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Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model
Tian, Xiao-Juan2; Yang, Xiu-Wei2; Yang, Xiaoda1; Wang, Kui2
关键词Flavonoids Caco-2 cell monolayer Permeability Structure-permeability relationship
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2009-02-09
DOI10.1016/j.ijpharm.2008.09.023
367期:1-2页:58-64
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]DRUG PERMEABILITY ; LINE CACO-2 ; QUERCETIN 4&prime ; -BETA-GLUCOSIDE ; TRANSPORT ; EFFLUX ; ISOFLAVONOIDS ; ANTIOXIDANT ; ABSORPTION ; PHENOTYPE ; SYSTEM
英文摘要

To investigate the structure-permeability relationship of dietary/nutriceutic flavonoids, the transepithelial transport and cellular uptake of 36 flavonoids (including flavones, flavonols, dihydroflavones. dihydroflavonols, isoflavones, chalcones, flavanes, flavanols, methylated and glycosidic derivatives) were investigated using the Caco-2 cell monolayer. The apparent permeability coefficients (P,,pp) of the flavonoids were calculated from bilateral transport assays in the Transwell system with flavonoid determination using a high performance liquid chromatography (HPLC) coupled with a UV detector. The most flavonoids exhibited concentration-independent P-app values and a ratio of 0.5-1.8 for P-app (AB to BL)/P-app BL to AB, suggesting passive diffusion pathways. However, certain flavonoids e.g. morin and some flavonoid glycosides may involve the efflux mechanisms. For isoflavones, flavones, and dihydroflavones, the oil/water partition coefficients (additionally modified by the number and position of the three hydroxyl groups) was the key determinant for Caco-2 cell permeation. However, the permeability of flavonols is more complex with their structure possibly related to their high rate of cell accumulation. Overall, the parental skeleton structure, the number and position of free hydroxyl groups, accumulation and efflux in Caco-2 cell play the key roles in the transport of flavonoids across Caco-2 cell monolayer. (C) 2008 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000263458600008
项目编号2002AA2Z343C ; 2004AA2Z3783 ; 2006BA106A 01-02 ; Z0004105040311
资助机构National High Technology Research and Development Program of China ; Beijing Municipal Special-purpose Science Foundation of China
引用统计
被引频次:105[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/400002259/58254
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Tian, Xiao-Juan,Yang, Xiu-Wei,Yang, Xiaoda,et al. Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2009,367(1-2):58-64.
APA Tian, Xiao-Juan,Yang, Xiu-Wei,Yang, Xiaoda,&Wang, Kui.(2009).Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model.INTERNATIONAL JOURNAL OF PHARMACEUTICS,367(1-2),58-64.
MLA Tian, Xiao-Juan,et al."Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model".INTERNATIONAL JOURNAL OF PHARMACEUTICS 367.1-2(2009):58-64.
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