title: Cysticidal activity of extracts and isolated compounds from Teloxys graveolens: In vitro and in vivo studies.
abstract: In the search of new alternatives for neurocysticercosis treatment, the cysticidal activity of organic extracts of Teloxys graveolens was evaluated. The in vitro activity of hexane, ethyl acetate and methanol extracts against Taenia crassiceps cysts was tested and the selectivity index relative to human fibroblasts was determined. Subsequently, the in vivo efficacy of the methanolic extract at doses of 200 and 500 mg/kg in the murine cysticercosis model was evaluated. The ultrastructural effects in vitro and in vivo of the methanolic extract were also investigated using scanning electron microscopy. Additionally, a bioassay-guided fractionation for the isolation of the cysticidal components was performed. Our in vitro findings revealed that all extracts exhibited good cysticidal activity with EC50 values from 44.8 to 67.1 µg/mL. Although the ethyl acetate and methanolic extracts displayed low cytotoxicity, the methanolic extract was the most selective. The methanolic extract also showed in vivo efficacy which was similar to that obtained with ABZ. Significant alterations were found on the germinal layer of the cysts, with a high accumulation of granules of glycogen and vacuoles. The bioguided fractionation of methanolic extract led to the isolation of three flavonoids: chrysin, pinocembrin and pinostrobin; among them, pinocembrin was the compound that displayed cysticidal activity. This is the first study which reveals that T. graveolens could be a potential source for cysticidal and non-toxic compounds.
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, 14269 Mexico D.F., Mexico.
authors.forename: Francisca
authors.initials: F
authors.lastname: Palomares-Alonso
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, 14269 Mexico D.F., Mexico; Facultad de Ciencia y Tecnología, Universidad Simón Bolívar, 03920 Mexico D.F., Mexico.
authors.forename: Irma Susana
authors.initials: IS
authors.lastname: Rojas-Tomé
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, 14269 Mexico D.F., Mexico.
authors.forename: Victorino
authors.initials: V
authors.lastname: Juárez Rocha
authors.affiliation: Laboratorio de Neuroinmunología, Instituto Nacional de Neurología y Neurocirugía, 14269 México D.F., Mexico.
authors.forename: Guadalupe
authors.initials: G
authors.lastname: Palencia Hernández
authors.affiliation: Laboratorio de Morfología Celular y Tisular, Instituto Nacional de Pediatría, 04530 México D.F., Mexico.
authors.forename: Angélica
authors.initials: A
authors.lastname: González-Maciel
authors.affiliation: Laboratorio de Morfología Celular y Tisular, Instituto Nacional de Pediatría, 04530 México D.F., Mexico.
authors.forename: Andrea
authors.initials: A
authors.lastname: Ramos-Morales
authors.affiliation: Facultad de Ciencia y Tecnología, Universidad Simón Bolívar, 03920 Mexico D.F., Mexico.
authors.forename: Rosalba
authors.initials: R
authors.lastname: Santiago-Reyes
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, 14269 Mexico D.F., Mexico.
authors.forename: Iliana Elvira
authors.initials: IE
authors.lastname: González-Hernández
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, 14269 Mexico D.F., Mexico; Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, 04510 México D.F., Mexico. Electronic address: helgi@servidor.unam.mx.
authors.forename: Helgi
authors.initials: H
authors.lastname: Jung-Cook
mesh_terms: D027703:Amaranthaceae / Q000737:chemistry*; D000818:Animals; D001681:Biological Assay; D003551:Cysticercosis / Q000188:drug therapy*; D003552:Cysticercus / Q000187:drug effects* / Q000648:ultrastructure; D005260:Female; D005347:Fibroblasts / Q000187:drug effects; D044950:Flavanones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005881:Gingiva / Q000166:cytology; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D046529:Microscopy, Electron, Transmission; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity
chemical_list: D044950:Flavanones; D005419:Flavonoids; D010936:Plant Extracts; C043561:chrysin; C016063:pinocembrin; C411294:pinostrobin
keywords: Cysticercus; Cysticidal activity; Cytotoxicity; Murine cysticercosis; Taenia crassiceps; Teloxys graveolens