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Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana

An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids were not detected in plasma over 24 h. However, meta and para hydroxyphenylacetic acid...

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Autores principales: Juárez Ramírez, Virgilio Alfonso, Jiménez-Beltrán, María Isabel, Zamilpa, Alejandro, Herrera-Ruiz, Maribel, Abarca-Vargas, Rodolfo, Lombardo-Earl, Galia, Tortoriello, Jaime, Jiménez-Ferrer, Enrique
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152131/
https://www.ncbi.nlm.nih.gov/pubmed/28749448
http://dx.doi.org/10.3390/molecules22081260
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author Juárez Ramírez, Virgilio Alfonso
Jiménez-Beltrán, María Isabel
Zamilpa, Alejandro
Herrera-Ruiz, Maribel
Abarca-Vargas, Rodolfo
Lombardo-Earl, Galia
Tortoriello, Jaime
Jiménez-Ferrer, Enrique
author_facet Juárez Ramírez, Virgilio Alfonso
Jiménez-Beltrán, María Isabel
Zamilpa, Alejandro
Herrera-Ruiz, Maribel
Abarca-Vargas, Rodolfo
Lombardo-Earl, Galia
Tortoriello, Jaime
Jiménez-Ferrer, Enrique
author_sort Juárez Ramírez, Virgilio Alfonso
collection PubMed
description An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids were not detected in plasma over 24 h. However, meta and para hydroxyphenylacetic acid and dihydroxyphenylacetic acid (m-HPAA, p-HPAA and DOPAC) were monitored. These are the biotransformation compounds of the aglycones of kaempferol and quercetin; these aglycones are products of the other flavonoids present in the anxiolytic fraction. The analytical methods (HPLC) for flavonoids and the related compounds (m-HPAA, p-HPAA and DOPAC) were validated, determining the parameters of accuracy, precision, specificity or selectivity, limit of detection, quantification range, and robustness. The pharmacokinetic assay was performed with ICR mice strains, which were given 200 mg/kg of the standardized active fraction. The results of validation of the analytical methods were obtained, allowing it to be established in a validated way that no flavonoids present in the anxiolytic fraction of T. americana were detected in plasma. However, detection and follow up was possible for the serum levels of m-HPAA, p-HPAA, and DOPAC. The three compounds follow a two-compartment model with very similar parameters between m-HPAA and p-HPAA, some being different from the ones characterized in the pharmacokinetics of DOPAC.
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spelling pubmed-61521312018-11-13 Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana Juárez Ramírez, Virgilio Alfonso Jiménez-Beltrán, María Isabel Zamilpa, Alejandro Herrera-Ruiz, Maribel Abarca-Vargas, Rodolfo Lombardo-Earl, Galia Tortoriello, Jaime Jiménez-Ferrer, Enrique Molecules Article An anxiolytic fraction of Tilia americana standardized in tiliroside, rutin, quercitrin, quercetin glucoside, and kaempferol was obtained. After oral administration of the fraction, the above-mentioned flavonoids were not detected in plasma over 24 h. However, meta and para hydroxyphenylacetic acid and dihydroxyphenylacetic acid (m-HPAA, p-HPAA and DOPAC) were monitored. These are the biotransformation compounds of the aglycones of kaempferol and quercetin; these aglycones are products of the other flavonoids present in the anxiolytic fraction. The analytical methods (HPLC) for flavonoids and the related compounds (m-HPAA, p-HPAA and DOPAC) were validated, determining the parameters of accuracy, precision, specificity or selectivity, limit of detection, quantification range, and robustness. The pharmacokinetic assay was performed with ICR mice strains, which were given 200 mg/kg of the standardized active fraction. The results of validation of the analytical methods were obtained, allowing it to be established in a validated way that no flavonoids present in the anxiolytic fraction of T. americana were detected in plasma. However, detection and follow up was possible for the serum levels of m-HPAA, p-HPAA, and DOPAC. The three compounds follow a two-compartment model with very similar parameters between m-HPAA and p-HPAA, some being different from the ones characterized in the pharmacokinetics of DOPAC. MDPI 2017-07-27 /pmc/articles/PMC6152131/ /pubmed/28749448 http://dx.doi.org/10.3390/molecules22081260 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Juárez Ramírez, Virgilio Alfonso
Jiménez-Beltrán, María Isabel
Zamilpa, Alejandro
Herrera-Ruiz, Maribel
Abarca-Vargas, Rodolfo
Lombardo-Earl, Galia
Tortoriello, Jaime
Jiménez-Ferrer, Enrique
Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title_full Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title_fullStr Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title_full_unstemmed Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title_short Pharmacokinetic Study of Biotransformation Products from an Anxiolytic Fraction of Tilia americana
title_sort pharmacokinetic study of biotransformation products from an anxiolytic fraction of tilia americana
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152131/
https://www.ncbi.nlm.nih.gov/pubmed/28749448
http://dx.doi.org/10.3390/molecules22081260
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