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学科主题: 物理化学
题名: Schisandra Lignans, Deoxyschizandrin and Gomisin A, Enhanced the Transport of Drugs as a P-gp Substrate by Inhibiting the P-gp-mediated Efflux Effectively
作者: Li N(李娜) ;  Hu Y(胡莹) ;  Yu Y(于洋) ;  Yang L(杨凌)
会议名称: 第十八届微粒体与药物氧化国际学术会议
会议日期: 2010-5-16
出版日期: 2010-05-16
会议地点: 中国
通讯作者: 杨凌
部门归属: 十八室
主办者: 中国医学科学院
摘要: BACKGROUND. Schisandra fruits are extensively used as traditional medicine in China, Japan and Korea(Chang et al., 2005). Deoxyschizandrin(DSZ), gomisin A(Go A) and schizandrin, the major active components of S. chinensis, have been reported to show anti-inflammatory, anti-cancer, and anti-hepatocarcinogenesis activity (Wagner et al., 1996). Recently, schizandrin B was reported to have an inhibitory effect on P-glycoprotein (P-gp), a drug efflux pump(Qiangrong et al., 2005). The report suggested that lignans from S. chinensis can influence intestinal absorption of drugs that are P-gp substrates. In the study, we investigated the effects of DSZ and Go A on P-gp mediated transport of rhodamine 123 (R123) in Caco-2 cell monolayer. METHOD. The Caco-2 cells were cultured in Transwell with 0.33cm2 permeable polycarbonateinserts in 24-well plates for 21days. The integrity of the cell monolayers was measured by transepithelial electrical resistance (TEER) using a Millicell-ERS voltohmmeter. Transport studies were initiated by replacing the transport medium on the apical with an equal volume of HBSS/HEPES buffer containing 25 μM R123 and fresh HBSS/HEPES buffer on the basolateral side. Sixty microliters of the medium from the receiver compartment were taken at every 30 min, and R123 was quantified by fluorescence detector. In inhibition experiments, 50μM verapamil hydrochloride was added to both the apical and basal side. RESULTS. The transport of R123 in two directions was approximately proportional to incubation time up to 1.5 h. DSZ and Go A increased its absorptive transport and reduced its excretive transport in a time dependent manner. At the presence of 50 μM DSZ, the Papp,A-B of R123 was increased from 2.5±0.2 nm/s to 7.9±1.0 nm/s, whereas its Papp,B-A was decreased from 12.1 ±0.7 nm/s to 8.1 ±0.7 nm/s. At the presence of 50 μM Go A, the Papp,A-B of R123 was increased from 2.5±0.2 nm/s to 6.9±0.5 nm/s, whereas its Papp,B-A was decreased from 12.1±0.7nm/s to 8.5 ±1.2nm/s. Verapamil increased its Papp,A-B from 2.5±0.2 nm/s to 6.6±0.8 nm/s, and decreased its Papp,B-A from 12.1 ±0.7nm/s to 8.2 ±1.0 nm/s. CONCLUSION. Two dibenzocyclooctadiene lignans from S.chinensis, DSZ and Go A, could increase the transport of R123 by inhibiting the P-gp-mediated efflux. The results suggested that they could potentially increase the absorption of drugs that can act as a P-gp substrate.
语种: 中文
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/114054
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Li N,Hu Y,Yu Y,et al. Schisandra Lignans, Deoxyschizandrin and Gomisin A, Enhanced the Transport of Drugs as a P-gp Substrate by Inhibiting the P-gp-mediated Efflux Effectively[C]. 见:第十八届微粒体与药物氧化国际学术会议. 中国. 2010-5-16.
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