Effects of Schisandra lignans on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells
- Authors
- Yoo, Hye Hyun; Lee, Mijin; Lee, Min Woo; Lim, Sun Young; Shin, Jongheon; Kim, Dong-Hyun
- Issue Date
- May-2007
- Publisher
- GEORG THIEME VERLAG KG
- Keywords
- Schisandra chinensis; Schisandraceae; P-glycoprotein; dibenzo-cyclooctadiene lignans; deoxyschizandrin; Caco-2 cells
- Citation
- PLANTA MEDICA, v.73, no.5, pp.444 - 450
- Indexed
- SCIE
SCOPUS
- Journal Title
- PLANTA MEDICA
- Volume
- 73
- Number
- 5
- Start Page
- 444
- End Page
- 450
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/43754
- DOI
- 10.1055/s-2007-967178
- ISSN
- 0032-0943
- 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.
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