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

✍ Scribed by Denpong Patanasethanont; Junya Nagai; Ryoko Yumoto; Teruo Murakami; Khaetthareeya Sutthanut; Bung-orn Sripanidkulchai; Chavi Yenjai; Mikihisa Takano

• Book ID: 102397084
• Publisher: John Wiley and Sons
• Year: 2007
• Tongue: English
• Weight: 203 KB
• Volume: 96
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.20769

✦ Synopsis

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-PK 1 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-PK 1 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 0 ,4 0 -pentamethoxyflavone most potently increased the accumulation of rhodamine 123 and daunorubicin in LLC-GA5-COL150 cells in a concentrationdependent 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.