Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don

Fernando Calzada, Jose Correa Basurto, Elizabeth Barbosa, Claudia Velázquez, Normand García Hernández, R. M. Ordoñez Razo, David Mendez Luna, Lilian Yepez Mulia

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Background: Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. Objective: The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. Materials and Methods: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. Results: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 μg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from-9.92 kcal/mol and 53.57 μM, respectively) and G/FBPA (free binding energy from-7.17 kcal/mol and 55.5 μM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. Conclusion: The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery.
Original languageAmerican English
Pages (from-to)133-137
Number of pages119
JournalPharmacognosy Research
DOIs
StatePublished - 1 Apr 2017

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Protozoa
Pyruvate Synthase
Binding energy
Dysentery
Acids
Diarrhea
Flavonoids
Giardia lamblia
Entamoeba histolytica
Fructose
Bioassay
Fractionation
Medicine
Assays
Ethanol
Malvaceae
Enzymes
Antennas
Apigenin
Trophozoites

Cite this

Calzada, F., Basurto, J. C., Barbosa, E., Velázquez, C., Hernández, N. G., Ordoñez Razo, R. M., ... Mulia, L. Y. (2017). Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don. Pharmacognosy Research, 133-137. https://doi.org/10.4103/0974-8490.204644
Calzada, Fernando ; Basurto, Jose Correa ; Barbosa, Elizabeth ; Velázquez, Claudia ; Hernández, Normand García ; Ordoñez Razo, R. M. ; Luna, David Mendez ; Mulia, Lilian Yepez. / Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don. In: Pharmacognosy Research. 2017 ; pp. 133-137.
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title = "Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don",
abstract = "Background: Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. Objective: The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. Materials and Methods: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. Results: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50{\%} inhibitory concentration values of 17.5 μg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from-9.92 kcal/mol and 53.57 μM, respectively) and G/FBPA (free binding energy from-7.17 kcal/mol and 55.5 μM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. Conclusion: The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery.",
author = "Fernando Calzada and Basurto, {Jose Correa} and Elizabeth Barbosa and Claudia Vel{\'a}zquez and Hern{\'a}ndez, {Normand Garc{\'i}a} and {Ordo{\~n}ez Razo}, {R. M.} and Luna, {David Mendez} and Mulia, {Lilian Yepez}",
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Calzada, F, Basurto, JC, Barbosa, E, Velázquez, C, Hernández, NG, Ordoñez Razo, RM, Luna, DM & Mulia, LY 2017, 'Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don', Pharmacognosy Research, pp. 133-137. https://doi.org/10.4103/0974-8490.204644

Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don. / Calzada, Fernando; Basurto, Jose Correa; Barbosa, Elizabeth; Velázquez, Claudia; Hernández, Normand García; Ordoñez Razo, R. M.; Luna, David Mendez; Mulia, Lilian Yepez.

In: Pharmacognosy Research, 01.04.2017, p. 133-137.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Antiprotozoal activities of tiliroside and other compounds from Sphaeralcea angustifolia (Cav.) G. don

AU - Calzada, Fernando

AU - Basurto, Jose Correa

AU - Barbosa, Elizabeth

AU - Velázquez, Claudia

AU - Hernández, Normand García

AU - Ordoñez Razo, R. M.

AU - Luna, David Mendez

AU - Mulia, Lilian Yepez

PY - 2017/4/1

Y1 - 2017/4/1

N2 - Background: Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. Objective: The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. Materials and Methods: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. Results: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 μg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from-9.92 kcal/mol and 53.57 μM, respectively) and G/FBPA (free binding energy from-7.17 kcal/mol and 55.5 μM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. Conclusion: The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery.

AB - Background: Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. Objective: The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. Materials and Methods: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. Results: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 μg/mL for E. histolytica and 17.4 μg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from-9.92 kcal/mol and 53.57 μM, respectively) and G/FBPA (free binding energy from-7.17 kcal/mol and 55.5 μM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. Conclusion: The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery.

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