Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function.
Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function.
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DOI：
10.1002/jps.20769
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发表时间：
2007
影响因子：
3.8
通讯作者：
Denpong Patanasethanont;J. Nagai;R. Yumoto;T. Murakami;Khaetthareeya Sutthanut;B. Sripanidkulchai;C. Yenjai;M. Takano
中科院分区：
文献类型：
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作者：
Denpong Patanasethanont;J. Nagai;R. Yumoto;T. Murakami;Khaetthareeya Sutthanut;B. Sripanidkulchai;C. Yenjai;M. Takano
本研究的目的是检查提取物和黄酮衍生物从山奈的根茎P-糖蛋白（P-gp）介导的运输在LLC-GA 5-COL 150，一个转染细胞系的猪肾上皮细胞株LLC-PK 1与人MDR 1 cDNA的影响。从山柰根茎获得的乙醇提取物显着增加罗丹明123和柔红霉素，P-gp底物，在LLC-GA 5-COL 150细胞中的积累，但在LLC-PK 1细胞中不。水提取物还增加了LLC-GA 5-COL 150细胞中的蓄积，效力低于乙醇提取物。本文研究了从小花山奈根茎中提取的黄酮类化合物对P-糖蛋白功能的影响。在所测试的六种黄酮中，3，5，7，3 '，4'-五甲氧基黄酮以浓度依赖性方式最有效地增加LLC-GA 5-COL 150细胞中罗丹明123和柔红霉素的积累。此外，5，7-二甲氧基黄酮在较小程度上增加了LLC-GA 5-COL 150细胞中罗丹明123的积累。相比之下，其他四种黄酮衍生物在测试的浓度范围内对LLC-GA 5-COL 150细胞中罗丹明123的积累没有显著影响。这些结果表明，山柰根茎提取物和黄酮类化合物具有抑制P-gp功能的作用，可能有助于克服P-gp介导的多药耐药，提高抗癌药物的口服生物利用度。
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.