title: Pharmacokinetic study in mice of galphimine-A, an anxiolytic compound from Galphimia glauca.
abstract: The aim of this study was to obtain pharmacokinetic data for the anxiolytic compound galphimine-A (G-A) from Galphimia glauca. G-A is the most abundant anxiolytic compound in this plant, while Galphimine-E (G-E) is the most abundant galphimine, but inactive. G-E was transformed chemically into G-A. The pharmacokinetic study was carried out in ICR mice, which were orally administered a single 200 mg/kg dose of G-A. Samples of blood and brain were taken at different times after administration of G-A. Previously, we established the validation of methods for determining the concentration of G-A. The G-A was detected in plasma 5 min after oral administration, and its concentration reached 2.47 μg/mL. Data from concentration-time curves allowed us to establish the main pharmacokinetic parameters in two models: one- and/or two-compartment. C(max) values were 3.33 and 3.42 μg/mL respectively, likewise AUC(0→1440 min) were 1,951.58 and 1,824.95 μg/mL·min. The G-A in brain tissue was noted to cross the blood-brain barrier, reaching C(max) 2.74 μg/mL, T(max) 81.6 min, and then drop gradually to 0.32 μg/mL detected at 24 h. The presence of G-A in brain tissue, confirmed that this anxiolytic compound can access the target organ and acts directly on the CNS.
authors.affiliation: Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, Xochitepec 62790, Morelos, Mexico. aaaf@xanum.uam.mx.
authors.forename: Rodolfo
authors.initials: R
authors.lastname: Abarca Vargas
authors.affiliation: Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, Xochitepec 62790, Morelos, Mexico. azamilpa_2000@yahoo.com.mx.
authors.forename: Alejandro
authors.initials: A
authors.lastname: Zamilpa
authors.affiliation: Doctorado en Ciencias Biológicas y de la Salud, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Iztapalapa, San Rafael Actlixco No. 186, Col. Vicentina, Iztapalapa 09340, Mexico. aaaf@xanum.uam.mx.
authors.forename: Francisco Alarcón
authors.initials: FA
authors.lastname: Aguilar
authors.affiliation: Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, Xochitepec 62790, Morelos, Mexico.
authors.forename: Maribel
authors.initials: M
authors.lastname: Herrera-Ruiz
authors.affiliation: Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, Xochitepec 62790, Morelos, Mexico. jtortora2@yahoo.es.
authors.forename: Jaime
authors.initials: J
authors.lastname: Tortoriello
authors.affiliation: Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina No. 1, Col. Centro, Xochitepec 62790, Morelos, Mexico. enriqueferrer_mx@yahoo.com.
authors.forename: Enrique
authors.initials: E
authors.lastname: Jiménez-Ferrer
mesh_terms: D000284:Administration, Oral; D000818:Animals; D014151:Anti-Anxiety Agents / Q000737:chemistry* / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D031582:Galphimia / Q000737:chemistry*; D051379:Mice; D010936:Plant Extracts / Q000737:chemistry; D015203:Reproducibility of Results; D014315:Triterpenes / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D014151:Anti-Anxiety Agents; D010936:Plant Extracts; D014315:Triterpenes; C504560:galphimine A; C508540:galphimine E