RRC ID 42787
著者 Patanasethanont D, Nagai J, Yumoto R, Murakami T, Sutthanut K, Sripanidkulchai BO, Yenjai C, Takano M.
タイトル Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function.
ジャーナル J Pharm Sci
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.
巻・号 96(1)
ページ 223-33
公開日 2007-1-1
DOI 10.1002/jps.20769
PII S0022-3549(16)32155-4
PMID 17031860
MeSH ATP Binding Cassette Transporter, Subfamily B, Member 1 / drug effects* ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism Animals Antibiotics, Antineoplastic / metabolism Daunorubicin / metabolism Dose-Response Relationship, Drug Drug Resistance, Neoplasm / drug effects* Ethanol / chemistry Flavones / isolation & purification Flavones / pharmacology* Flavonoids / pharmacology Fluorescent Dyes / metabolism Humans LLC-PK1 Cells Plant Extracts / chemistry Plant Extracts / pharmacology Rhizome Rhodamine 123 / metabolism Solvents / chemistry Swine Time Factors Transfection Water / chemistry Zingiberaceae*
IF 2.997
引用数 55
WOS 分野 CHEMISTRY, MEDICINAL PHARMACOLOGY & PHARMACY CHEMISTRY, MULTIDISCIPLINARY
リソース情報
ヒト・動物細胞 LLC-GA5-CoL150(RCB0871)