title: In vitro and in vivo cysticidal activity of extracts and isolated flavanone from the bark of Prunus serotina: A bio-guided study.
abstract: Currently, neurocysticercosis treatment involves two drugs: albendazole and praziquantel; however, their efficacy is suboptimal and new cysticidal drugs are needed. The present paper reports the cysticidal activity of extracts of the bark from Prunus serotina against Taenia crassiceps cysts and the isolation and identification of the main components of the most active extract. Results showed that all extracts displayed in vitro cysticidal activity (EC50=17.9-88.5μg/mL), being the methanolic the most active and selective. Also, methanolic extract exhibited in vivo efficacy at 300mg/kg which was similar to that obtained with albendazole. Bio-guided fractionation of methanolic extract led the isolation of 2,3-dihydro-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one (naringenin, NGN), 3,4,5-trimethoxybenzoic acid and 1,3,5-trimethoxybenzene. NGN exhibited in vitro activity, in a time-concentration-dependent manner (EC50=89.3μM]. Furthermore, NGN at a dose of 376.1μmol/kg displayed similar in vivo efficacy than those obtained with albendazole at 188.4μmol/kg. NGN also caused a high level of damage in all parasite tissue in a similar manner than that observed with the methanolic extract. This study represents the first report of the cysticidal properties of the bark of P. serotina. NGN was identified as the main active compound of this specie and other studies are required to explore the potential of this flavanone as cysticidal agent.
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México.
authors.forename: Francisca
authors.initials: F
authors.lastname: Palomares-Alonso
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México; Facultad de Ciencia y Tecnología, Universidad Simón Bolívar, Ciudad de México 03920, México.
authors.forename: Irma Susana
authors.initials: IS
authors.lastname: Rojas-Tomé
authors.affiliation: Laboratorio de Neuroinmunología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México.
authors.forename: Guadalupe
authors.initials: G
authors.lastname: Palencia Hernández
authors.affiliation: Unidad de Investigación Médica en Farmacología, Unidad Médica de Alta Especialidad, Hospital de Especialidades, Centro Médico Nacional-Siglo XXI, Instituto Mexicano del Seguro Social, Ciudad de México 06720, México.
authors.forename: María Adelina
authors.initials: MA
authors.lastname: Jiménez-Arellanes
authors.affiliation: Departamento de Productos Naturales, Instituto de Química, Universidad Nacional Autónoma de México, Ciudad de México 04510, México.
authors.forename: Martha Lydia
authors.initials: ML
authors.lastname: Macías-Rubalcava
authors.affiliation: Laboratorio de Morfología Celular y Tisular, Instituto Nacional de Pediatría, Ciudad de México 04530, México.
authors.forename: Angélica
authors.initials: A
authors.lastname: González-Maciel
authors.affiliation: Laboratorio de Morfología Celular y Tisular, Instituto Nacional de Pediatría, Ciudad de México 04530, México.
authors.forename: Andrea
authors.initials: A
authors.lastname: Ramos-Morales
authors.affiliation: Facultad de Ciencia y Tecnología, Universidad Simón Bolívar, Ciudad de México 03920, México.
authors.forename: Rosalba
authors.initials: R
authors.lastname: Santiago-Reyes
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México.
authors.forename: Nelly
authors.initials: N
authors.lastname: Castro
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México.
authors.forename: Iliana
authors.initials: I
authors.lastname: González-Hernández
authors.affiliation: Laboratorio de Parasitología, Instituto Nacional de Pediatría, Ciudad de México 04530, México.
authors.forename: Yadira
authors.initials: Y
authors.lastname: Rufino-González
authors.affiliation: Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México; Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad de México 04510, México. Electronic address: helgijung@yahoo.com.mx.
authors.forename: Helgi
authors.initials: H
authors.lastname: Jung-Cook
mesh_terms: D015766:Albendazole / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D003551:Cysticercosis / Q000188:drug therapy*; D005260:Female; D044950:Flavanones / Q000494:pharmacology*; D051379:Mice; D008807:Mice, Inbred BALB C; D010936:Plant Extracts / Q000494:pharmacology*; D000068220:Prunus avium; D013621:Taenia / Q000187:drug effects*
chemical_list: D000871:Anthelmintics; D044950:Flavanones; D010936:Plant Extracts; D015766:Albendazole
keywords: 2,3-Dihydro-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one [naringenin]; Cysticidal activity; Prunus serotina; Selectivity index; Taenia crassiceps cysts