Yoo, Hye Hyun Lee, Mijin Lee, Min Woo Lim, Sun Young Shin, Jongheon Kim, Dong-Hyun 2024-01-21T01:03:42Z 2024-01-21T01:03:42Z 2021-09-02 2007-05 0032-0943 https://pubs.kist.re.kr/handle/201004/134428 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. English GEORG THIEME VERLAG KG GOMISIN-A DIBENZOCYCLOOCTADIENE LIGNANS ANTIOXIDANT ACTIVITY HEPATOCARCINOGENESIS CYTOCHROME-P450 METABOLISM CHINENSIS TRANSPORT CYP3A4 DIET Effects of Schisandra lignans on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells Article 10.1055/s-2007-967178 1 PLANTA MEDICA, v.73, no.5, pp.444 - 450 PLANTA MEDICA 73 5 444 450 scie scopus 000246963300006 2-s2.0-34250365825 Plant Sciences Chemistry, Medicinal Integrative & Complementary Medicine Pharmacology & Pharmacy Plant Sciences Pharmacology & Pharmacy Integrative & Complementary Medicine Article GOMISIN-A DIBENZOCYCLOOCTADIENE LIGNANS ANTIOXIDANT ACTIVITY HEPATOCARCINOGENESIS CYTOCHROME-P450 METABOLISM CHINENSIS TRANSPORT CYP3A4 DIET Schisandra chinensis Schisandraceae P-glycoprotein dibenzo-cyclooctadiene lignans deoxyschizandrin Caco-2 cells