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Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against Vibrio cholerae and Its Enterotoxin Inhibition

dc.contributor.authorCalzada, Fernando
dc.contributor.authorBautista Redonda, Francisco Elihú
dc.contributor.authorHidalgo Figueroa, Sergio Nemorio
dc.contributor.authorGarcía Hernández, Normand
dc.contributor.authorVelázquez, Claudia
dc.contributor.authorBarbosa Cabrera, Reyna Elizabeth
dc.contributor.authorValdes Guevara, Miguel Andrés
dc.contributor.authorSolares Pascasio, Jesús Iván
dc.date.accessioned2023-06-14T16:12:29Z
dc.date.available2023-06-14T16:12:29Z
dc.date.issued2022
dc.identifier.citationCalzada, F.; Bautista, E.; Hidalgo-Figueroa, S.; García-Hernández, N.; Velázquez, C.; Barbosa, E.; Valdes, M.; Solares-Pascasio, J.I. Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against Vibrio cholerae and Its Enterotoxin Inhibition. Pharmaceuticals 2022, 15, 196. https://doi.org/10.3390/ph15020196
dc.identifier.urihttp://hdl.handle.net/11627/6352
dc.description.abstract"Incomptines A (IA) and B (IB) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of IA and IB against bacteria causing diarrhoea have been reported; however, no information is available regarding their antibacterial activity on Vibrio cholerae. In this work, both compounds were evaluated for their anti-diarrhoeal potential using the bacterium V. cholerae, sodium dodecyl sulphate–polyacrylamide gel electrophoresis (SDS-PAGE) analysis on cholera toxin, and a cholera toxin-induced diarrhoea model in male Balb/c mice. In addition, a molecular docking study was carried out to understand the interaction of IA and IB with cholera toxin. In terms of antibacterial activity, IB was three times more active than IA on V. cholerae. In the case of SDS-PAGE analysis and the in silico study, IA was most effective, revealing its potential binding mode at a molecular level. In terms of anti-diarrhoeal activity, IA was 10 times more active than IB and racecadotril, an antisecretory drug used as positive control; the anti-diarrheal activity of IB was also closer than racecadotril. The results obtained from in vitro, in vivo, and computational studies on V. cholerae and cholera toxin support the potential of IA and IB as new anti-diarrhoeal compounds."
dc.publisherMDPI
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internacional
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectIncomptine A
dc.subjectIncomptine B
dc.subjectSesquiterpene lactones
dc.subjectDecachaeta incompta
dc.subjectVibrio cholerae
dc.subjectCholera toxin
dc.subjectCholera toxin-induced diarrhoea
dc.subjectSDS-PAGE analysis
dc.subjectDocking analysis
dc.subject.classificationFARMACOLOGÍA
dc.titleUnderstanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against Vibrio cholerae and Its Enterotoxin Inhibition
dc.typearticle
dc.identifier.doihttps://doi.org/10.3390/ph15020196
dc.rights.accessAcceso Abierto


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Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 Internacional