Effects of Schisandra lignans on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells

Title
Effects of Schisandra lignans on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells
Author
유혜현
Keywords
Schisandra chinensis; Schisandraceae; P-glycoprotein; dibenzo-cyclooctadiene lignans; deoxyschizandrin; Caco-2 cells
Issue Date
2007-05
Publisher
GEORG THIEME VERLAG KG
Citation
PLANTA MEDICA, v. 73, No. 5, Page. 444-450
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-1 23 cellular uptake, indicating their P-gp inhibitory activity. Among them, cleoxyschizandrin 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 cleoxyschizandrin, 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 mu M 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.
URI
https://www.thieme-connect.com/products/ejournals/html/10.1055/s-2007-967178http://repository.hanyang.ac.kr/handle/20.500.11754/106508
ISSN
0032-0943; 1439-0221
DOI
10.1055/s-2007-967178
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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