Ginsenoside Metabolites Inhibit P-Glycoprotein In Vitro and In Situ Using Three Absorption Models
文献类型：期刊论文
| 作者 | Li, Na1,2; Wang, Dandan1,2; Ge, Guangbo1; Wang, Xiuli3; Liu, Yong1; Yang, Ling1 |
| 刊名 | planta medica
 |
| 出版日期 | 2014-03-01 |
| 卷号 | 80期号:4页码:290-296 |
| 关键词 | ginseng ginsenoside intestinal metabolism P-glycoprotein inhibitor |
| 通讯作者 | 杨凌 |
| 英文摘要 | p-glycoprotein, an atp-dependent transporter expressed in the gastrointestinal tract and tumor cells, mediates the efflux transport of multiple drugs. inhibition or induction of p-glycoprotein by herbal ingredients can lead to herb-drug interactions and thus influence the activities of p-glycoprotein substrate drugs. the present study aimed to explore the effect of nine naturally occurring ginsenosides and their intestinal bacterial metabolites on p-glycoprotein-mediated transport. the results showed that three ginsenoside metabolites (ck, ppd, and ppt) formed by intestinal bacteria significantly enhanced rhodamine 123 retention in caco-2 cells, increased the absorptive permeability of rhodamine 123, and decreased the efflux ratio of digoxin in two absorption models, which were comparable to the effects of the known p-glycoprotein inhibitor verapamil. however, the prototype ginsenosides such as rb1, rb2, and re showed no inhibitory effect on p-glycoprotein activity. in situ intestinal perfusion experiments also showed that ck, ppd, and ppt increased the absorption rate constant and permeability coefficient of rhodamine 123. long-term treatment with ck, ppd, and ppt had no effect on p-glycoprotein mrna expression in caco-2 cells. in conclusion, ck, ppd, and ppt are potent p-glycoprotein inhibitors, indicating an unpredictable herb-drug interaction when ginsenosides are coadministered orally with p-glycoprotein substrate drugs. |
| WOS标题词 | science & technology ; life sciences & biomedicine |
| 学科主题 | 物理化学 |
| 类目[WOS] | plant sciences ; chemistry, medicinal ; pharmacology & pharmacy |
| 研究领域[WOS] | plant sciences ; pharmacology & pharmacy |
| 关键词[WOS] | mediated multidrug-resistance ; herb-drug interactions ; caco-2 cell monolayer ; compound k ; 20(s)-ginsenoside rh2 ; intestinal-absorption ; oral bioavailability ; mcf-7/adr cells ; tumor-cells ; red ginseng |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000332395000007 |
| 公开日期 | 2016-05-09 |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/144432]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 作者单位 | 1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China 2.Univ Chinese Acad Sci, Beijing, Peoples R China 3.Dalian Med Univ, Dalian, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Na,Wang, Dandan,Ge, Guangbo,et al. Ginsenoside Metabolites Inhibit P-Glycoprotein In Vitro and In Situ Using Three Absorption Models[J]. planta medica,2014,80(4):290-296. |
| APA | Li, Na,Wang, Dandan,Ge, Guangbo,Wang, Xiuli,Liu, Yong,&Yang, Ling.(2014).Ginsenoside Metabolites Inhibit P-Glycoprotein In Vitro and In Situ Using Three Absorption Models.planta medica,80(4),290-296. |
| MLA | Li, Na,et al."Ginsenoside Metabolites Inhibit P-Glycoprotein In Vitro and In Situ Using Three Absorption Models".planta medica 80.4(2014):290-296. |
入库方式： OAI收割
来源：大连化学物理研究所
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