{"refrec":{"BRefID":307886,"RR":"<b>Martin-Rodriguez, A.J.; Alvarez-Mendez, S.J.; Overa, C.; Baruah, K.; Lourenço, T.M.; Norouzitallab, P.; Bossier, P.; Martin, V.S.; Fernández, J.J.</b> (2018). The 9<i>H</i>-fluoren vinyl ether derivative SAM461 inhibits bacterial luciferase activity and protects <i>Artemia franciscana</i> from luminescent vibriosis. <i>Frontiers in Cellular and Infection Microbiology 8</i>: 11. <a href=\"https://dx.doi.org/10.3389/fcimb.2018.00368\" target=\"_blank\">https://dx.doi.org/10.3389/fcimb.2018.00368</a>","BEntID":300212,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":0,"RefStringPartII":". <i>Frontiers in Cellular and Infection Microbiology 8</i>: 11. <a href=\"https://dx.doi.org/10.3389/fcimb.2018.00368\" target=\"_blank\">https://dx.doi.org/10.3389/fcimb.2018.00368</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":0,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Martin-Rodriguez, A.J.; Alvarez-Mendez, S.J.; Overa, C.; Baruah, K.; Lourenço, T.M.; Norouzitallab, P.; Bossier, P.; Martin, V.S.; Fernández, J.J.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Martin-Rodriguez, A.J. <i>et al.</i>","Englishabstract":"<i>Vibrio campbellii</i> is a major pathogen in aquaculture. It is a causative agent of the so-called “luminescent vibriosis,” a life-threatening condition caused by bioluminescent <i>Vibrio</i> spp. that often involves mass mortality of farmed shrimps. The emergence of multidrug resistant <i>Vibrio</i> strains raises a concern and poses a challenge for the treatment of this infection in the coming years. Inhibition of bacterial cell-to-cell communication or quorum sensing (QS) has been proposed as an alternative to antibiotic therapies. Aiming to identify novel QS disruptors, the 9H-fluroen-9yl vinyl ether derivative SAM461 was found to thwart <i>V. campbellii</i> bioluminescence, a QS-regulated phenotype. Phenotypic and gene expression analyses revealed, however, that the mode of action of SAM461 was unrelated to QS inhibition. Further evaluation with purified <i>Vibrio fischeri</i> and NanoLuc luciferases revealed enzymatic inhibition at micromolar concentrations. <i>In silico</i> analysis by molecular docking suggested binding of SAM461 in the active site cavities of both luciferase enzymes. Subsequent <i>in vivo</i> testing of SAM461 with gnotobiotic <i>Artemia franciscana</i> nauplii demonstrated naupliar protection against <i>V. campbellii</i> infection at low micromolar concentrations. Taken together, these findings suggest that suppression of luciferase activity could constitute a novel paradigm in the development of alternative anti-infective chemotherapies against luminescent vibriosis, and pave the ground for the chemical synthesis and biological characterization of derivatives with promising antimicrobial prospects.","AbstractOtherLang":null,"BibLvlCode":"AS","StandardTitle":"The 9<i>H</i>-fluoren vinyl ether derivative SAM461 inhibits bacterial luciferase activity and protects <i>Artemia franciscana</i> from luminescent vibriosis","OrigTitleLangCode":"en","OrigTitleLangCodeExtended":"eng","OrigTitleLangID":15,"DateLastModified":{"date":"2024-12-10 01:33:17.368041","timezone_type":1,"timezone":"+01:00"},"UserAccessRight":null,"UserAccID":null,"AuthorKeywords":"vinyl ether; luciferase; Artemia; vibriosis; alternative anti-infectives","OtherDescriptors":null,"Notes":null,"AnaPub":2018,"MonPub":null,"DateUpdate":"2020-09-07","DateCreate":"2019-03-13","SecASFANote":null,"ConfID":null,"PeerRev":1,"VlizCoreFlag":1,"WoScode":"WOS:000449611900001","VABBcode":null,"OpenAcc":1,"DOI":"10.3389/fcimb.2018.00368"},"refs":null,"anarec":{"AnaID":307886,"PubliDate":2018,"Pagination":"11","XtraPublOfAnaID":null,"ISBN":null,"Volume":"8","Issue":null,"BRefMon":null,"BRefMonRR":null,"BRefXtra":null,"BRefXtraRR":null,"SerBRefID":268431,"SerRR":"Frontiers in Cellular and Infection Microbiology. 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