa. These characteristics make RhlR antagonist 1 a valuable tool for the development of molecules that modulate quorum sensing and control P. aeruginosa infections [1].

LasR-IN-4 is a potent inhibitor of LasR, effectively inhibiting Pseudomonas aeruginosa, its biofilm formation, pyocyanin production, and rhamnolipids production [1].

Antibacterial synergist 1 (compound 20P) is a potent inhibitor of bacterial biofilm formation, effectively suppressing pyocyanin production with an IC50 of 8.6 μM and inhibiting biofilm formation with an IC50 of 4.5 μM. Antibacterial synergist 1 shows promise in the research of P. aeruginosa infections [1].

PqsR-IN-1 (Compound 18) is a potent inhibitor of PqsR, a transcriptional regulator in the quorum sensing mechanism of Pseudomonas aeruginosa, that effectively reduces pyocyanin production and exhibits minimal cytotoxicity [1].

PqsR-IN-2 (Compound 19) is a highly potent inhibitor of PqsR, the transcriptional regulator of quorum sensing in Pseudomonas aeruginosa. It efficiently suppresses pyocyanin production without significant cytotoxicity, making it a promising candidate for therapeutic applications [1].

F-17 is a promising virulence factor inhibitor, displaying substantial inhibitory effects on biofilm formation, elastase activity, pyocyanin production, and swarming motility. Additionally, F-17 exhibits a strong binding affinity towards LasR and PqsR. Notably, F-17 does not exhibit any discernible cytotoxicity [1].

N-Decanoyl cyclopentylamide (C10-CPA) serves as a potent quorum sensing inhibitor in Pseudomonas aeruginosa, disrupting the expression of virulence factors governed by both the las and rhl systems. It effectively suppresses the production of elastase, pyocyanin, rhamnolipid, and hinders biofilm formation.

Quorum sensing-IN-6 (compound 27) is a quorum sensing (QS) inhibitor with IC50 values of 8 nM and 106 nM against E.coli and Pyocyanin, respectively.

Aeruginoic acid is a byproduct of pyocyanin biosynthesis and functions as an iron chelator. Additionally, aeruginoic acid exhibits antihypertensive activity.