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学科主题物理化学
Ginsenoside Metabolites Inhibit P-Glycoprotein In Vitro and In Situ Using Three Absorption Models
Li, Na1,2; Wang, Dandan1,2; Ge, Guangbo1; Wang, Xiuli3; Liu, Yong1; Yang, Ling1; Yang L(杨凌)
关键词Ginseng Ginsenoside Intestinal Metabolism P-glycoprotein Inhibitor
刊名PLANTA MEDICA
2014-03-01
DOI10.1055/s-0033-1360334
80期:4页:290-296
收录类别SCI
文章类型Article
WOS标题词Science & Technology ; Life Sciences & Biomedicine
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
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.
语种英语
WOS记录号WOS:000332395000007
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/144432
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
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
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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.,...&杨凌.(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.
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