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Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus

The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A(1); the findings indicated that the bioavailability of Holotoxin A(1) was lower than Echinoside A. We inferred tha...

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Detalles Bibliográficos
Autores principales: Li, Shuai, Wang, Yuanhong, Jiang, Tingfu, Wang, Han, Yang, Shuang, Lv, Zhihua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4926073/
https://www.ncbi.nlm.nih.gov/pubmed/27322290
http://dx.doi.org/10.3390/md14060114
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author Li, Shuai
Wang, Yuanhong
Jiang, Tingfu
Wang, Han
Yang, Shuang
Lv, Zhihua
author_facet Li, Shuai
Wang, Yuanhong
Jiang, Tingfu
Wang, Han
Yang, Shuang
Lv, Zhihua
author_sort Li, Shuai
collection PubMed
description The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A(1); the findings indicated that the bioavailability of Holotoxin A(1) was lower than Echinoside A. We inferred that the differences in chemical structure between compounds was a factor that explained their different characteristics of transport across the intestine. In order to confirm the absorption characteristics of Echinoside A and Holotoxin A(1), we examined their transport across Caco-2 cell monolayer and effective permeability by single-pass intestinal perfusion. The results of Caco-2 cell model indicate that Echinoside A is transported by passive diffusion, and not influenced by the exocytosis of P-glycoprotein (P-gp, expressed in the apical side of Caco-2 monolayers as the classic inhibitor). The intestinal perfusion also demonstrated well the absorption of Echinoside A and poor absorption of Holotoxin A(1), which matched up with the result of the Caco-2 cell model. The results demonstrated our conjecture and provides fundamental information on the relationship between the chemical structure of these sea cucumber saponins and their absorption characteristics, and we believe that our findings build a foundation for the further metabolism study of sea cucumber saponins and contribute to the further clinical research of saponins.
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spelling pubmed-49260732016-07-06 Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus Li, Shuai Wang, Yuanhong Jiang, Tingfu Wang, Han Yang, Shuang Lv, Zhihua Mar Drugs Article The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A(1); the findings indicated that the bioavailability of Holotoxin A(1) was lower than Echinoside A. We inferred that the differences in chemical structure between compounds was a factor that explained their different characteristics of transport across the intestine. In order to confirm the absorption characteristics of Echinoside A and Holotoxin A(1), we examined their transport across Caco-2 cell monolayer and effective permeability by single-pass intestinal perfusion. The results of Caco-2 cell model indicate that Echinoside A is transported by passive diffusion, and not influenced by the exocytosis of P-glycoprotein (P-gp, expressed in the apical side of Caco-2 monolayers as the classic inhibitor). The intestinal perfusion also demonstrated well the absorption of Echinoside A and poor absorption of Holotoxin A(1), which matched up with the result of the Caco-2 cell model. The results demonstrated our conjecture and provides fundamental information on the relationship between the chemical structure of these sea cucumber saponins and their absorption characteristics, and we believe that our findings build a foundation for the further metabolism study of sea cucumber saponins and contribute to the further clinical research of saponins. MDPI 2016-06-17 /pmc/articles/PMC4926073/ /pubmed/27322290 http://dx.doi.org/10.3390/md14060114 Text en © 2016 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
Li, Shuai
Wang, Yuanhong
Jiang, Tingfu
Wang, Han
Yang, Shuang
Lv, Zhihua
Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title_full Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title_fullStr Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title_full_unstemmed Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title_short Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
title_sort absorption and transport of sea cucumber saponins from apostichopus japonicus
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4926073/
https://www.ncbi.nlm.nih.gov/pubmed/27322290
http://dx.doi.org/10.3390/md14060114
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