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Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model
Epimedium spp. is commonly used in Traditional Chinese Medicine. Epimedins A, B, and C are three major bioactive flavonoids found in Epimedium spp. that share similar chemical structures. In this study, the intestinal absorption mechanism of these three compounds was investigated using the Caco-2 ce...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270917/ https://www.ncbi.nlm.nih.gov/pubmed/24402200 http://dx.doi.org/10.3390/molecules19010686 |
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author | Chen, Yan Wang, Ying Zhou, Jing Gao, Xia Qu, Ding Liu, Congyan |
author_facet | Chen, Yan Wang, Ying Zhou, Jing Gao, Xia Qu, Ding Liu, Congyan |
author_sort | Chen, Yan |
collection | PubMed |
description | Epimedium spp. is commonly used in Traditional Chinese Medicine. Epimedins A, B, and C are three major bioactive flavonoids found in Epimedium spp. that share similar chemical structures. In this study, the intestinal absorption mechanism of these three compounds was investigated using the Caco-2 cell monolayer model in both the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) direction. The absorption permeability (P(AB)) of epimedins A, B, and C were extremely low and increased as the concentration of the epimedins increased from 5 to 20 μM, but, at 40 μM, the P(AB) values were reduced. Meanwhile, the amount of transported compounds increased in a time-dependent manner. The P(AB) of epimedins A and C were significantly increased and efflux ratios decreased in the presence of verapamil (an inhibitor of P-glycoprotein) and dipyridamole (an inhibitor of breast cancer resistance protein) while, in the presence of MK571 (an inhibitor of multidrug resistance proteins), the absorption of epimedins A and C did not change significantly, indicating that P-gp and BCRP might be involved in the transport of epimedins A and C. The P(AB) of epimedin B significantly increased while its secretory permeability (P(BA)) significantly decreased in the presence of dipyridamole, indicating that BCRP might be involved in the transport of epimedin B. No obvious changes in the transport of epimedin B were observed in the presence of verapamil and MK571. In summary, our results clearly demonstrate, for the first time, that poor bioavailability of these three prenylated flavonoids is the result of poor intrinsic permeability and efflux by apical efflux transporters. |
format | Online Article Text |
id | pubmed-6270917 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62709172018-12-20 Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model Chen, Yan Wang, Ying Zhou, Jing Gao, Xia Qu, Ding Liu, Congyan Molecules Article Epimedium spp. is commonly used in Traditional Chinese Medicine. Epimedins A, B, and C are three major bioactive flavonoids found in Epimedium spp. that share similar chemical structures. In this study, the intestinal absorption mechanism of these three compounds was investigated using the Caco-2 cell monolayer model in both the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) direction. The absorption permeability (P(AB)) of epimedins A, B, and C were extremely low and increased as the concentration of the epimedins increased from 5 to 20 μM, but, at 40 μM, the P(AB) values were reduced. Meanwhile, the amount of transported compounds increased in a time-dependent manner. The P(AB) of epimedins A and C were significantly increased and efflux ratios decreased in the presence of verapamil (an inhibitor of P-glycoprotein) and dipyridamole (an inhibitor of breast cancer resistance protein) while, in the presence of MK571 (an inhibitor of multidrug resistance proteins), the absorption of epimedins A and C did not change significantly, indicating that P-gp and BCRP might be involved in the transport of epimedins A and C. The P(AB) of epimedin B significantly increased while its secretory permeability (P(BA)) significantly decreased in the presence of dipyridamole, indicating that BCRP might be involved in the transport of epimedin B. No obvious changes in the transport of epimedin B were observed in the presence of verapamil and MK571. In summary, our results clearly demonstrate, for the first time, that poor bioavailability of these three prenylated flavonoids is the result of poor intrinsic permeability and efflux by apical efflux transporters. MDPI 2014-01-07 /pmc/articles/PMC6270917/ /pubmed/24402200 http://dx.doi.org/10.3390/molecules19010686 Text en © 2014 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 license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Chen, Yan Wang, Ying Zhou, Jing Gao, Xia Qu, Ding Liu, Congyan Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title | Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title_full | Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title_fullStr | Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title_full_unstemmed | Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title_short | Study on the Mechanism of Intestinal Absorption of Epimedins A, B and C in the Caco-2 Cell Model |
title_sort | study on the mechanism of intestinal absorption of epimedins a, b and c in the caco-2 cell model |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270917/ https://www.ncbi.nlm.nih.gov/pubmed/24402200 http://dx.doi.org/10.3390/molecules19010686 |
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