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The Membrane Transport of Flavonoids from Crossostephium chinense across the Caco-2 Monolayer
Wang, Ying1; Wu, Qi1; Yang, Xiu-Wei1; Yang, Xiaoda2; Wang, Kui1,2
关键词Flavonoids Selagin Caco-2 Efflux Mrp
刊名BIOPHARMACEUTICS & DRUG DISPOSITION
2011
DOI10.1002/bdd.735
32期:1页:16-24
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]CELL LINE CACO-2 ; MULTIDRUG-RESISTANCE PROTEIN-1 ; IN-VITRO ; INTESTINAL-ABSORPTION ; DRUG-RESISTANCE ; METABOLISM ; EFFLUX ; SPECIFICITY ; QUERCETIN ; VIVO
英文摘要

The permeation and efflux of six polysubstituted flavonoids isolated from Crossostephium chinense, a Chinese traditional and herbal drug for the treatment of diabetes, were investigated using the Caco-2 cell monolayer. The six flavonoids (selagin, apometzgerin, tricetin-3′,4′,5′- trimethylether, quercetagetin-3,6,7-trimethylether, hispidulin and quercetagetin) sharing a similar parent skeleton structure with varied substituents in the heterocyclic ring B were selected for the study. Quercetagetin exhibited a low bi-directional permeability comparable to that of atenolol, suggesting a paracellular diffusion mechanism. The remaining compounds exhibited time- and concentration-dependent permeation with apparent permeability coefficient (P(app)) values in the range 10(-6)-10(-5) cm/s, suggesting transcellular diffusion pathways. Selagin exhibited significantly larger basolateral to apical P(app) than that of the reverse direction, suggesting the existence of efflux mechanisms. ATP-depletion and probenecid pretreatment led to a significant inhibition of the efflux of selagin, whereas verapamil had no effect on the basolateral to apical transport of selagin, suggesting that multidrug resistance proteins (MRPs) and not P-glycoprotein play a role in the intestinal efflux of selagin. Based on present and previous results, the structure-permeation relationship and the role of MRPs in mediating the efflux of flavonoids are discussed. Experimental results in this study provide useful information for pharmacological applications of the flavonoids from C. chinense. Copyright (C) 2010 John Wiley & Sons, Ltd.

语种英语
WOS记录号WOS:000285392400002
项目编号2009ZX09502-006 ; Z0004105040311
资助机构Major New Medicine Project in Mega-projects of Science Research of China ; Beijing Municipal Special purpose Science Foundation of China
引用统计
被引频次:10[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/56668
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学临床肿瘤学院_内镜中心
作者单位1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Wang, Ying,Wu, Qi,Yang, Xiu-Wei,et al. The Membrane Transport of Flavonoids from Crossostephium chinense across the Caco-2 Monolayer[J]. BIOPHARMACEUTICS & DRUG DISPOSITION,2011,32(1):16-24.
APA Wang, Ying,Wu, Qi,Yang, Xiu-Wei,Yang, Xiaoda,&Wang, Kui.(2011).The Membrane Transport of Flavonoids from Crossostephium chinense across the Caco-2 Monolayer.BIOPHARMACEUTICS & DRUG DISPOSITION,32(1),16-24.
MLA Wang, Ying,et al."The Membrane Transport of Flavonoids from Crossostephium chinense across the Caco-2 Monolayer".BIOPHARMACEUTICS & DRUG DISPOSITION 32.1(2011):16-24.
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