The 9H-Fluoren Vinyl Ether Derivative SAM461 Inhibits Bacterial Luciferase Activity and Protects Artemia franciscana From Luminescent Vibriosis.

摘要: Vibrio campbellii is a major pathogen in aquaculture. It causative agent of the so-called "luminescent vibriosis," life-threatening condition caused by bioluminescent spp. that often involves mass mortality farmed shrimps. The emergence multidrug resistant strains raises concern and poses challenge for treatment this infection coming years. Inhibition bacterial cell-to-cell communication or quorum sensing (QS) has been proposed as an alternative to antibiotic therapies. Aiming identify novel QS disruptors, 9H-fluroen-9yl vinyl ether derivative SAM461 was found thwart V. bioluminescence, QS-regulated phenotype. Phenotypic gene expression analyses revealed, however, mode action unrelated inhibition. Further evaluation with purified fischeri NanoLuc luciferases revealed enzymatic inhibition at micromolar concentrations. In silico analysis molecular docking suggested binding active site cavities both luciferase enzymes. Subsequent vivo testing gnotobiotic Artemia franciscana nauplii demonstrated naupliar protection against low Taken together, these findings suggest suppression activity could constitute paradigm development anti-infective chemotherapies luminescent vibriosis, pave ground chemical synthesis biological characterization derivatives promising antimicrobial prospects.