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

Patanasethanont Denpong

Nagai Junya

Yumoto Ryoko

Murakami Teruo

Sutthanut Khaetthareeya

Sripanidkulchai Bung-Orn

Yenjai Chavi

Takano Mikihisa

Journal of Pharmaceutical Sciences

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.

Multidrug resistance

P-glycoprotein

Cancer chemotherapy

Bioavailability

Cell culture

医学 [ 490 ]

英語

John Wiley & Sons Inc

Copyright (c) 2006 John Wiley & Sons, Inc.

[ISSN] 0022-3549

[DOI] 10.1002/jps.20769

[PMID] 17031860

[NCID] AA00704450

[DOI] http://dx.doi.org/10.1002/jps.20769