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In this study, oroxylin A showed strong reversal potency in BEL7402/5-FU cells and the reversal fold (RF) reached 4.69. Simultaneously, rhodamine-123 accumulation assay and flow cytometry analysis demonstrated oroxylin A could increase drug accumulation. When combined with oroxylin A, 5-FU showed inducing apoptosis effect more seriously in DAPI staining experiment. Moreover, the mRNA and protein expression of multi-drug resistance gene (MDR1) were also decreased by oroxylin A. Further experiments exhibited that oroxylin A can downregulate P-gp expression through inhibiting nuclear factor-κB (NF-κB) signaling pathway, which might be the mechanism of reversal resistance of oroxylin A. In summary, oroxylin A could be a good candidate for the development of new MDR reversal agent and its reversal mechanism probably due to the suppression of P-gp expression via inhibiting NF-κB signaling pathway. Copyright © 2011 Wiley Periodicals, Inc.

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Hui-Ying Yang, Li Zhao, Zhen Yang, Qing Zhao, Lei Qiang, Jun Ha, Zhi-Yu Li, Qi-Dong You, Qing-Long Guo. Oroxylin A reverses multi-drug resistance of human hepatoma BEL7402/5-FU cells via downregulation of P-glycoprotein expression by inhibiting NF-κB signaling pathway. Molecular carcinogenesis. 2012 Feb;51(2):185-95

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PMID: 21557331

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