Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition
Incomptines A (<b>IA</b>) and B (<b>IB</b>) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of <b>IA</b> and <b>IB</b> against bacteria causing d...
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MDPI AG
2022-02-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/2/196 |
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| author | Fernando Calzada Elihu Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Claudia Velázquez Elizabeth Barbosa Miguel Valdes Jesús Iván Solares-Pascasio |
| author_facet | Fernando Calzada Elihu Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Claudia Velázquez Elizabeth Barbosa Miguel Valdes Jesús Iván Solares-Pascasio |
| author_sort | Fernando Calzada |
| collection | DOAJ |
| description | Incomptines A (<b>IA</b>) and B (<b>IB</b>) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of <b>IA</b> and <b>IB</b> against bacteria causing diarrhoea have been reported; however, no information is available regarding their antibacterial activity on <i>Vibrio cholerae</i>. In this work, both compounds were evaluated for their anti-diarrhoeal potential using the bacterium <i>V. cholerae</i>, 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 <b>IA</b> and <b>IB</b> with cholera toxin. In terms of antibacterial activity, <b>IB</b> was three times more active than <b>IA</b> on <i>V. cholerae</i>. In the case of SDS-PAGE analysis and the in silico study, <b>IA</b> was most effective, revealing its potential binding mode at a molecular level. In terms of anti-diarrhoeal activity, <b>IA</b> was 10 times more active than <b>IB</b> and racecadotril, an antisecretory drug used as positive control; the anti-diarrheal activity of <b>IB</b> was also closer than racecadotril. The results obtained from in vitro, in vivo, and computational studies on <i>V. cholerae</i> and cholera toxin support the potential of <b>IA</b> and <b>IB</b> as new anti-diarrhoeal compounds. |
| first_indexed | 2024-03-09T21:15:40Z |
| format | Article |
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| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T21:15:40Z |
| publishDate | 2022-02-01 |
| publisher | MDPI AG |
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| series | Pharmaceuticals |
| spelling | doaj.art-25f1f65134eb454fb6f009d4905ab2a22023-11-23T21:34:33ZengMDPI AGPharmaceuticals1424-82472022-02-0115219610.3390/ph15020196Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin InhibitionFernando Calzada0Elihu Bautista1Sergio Hidalgo-Figueroa2Normand García-Hernández3Claudia Velázquez4Elizabeth Barbosa5Miguel Valdes6Jesús Iván Solares-Pascasio7Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORSE, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Cd Mexico 06725, MexicoCONACYT-División de Biología Molecular, Instituto Potosino de Investigación Científica y Tecnológica A.C., San Luis Potosí 78216, MexicoCONACYT-División de Biología Molecular, Instituto Potosino de Investigación Científica y Tecnológica A.C., San Luis Potosí 78216, MexicoUnidad de Investigación Médica en Genética Humana, UMAE Hospital Pediatría 2º Piso, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Cd Mexico 06725, MexicoÁrea Académica de Farmacia, Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Km 4.5, Carretera Pachuca-Tulancingo, Unidad Universitaria, Pachuca 42076, MexicoSección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Salvador Díaz Mirón Esq. Plan de San Luis S/N, Miguel Hidalgo, Casco de Santo Tomas, Cd Mexico 11340, MexicoUnidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORSE, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Cd Mexico 06725, MexicoUnidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORSE, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Cd Mexico 06725, MexicoIncomptines A (<b>IA</b>) and B (<b>IB</b>) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of <b>IA</b> and <b>IB</b> against bacteria causing diarrhoea have been reported; however, no information is available regarding their antibacterial activity on <i>Vibrio cholerae</i>. In this work, both compounds were evaluated for their anti-diarrhoeal potential using the bacterium <i>V. cholerae</i>, 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 <b>IA</b> and <b>IB</b> with cholera toxin. In terms of antibacterial activity, <b>IB</b> was three times more active than <b>IA</b> on <i>V. cholerae</i>. In the case of SDS-PAGE analysis and the in silico study, <b>IA</b> was most effective, revealing its potential binding mode at a molecular level. In terms of anti-diarrhoeal activity, <b>IA</b> was 10 times more active than <b>IB</b> and racecadotril, an antisecretory drug used as positive control; the anti-diarrheal activity of <b>IB</b> was also closer than racecadotril. The results obtained from in vitro, in vivo, and computational studies on <i>V. cholerae</i> and cholera toxin support the potential of <b>IA</b> and <b>IB</b> as new anti-diarrhoeal compounds.https://www.mdpi.com/1424-8247/15/2/196incomptine Aincomptine Bsesquiterpene lactones<i>Decachaeta incompta</i><i>Vibrio cholerae</i>cholera toxin |
| spellingShingle | Fernando Calzada Elihu Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Claudia Velázquez Elizabeth Barbosa Miguel Valdes Jesús Iván Solares-Pascasio Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition Pharmaceuticals incomptine A incomptine B sesquiterpene lactones <i>Decachaeta incompta</i> <i>Vibrio cholerae</i> cholera toxin |
| title | Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition |
| title_full | Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition |
| title_fullStr | Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition |
| title_full_unstemmed | Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition |
| title_short | Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against <i>Vibrio cholerae</i> and Its Enterotoxin Inhibition |
| title_sort | understanding the anti diarrhoeal properties of incomptines a and b antibacterial activity against i vibrio cholerae i and its enterotoxin inhibition |
| topic | incomptine A incomptine B sesquiterpene lactones <i>Decachaeta incompta</i> <i>Vibrio cholerae</i> cholera toxin |
| url | https://www.mdpi.com/1424-8247/15/2/196 |
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