TY - JOUR
T1 - Anti-diarrheal activity of (-)-Epicatechin from Chiranthodendron pentadactylon Larreat
T2 - Experimental and computational studies
AU - Velázquez, Claudia
AU - Correa-Basurto, José
AU - Garcia-Hernandez, Normand
AU - Barbosa, Elizabeth
AU - Tesoro-Cruz, Emiliano
AU - Calzada, Samuel
AU - Calzada, Fernando
PY - 2012/9/28
Y1 - 2012/9/28
N2 - Ethnopharmacological relevance: Chiranthodendron pentadactylon Larreat is frequently used in Mexican traditional medicine as well as in Guatemalan for several medicinal purposes, including their use in the control of diarrhea. Aim of the study: This work was undertaken to obtain additional information that support the traditional use of Chiranthodendron pentadactylon Larreat, on pharmacological basis using the major antisecretory isolated compound from computational, in vitro and in vivo experiments. Materials and methods: (-)-Epicatechin was isolated from ethyl acetate fraction of the plant crude extract. In vivo toxin (Vibrio cholera or Escherichia coli)-induced intestinal secretion in rat jejunal loops models and sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis on Vibrio cholera toxin were used in experimental studies while the molecular docking technique was used to conduct computational study. Results: The antisecretory activity of epicatechin was tested against Vibrio cholera and Escherichia coli toxins at oral dose 10 mg/kg in the rat model. It exhibited the most potent activity on Vibrio cholera toxin (56.9% of inhibition). In the case of Escherichia coli toxin its effect was moderate (24.1% of inhibition). SDS-PAGE analysis revealed that both (-)-epicatechin and Chiranthodendron pentadactylon extract interacted with the Vibrio cholera toxin at concentration from 80 μg/mL and 300 μg/mL, respectively. Computational molecular docking showed that epicatechin interacted with four amino acid residues (Asn 103, Phe 31, Phe 223 and The 78) in the catalytic site of Vibrio cholera toxin, revealing its potential binding mode at molecular level. Conclusion: The results derived from computational, in vitro and in vivo experiments on Vibrio cholera and Escherichia coli toxins confirm the potential of epicatechin as a new antisecretory compound and give additional scientific support to anecdotal use of Chiranthodendron pentadactylon Larreat in Mexican traditional medicine to treat gastrointestinal disorders such as diarrhea.
AB - Ethnopharmacological relevance: Chiranthodendron pentadactylon Larreat is frequently used in Mexican traditional medicine as well as in Guatemalan for several medicinal purposes, including their use in the control of diarrhea. Aim of the study: This work was undertaken to obtain additional information that support the traditional use of Chiranthodendron pentadactylon Larreat, on pharmacological basis using the major antisecretory isolated compound from computational, in vitro and in vivo experiments. Materials and methods: (-)-Epicatechin was isolated from ethyl acetate fraction of the plant crude extract. In vivo toxin (Vibrio cholera or Escherichia coli)-induced intestinal secretion in rat jejunal loops models and sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis on Vibrio cholera toxin were used in experimental studies while the molecular docking technique was used to conduct computational study. Results: The antisecretory activity of epicatechin was tested against Vibrio cholera and Escherichia coli toxins at oral dose 10 mg/kg in the rat model. It exhibited the most potent activity on Vibrio cholera toxin (56.9% of inhibition). In the case of Escherichia coli toxin its effect was moderate (24.1% of inhibition). SDS-PAGE analysis revealed that both (-)-epicatechin and Chiranthodendron pentadactylon extract interacted with the Vibrio cholera toxin at concentration from 80 μg/mL and 300 μg/mL, respectively. Computational molecular docking showed that epicatechin interacted with four amino acid residues (Asn 103, Phe 31, Phe 223 and The 78) in the catalytic site of Vibrio cholera toxin, revealing its potential binding mode at molecular level. Conclusion: The results derived from computational, in vitro and in vivo experiments on Vibrio cholera and Escherichia coli toxins confirm the potential of epicatechin as a new antisecretory compound and give additional scientific support to anecdotal use of Chiranthodendron pentadactylon Larreat in Mexican traditional medicine to treat gastrointestinal disorders such as diarrhea.
KW - (-)-Epicatechin
KW - Antisecretory
KW - Chiranthodendron pentadactylon Larreat
KW - Diarrhea
KW - Escherichia coli toxin
KW - Flavan-3-ol
KW - Molecular docking
KW - SDS-PAGE analysis
KW - Sterculiaceae
KW - Vibrio cholerae toxin
UR - http://www.scopus.com/inward/record.url?scp=84866027930&partnerID=8YFLogxK
U2 - 10.1016/j.jep.2012.07.039
DO - 10.1016/j.jep.2012.07.039
M3 - Artículo
C2 - 22884870
SN - 0378-8741
VL - 143
SP - 716
EP - 719
JO - Journal of Ethnopharmacology
JF - Journal of Ethnopharmacology
IS - 2
ER -