Transport and metabolism of flavonoids from Chinese herbal remedy Xiaochaihu-tang across human intestinal Caco-2 cell monolayers
文献类型：期刊论文
| 作者 | Dai, Jie-Yu; Yang, Jun-ling ; Li, Chuan
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2008-09 |
| 卷号 | 29期号:9页码:1086-1093 |
| 关键词 | Caco-2 cell monolayer chemoinformatics transport efflux metabolism flavonoid Xiaochaihu-tang |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00850.x |
| 文献子类 | Article |
| 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 7-0-beta-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-beta-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. |
| WOS关键词 | SHOSAIKO-TO ; HUMAN URINE ; MASS-SPECTROMETRY ; DRUG ABSORPTION ; LINE CACO-2 ; DAISAIKO-TO ; PERMEABILITY ; BAICALEIN ; IDENTIFICATION ; INHIBITION |
| 资助项目 | National Natural Science Foundation of China[30271596] ; Chinese Ministry of Science and Technology[2004CB518902] ; Chinese Ministry of Science and Technology[2005CB523403] ; Science & Technology Commission of Shanghai Municipality[O1DJ19008] ; Science & Technology Commission of Shanghai Municipality[04DZ19215] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3330708 |
| WOS记录号 | WOS:000259038000012 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272814]  |
| 专题 | 上海药物代谢研究中心 科研与新药推进处 |
| 通讯作者 | Li, Chuan |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Ctr DMPK Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dai, Jie-Yu,Yang, Jun-ling,Li, Chuan. Transport and metabolism of flavonoids from Chinese herbal remedy Xiaochaihu-tang across human intestinal Caco-2 cell monolayers[J]. ACTA PHARMACOLOGICA SINICA,2008,29(9):1086-1093. |
| APA | Dai, Jie-Yu,Yang, Jun-ling,&Li, Chuan.(2008).Transport and metabolism of flavonoids from Chinese herbal remedy Xiaochaihu-tang across human intestinal Caco-2 cell monolayers.ACTA PHARMACOLOGICA SINICA,29(9),1086-1093. |
| MLA | Dai, Jie-Yu,et al."Transport and metabolism of flavonoids from Chinese herbal remedy Xiaochaihu-tang across human intestinal Caco-2 cell monolayers".ACTA PHARMACOLOGICA SINICA 29.9(2008):1086-1093. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。