Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model

Puerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the con...

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Main Authors: Li Jiang, Yanling Xiong, Yu Tu, Wentong Zhang, Qiyun Zhang, Peng Nie, Xiaojun Yan, Hongning Liu, Ronghua Liu, Guoliang Xu
Format: Article
Language:English
Published: MDPI AG 2022-02-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/4/1230
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author Li Jiang
Yanling Xiong
Yu Tu
Wentong Zhang
Qiyun Zhang
Peng Nie
Xiaojun Yan
Hongning Liu
Ronghua Liu
Guoliang Xu
author_facet Li Jiang
Yanling Xiong
Yu Tu
Wentong Zhang
Qiyun Zhang
Peng Nie
Xiaojun Yan
Hongning Liu
Ronghua Liu
Guoliang Xu
author_sort Li Jiang
collection DOAJ
description Puerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the concentration in Caco-2 cell of PUR and GAS was determined by HPLC method. The bidirectional transport of PUR and GAS and the inhibition of drug efflux including verapamil and cyclosporine on the transport of these two components were studied. The mutual influence between PUR and GAS, especially the effect of the latter on the former of the bidirectional transport were also investigated. The transport of 50 μg·mL<sup>−1</sup> PUR in Caco-2 cells has no obvious directionality. While the transport of 100 and 200 μg·mL<sup>−1</sup> PUR presents a strong directionality, and this directionality can be inhibited by verapamil and cyclosporine. When PUR and GAS were used in combination, GAS could increase the absorption of PUR while PUR had no obvious influence on GAS. Therefore, the compatibility of PUR and GAS is reasonable, and GAS can promote the transmembrane transport of PUR, the effect of which is similar to that of verapamil.
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spelling doaj.art-5653f689e8dc4f849a8e223fe71b479d2023-11-23T21:20:48ZengMDPI AGMolecules1420-30492022-02-01274123010.3390/molecules27041230Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer ModelLi Jiang0Yanling Xiong1Yu Tu2Wentong Zhang3Qiyun Zhang4Peng Nie5Xiaojun Yan6Hongning Liu7Ronghua Liu8Guoliang Xu9Center for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaDepartment of Clinical Pharmacology, Xiangya Hospital, Central South University, 87 Xiangya Road, Changsha 410008, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaDepartment of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaCenter for Differentiation and Development of TCM Basic Theory, Jiangxi University of Chinese Medicine, Nanchang 330004, ChinaPuerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the concentration in Caco-2 cell of PUR and GAS was determined by HPLC method. The bidirectional transport of PUR and GAS and the inhibition of drug efflux including verapamil and cyclosporine on the transport of these two components were studied. The mutual influence between PUR and GAS, especially the effect of the latter on the former of the bidirectional transport were also investigated. The transport of 50 μg·mL<sup>−1</sup> PUR in Caco-2 cells has no obvious directionality. While the transport of 100 and 200 μg·mL<sup>−1</sup> PUR presents a strong directionality, and this directionality can be inhibited by verapamil and cyclosporine. When PUR and GAS were used in combination, GAS could increase the absorption of PUR while PUR had no obvious influence on GAS. Therefore, the compatibility of PUR and GAS is reasonable, and GAS can promote the transmembrane transport of PUR, the effect of which is similar to that of verapamil.https://www.mdpi.com/1420-3049/27/4/1230transport mechanismpueraringastrodinabsorptionCaco-2 cell monolayer
spellingShingle Li Jiang
Yanling Xiong
Yu Tu
Wentong Zhang
Qiyun Zhang
Peng Nie
Xiaojun Yan
Hongning Liu
Ronghua Liu
Guoliang Xu
Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
Molecules
transport mechanism
puerarin
gastrodin
absorption
Caco-2 cell monolayer
title Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
title_full Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
title_fullStr Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
title_full_unstemmed Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
title_short Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model
title_sort elucidation of the transport mechanism of puerarin and gastrodin and their interaction on the absorption in a caco 2 cell monolayer model
topic transport mechanism
puerarin
gastrodin
absorption
Caco-2 cell monolayer
url https://www.mdpi.com/1420-3049/27/4/1230
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