| Inhibitory effects of ginsenosides and their hydrolyzed metabolites on daunorubicin transport in KB-C2 cells. | |
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MedLine Citation:
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PMID: 17917277 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We studied the effects of ginsenosides and their metabolites on daunorubicin transport in multidrug-resistant P-glycoprotein (P-gp)-overexpressing KB-C2 cells. Ginsenoside Rg1, which is a protopanaxatriol-type ginseng saponin, did not have any effects on the accumulation of P-gp substrate daunorubicin. On the other hand, its metabolite M4, which has no sugar moiety, increased the accumulation 3.6-fold at 5 microM. Metabolites of protoanaxadiol-type saponin M1 and M12 also increased accumulation, but the effects were less than that of M4. The findings showed larger effects of metabolites without glucose moieties. Analysis of verapamil-stimulated ATPase activity in membrane vesicles expressing human P-gp suggested that the increased daunorubicin accumulation by M4 was at least partly due to ATPase inhibition of P-gp. |
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Authors:
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Shuji Kitagawa; Tomoharu Takahashi; Tomohiro Nabekura; Eiichi Tachikawa; Hideo Hasegawa |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biological & pharmaceutical bulletin Volume: 30 ISSN: 0918-6158 ISO Abbreviation: Biol. Pharm. Bull. Publication Date: 2007 Oct |
Date Detail:
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Created Date: 2007-10-05 Completed Date: 2007-11-06 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9311984 Medline TA: Biol Pharm Bull Country: Japan |
Other Details:
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Languages: eng Pagination: 1979-81 Citation Subset: IM |
Affiliation:
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Kobe Pharmaceutical University, Kobe, Japan. kitagawa@niigata-pharm.ac.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adenosine Triphosphatases
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metabolism Antibiotics, Antineoplastic / metabolism* Biological Transport, Active / drug effects Calcium Channel Blockers / pharmacology Cell Membrane / drug effects, enzymology Colchicine / pharmacology Cyclosporine / pharmacology Daunorubicin / metabolism* Drug Resistance, Neoplasm / drug effects Ginsenosides / chemistry, pharmacokinetics*, pharmacology* Humans Hydrolysis KB Cells Multidrug Resistance-Associated Proteins / genetics P-Glycoprotein / biosynthesis, genetics, physiology Structure-Activity Relationship Triterpenes / pharmacology Verapamil / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Antibiotics, Antineoplastic; 0/Calcium Channel Blockers; 0/Ginsenosides; 0/Multidrug Resistance-Associated Proteins; 0/P-Glycoprotein; 0/Triterpenes; 0/multidrug resistance-associated protein 1; 20830-81-3/Daunorubicin; 52-53-9/Verapamil; 545-22-2/dammarane; 59865-13-3/Cyclosporine; 64-86-8/Colchicine; EC 3.6.1.-/Adenosine Triphosphatases |
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