DICP OpenIR
学科主题物理化学
Schisandra Lignans, Deoxyschizandrin and Gomisin A, Enhanced the Transport of Drugs as a P-gp Substrate by Inhibiting the P-gp-mediated Efflux Effectively
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
2010-05-16
会议地点中国
页码304/1
部门归属十八室
主办者中国医学科学院
英文摘要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
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/114054
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
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],2010:304/1.
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