Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers

doi:10.5246/jcps.2011.06.075

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Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers

Cheng-Yue Zhang, Pan Zhao, Zhe Shi, Xiao-Da Yang^*

State Key Laboratories of Natural and Biomimetic Drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2011-05-10 Revised:2011-09-28 Online:2011-11-15 Published:2011-11-15
Contact: Xiao-Da Yang*

Abstract

Abstract:

Inducing resuscitation with herbal aromatics is important to modulate the brain intake of drugs in traditional Chinese medicine, but limited information has been available on the mechanism of action. The MDCK-MDR1 monolayer is an excellent in vitro cell model to use as a tool to study blood brain barrier (BBB) screening. In this study, we established MDCK-MDR1 cell line by stable transfection and investigated the effects of several important herbal aromatics on BBB permeability. The characterization experiment demonstrated the MDCK-MDR1 used in this study was valid. In a transport study, we found several herbal aromatics increased the permeability of fluorescein isothiocyanate-labeled dextran 4kDa (FD4) and inhibited efflux of Rhodamine123 (Rho123). These results demonstrated that herbal aromatics enhanced the BBB permeation of drugs by both inhibition of P-gp and opening of the BBB tight junction, thus providing new insights for understanding the mechanisms of aromatic compounds’ BBB permeability.

Key words: Herbal aromatics, MDCK-MDR1, Tight junction, P-gp

CLC Number:

R962

Supporting:

Cheng-Yue Zhang, Pan Zhao, Zhe Shi, Xiao-Da Yang^*. Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers [J]. , DOI: 10.5246/jcps.2011.06.075.

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Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers

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