Table 3.
Anti-QS and anti-virulence properties of RhlR-modulating QSIs.
QSIs | Anti-QS Properties | Anti-Virulence Properties | Ref. | |||
---|---|---|---|---|---|---|
Target | % Inhibition/Activation (IC50/EC50) | Anti-Biofilm Activity | Anti-Rhamnolipid Activity | Anti-Pyocyanin Activity | ||
% Inhibition | % Inhibition | IC50 | ||||
24 | RhlR (agonist) | 43% at 1 mM (a) | ≈40% at 100 µM (e) | ND | 8 µM (g) | [100] |
80% at 20 µM (b) | ||||||
25 | RhlR (agonist) | 4.5 µM (c) | ND | ND | ND | [101] |
26 | RhlR (agonist) | 7.2 µM (c) | ||||
27 | RhlR (antagonist) | 20% at 10 µM (d) | 15% at 10 µM (f) | ≈40% at 10 µM (h) | NA (h) | [105] |
NA = Not active, ND = Not Determined; Anti-QS evaluations carried out using reporter gene assays on/with (a) E. coli (rhlA-gfp)/competition against odDHL (100 nM); (b) E. coli (rhlA–gfp); (c) P. aeruginosa (PAO-JP2, prhlILVAGFP); (d) P. aeruginosa (PAO1, rhlA-lacZ); Anti-virulence evaluations carried out on/by (e) static biofilm assay with P. aeruginosa (PA14)/confocal laser scanning microscopy; (f) static biofilm assay with P. aeruginosa (PAO1)/CV dyeing and OD measurement; (g) P. aeruginosa (PA14)/OD measurement; (h) P. aeruginosa (PAO1)/OD measurement.