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    Antiprotozoal Activities of Tiliroside and other Compounds from Sphaeralcea angustifolia (Cav.) G. Don

    Fernando Calzada1★, Jose Correa Basurto2, Elizabeth Barbosa3, Claudia Velázquez4, Normand García Hernández5, RM Ordoñez Razo5, David Mendez Luna2, Lilian Yepez Mulia6★ Corresponding author

    1. 1Medical Research Unit in Pharmacology, UMAE Speciality Hospital-2° Floor CORCE National Medical Center Siglo XXI, IMSS, Av. Cuauhtemoc 330, Col. Doctores, CP 06725, México City, MEXICO.
    2. 2Laboratory of Molecular Modeling and Bioinformátics & Drug Design, Superior School of Medicine of IPN, Plan de San Luis y Díaz Mirón s/n, 11340 México City, MEXICO.
    3. 3Postgraduate Studies and Research, Superior School of Medicine of IPN, Plan de San Luís y Díaz Mirón, CP 11340, México City, MEXICO.
    4. 4Institute of Health Sciences, Autonomous University of the State of Hidalgo, Km. 4.5 Carretera Pachuca-Tulancingo, Unidad Universitaria, C. P. 42076 Pachuca, Hidalgo, MEXICO.
    5. 5Medical Research Unit in Human Genetics UMAE Pediatric Hospital, Medical Center Siglo XXI, IMSS, MEXICO.
    6. 6Medical Research Unit in Infectious and Parasitic Diseases UMAE Pediatric Hospital, Medical Center Siglo XXI, IMSS, MEXICO.

    CORRESPONDENCE

    Fernando Calzada

    Medical Research Unit in Pharmacology, UMAE Speciality Hospital-2° Floor CORCE National Medical Center Siglo XXI, IMSS, Av. Cuauhtemoc 330, Col. Doctores, CP 06725, México City, MEXICO.

    fercalber10@gmail.com

    Volume 9, Issue 2 · pp. 133–137 · PUBLISHED · DOI: 10.4103/0974-8490.204644

    View on Pharmacogn. Res. original site ↗

    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 usingin vitro antiprotozoal activity and computational experiments. Materials and Methods: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolyticaand 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 ofS. angustifoliagives tiliroside and apigenin, caffeic acid, protocatechuic acid, and β‑sitosterol. The in vitroantiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 μg/mL forE. histolytica and 17.4 μg/mL forG. 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 ofS. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifoliain gastrointestinal disorders such as diarrhea and dysentery.

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      Calzada, F., Basurto, J. C., Barbosa, E., Velázquez, C., Hernández, N. G., Razo, R. O., Luna, D. M., & Mulia, L. Y. (). Antiprotozoal Activities of Tiliroside and other Compounds from Sphaeralcea angustifolia (Cav.) G. Don. Pharmacognosy Research, 9(2), 133–137. https://doi.org/10.4103/0974-8490.204644