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DOI: 10.1055/s-2007-967178
© Georg Thieme Verlag KG Stuttgart · New York
Effects of Schisandra Lignans on P-Glycoprotein-Mediated Drug Efflux in Human Intestinal Caco-2 Cells
Publikationsverlauf
Received: September 12, 2006
Revised: February 20, 2007
Accepted: March 12, 2007
Publikationsdatum:
16. April 2007 (online)
![](https://www.thieme-connect.de/media/plantamedica/200705/lookinside/thumbnails/10.1055-s-2007-967178-1.jpg)
Abstract
Schisandra fruits (Schisandraceae) are often used in traditional medicine and can be taken concomitantly with conventional medicine. In this study, the effects of dibenzocyclooctadiene lignans from Schizandra chinensis on P-gp-mediated efflux were examined to investigate a possible interaction with P-gp substrates. The cellular accumulation of rhodamine-123 in Caco-2 cells was measured with 12 Schisandra lignans. Most compounds resulted in slight or moderate increases of rhodamin-123 cellular uptake, indicating their P-gp inhibitory activity. Among them, deoxyschizandrin exhibited the most potent effect on the accumulation of rhodamine-123. Subsequently, bidirectional transports of digoxin and rhodamine-123 in Caco-2 cells were determined with deoxyschizandrin, the most active compound for the rhodamine-123 assay. In the bidirectional transport study, apical-to-basal (A-to-B) transports of digoxin and rhodamine-123 were increased, whereas basal-to-apical (B-to-A) transports were decreased by deoxyschizandrin in concentration- and time-dependent manners. At 50 μM of deoxyschizandrin, the transport ratios (B-A/A-B) for digoxin and rhodamine-123 were 2.2 and 2.1 compared with the control ratios of 15.2 and 12.2, respectively. These results demonstrated that deoxyschizandrin effectively inhibited the P-gp-mediated efflux in Caco-2 cells, suggesting they could potentially increase the absorption of drugs that can act as a P-gp substrate.
Key words
Schisandra chinensis - Schisandraceae - P-glycoprotein - dibenzocyclooctadiene lignans - deoxyschizandrin - Caco-2 cells
- Supporting Information for this article is available online at
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Dr. Dong-Hyun Kim
Bioanalysis and Biotransformation Research Center
Korea Institute of Science and Technology
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