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学科主题: 药学
题名:
Studies of intestinal permeability of 36 flavonoids using Caco-2 cell monolayer model
作者: 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
发表日期: 2009-02-09
DOI: 10.1016/j.ijpharm.2008.09.023
卷: 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
所属项目编号: 2002AA2Z343C ; 2004AA2Z3783 ; 2006BA106A 01-02 ; Z0004105040311
项目资助者: National High Technology Research and Development Program of China ; Beijing Municipal Special-purpose Science Foundation of China
WOS记录号: WOS:000263458600008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58254
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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

Recommended Citation:
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.
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