Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function

Journal of Pharmaceutical Sciences Volume 96 Issue 1 Page 223-233 published_at 2006
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Title ( eng )
Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function
Creator
Patanasethanont Denpong
Nagai Junya
Yumoto Ryoko
Murakami Teruo
Sutthanut Khaetthareeya
Sripanidkulchai Bung-Orn
Yenjai Chavi
Source Title
Journal of Pharmaceutical Sciences
Volume 96
Issue 1
Start Page 223
End Page 233
Abstract
The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from Kaempferia parviflora rhizome significantly increased the accumulation of rhodamine 123 and daunorubicin, P-gp substrates, in LLC-GA5-COL150 cells, but not in LLC-PK1 cells. The aqueous extract also increased the accumulation in LLC-GA5-COL150 cells with lower potency than the ethanol extract. The effects of flavone derivatives isolated from the rhizome of Kaempferia parviflora on P-gp function were examined. Among six flavones tested, 3,5,7,3',4'-pentamethoxyflavone most potently increased the accumulation of rhodamine 123 and daunorubicin in LLC-GA5-COL150 cells in a concentration-dependent manner. In addition, 5,7-dimethoxyflavone to lesser degree increased rhodamine 123 accumulation in LLC-GA5-COL150 cells. In contrast, the other four flavone derivatives had no significant effect on the accumulation of rhodamine 123 in LLC-GA5-COL150 cells in a concentration range tested. These results indicate that extracts and flavone derivatives from the rhizome of Kaempferia parviflora can inhibit P-gp function, which may be useful for overcoming P-gp-mediated multidrug resistance and improving the oral bioavailability of anticancer agents.
Keywords
Multidrug resistance
P-glycoprotein
Cancer chemotherapy
Bioavailability
Cell culture
NDC
Medical sciences [ 490 ]
Language
eng
Resource Type journal article
Publisher
John Wiley & Sons Inc
Date of Issued 2006
Rights
Copyright (c) 2006 John Wiley & Sons, Inc.
Publish Type Author’s Original
Access Rights open access
Source Identifier
[ISSN] 0022-3549
[DOI] 10.1002/jps.20769
[PMID] 17031860
[NCID] AA00704450
[DOI] http://dx.doi.org/10.1002/jps.20769