transportandmetabolismofflavonoidsfromchineseherbalremedyxiaochaihutangacrosshumanintestinalcaco2cellmonolayers1
文献类型：期刊论文
| 作者 | Jieyu DAI; Junling YANG ; Chuan LI
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2008 |
| 卷号 | 29期号:9页码:1086 |
| 关键词 | Caco-2 cell monolayer chemoinformatics transport efflux metabolism flavonoid Xiaochaihu-tang |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To investigate the limiting factors for oral bioavailability of flavonoids derived from the Chinese herbal remedy Xiaochaihu-tang. The investigational flavonoids included baicalin, wogonoside, oroxylin-A 7-O-β-D-glucopyranosiduronide, liquiritin, liquiritin apioside, isoliquiritin, and isoliquiritin apioside, as well as their aglycones baicalein, wogonin, oroxylin-A, liquiritigenin, and isoliquiritigenin. Methods: Caco-2 cell monolayers were used and the apparent permeability both in apical to basolateral and basolateral to apical directions was measured for each investigational compound. Meanwhile, chemoinformatics was carried out to provide insight into the mechanism governing the permeability. In addition, carrier-mediated transport with or without inhibitors, as well as the metabolism by conjugation, was also examined with Caco-2 cell monolayers for the flavonoids. Results: The investigational flavonoid aglycones exhibited favorable membrane permeability, but efficient glucuronidation and/or sulfation by the enterocytes may limit their bioavailability. For the flavonoid glycosides, their poor membrane permeability was found to be caused by high hydrogen-bonding potential. Among the glycosides, oroxylin-A 7-O-β-D-glucopyranosiduronide, isoliquiritin, and isoliquiritin apioside were transported under the mediation of the efflux transporters multidrug resistance-associated protein and/or P-glycoprotein. Conclusion: The limiting factors of oral bioavailability for the flavonoids derived from Xiaochaihu-tang appeared to include poor membrane permeability, significant efflux, and efficient intestinal metabolism by conjugation. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/284037]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Jieyu DAI,Junling YANG,Chuan LI. transportandmetabolismofflavonoidsfromchineseherbalremedyxiaochaihutangacrosshumanintestinalcaco2cellmonolayers1[J]. actapharmacologicasinica,2008,29(9):1086. |
| APA | Jieyu DAI,Junling YANG,&Chuan LI.(2008).transportandmetabolismofflavonoidsfromchineseherbalremedyxiaochaihutangacrosshumanintestinalcaco2cellmonolayers1.actapharmacologicasinica,29(9),1086. |
| MLA | Jieyu DAI,et al."transportandmetabolismofflavonoidsfromchineseherbalremedyxiaochaihutangacrosshumanintestinalcaco2cellmonolayers1".actapharmacologicasinica 29.9(2008):1086. |
入库方式： OAI收割
来源：上海药物研究所
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