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Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles

Mango seed kernel extract (MSKE) and its key components (gallic acid, GA; methyl gallate, MG; and pentagalloyl glucopyranose, PGG) have generated interest because of their pharmacological activities. To develop the potential use of the key components in MSKE as natural therapeutic agents, their phar...

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Autores principales: Jiamboonsri, Pimsumon, Pithayanukul, Pimolpan, Bavovada, Rapepol, Leanpolchareanchai, Jiraporn, Yin, Taijun, Gao, Song, Hu, Ming
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332320/
https://www.ncbi.nlm.nih.gov/pubmed/26633325
http://dx.doi.org/10.3390/molecules201219759
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author Jiamboonsri, Pimsumon
Pithayanukul, Pimolpan
Bavovada, Rapepol
Leanpolchareanchai, Jiraporn
Yin, Taijun
Gao, Song
Hu, Ming
author_facet Jiamboonsri, Pimsumon
Pithayanukul, Pimolpan
Bavovada, Rapepol
Leanpolchareanchai, Jiraporn
Yin, Taijun
Gao, Song
Hu, Ming
author_sort Jiamboonsri, Pimsumon
collection PubMed
description Mango seed kernel extract (MSKE) and its key components (gallic acid, GA; methyl gallate, MG; and pentagalloyl glucopyranose, PGG) have generated interest because of their pharmacological activities. To develop the potential use of the key components in MSKE as natural therapeutic agents, their pharmacokinetic data are necessary. Therefore, this study was performed to evaluate the factors affecting their oral bioavailability as pure compounds and as components in MSKE. The in vitro chemical stability, biological stability, and absorption were evaluated in Hanks’ Balanced Salt Solution, Caco-2 cell and rat fecal lysates, and the Caco-2 cell model, respectively. The in vivo oral pharmacokinetic behavior was elucidated in Sprague-Dawley rats. The key components were unstable under alkaline conditions and in Caco-2 cell lysates or rat fecal lysates. The absorptive permeability coefficient followed the order MG > GA > PGG. The in vivo results exhibited similar pharmacokinetic trends to the in vitro studies. Additionally, the co-components in MSKE may affect the pharmacokinetic behaviors of the key components in MSKE. In conclusion, chemical degradation under alkaline conditions, biological degradation by intestinal cell and colonic microflora enzymes, and low absorptive permeability could be important factors underlying the oral bioavailability of these polyphenols.
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spelling pubmed-63323202019-01-24 Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles Jiamboonsri, Pimsumon Pithayanukul, Pimolpan Bavovada, Rapepol Leanpolchareanchai, Jiraporn Yin, Taijun Gao, Song Hu, Ming Molecules Article Mango seed kernel extract (MSKE) and its key components (gallic acid, GA; methyl gallate, MG; and pentagalloyl glucopyranose, PGG) have generated interest because of their pharmacological activities. To develop the potential use of the key components in MSKE as natural therapeutic agents, their pharmacokinetic data are necessary. Therefore, this study was performed to evaluate the factors affecting their oral bioavailability as pure compounds and as components in MSKE. The in vitro chemical stability, biological stability, and absorption were evaluated in Hanks’ Balanced Salt Solution, Caco-2 cell and rat fecal lysates, and the Caco-2 cell model, respectively. The in vivo oral pharmacokinetic behavior was elucidated in Sprague-Dawley rats. The key components were unstable under alkaline conditions and in Caco-2 cell lysates or rat fecal lysates. The absorptive permeability coefficient followed the order MG > GA > PGG. The in vivo results exhibited similar pharmacokinetic trends to the in vitro studies. Additionally, the co-components in MSKE may affect the pharmacokinetic behaviors of the key components in MSKE. In conclusion, chemical degradation under alkaline conditions, biological degradation by intestinal cell and colonic microflora enzymes, and low absorptive permeability could be important factors underlying the oral bioavailability of these polyphenols. MDPI 2015-11-30 /pmc/articles/PMC6332320/ /pubmed/26633325 http://dx.doi.org/10.3390/molecules201219759 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Jiamboonsri, Pimsumon
Pithayanukul, Pimolpan
Bavovada, Rapepol
Leanpolchareanchai, Jiraporn
Yin, Taijun
Gao, Song
Hu, Ming
Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title_full Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title_fullStr Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title_full_unstemmed Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title_short Factors Influencing Oral Bioavailability of Thai Mango Seed Kernel Extract and Its Key Phenolic Principles
title_sort factors influencing oral bioavailability of thai mango seed kernel extract and its key phenolic principles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332320/
https://www.ncbi.nlm.nih.gov/pubmed/26633325
http://dx.doi.org/10.3390/molecules201219759
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