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Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein

  • Authors:
    • Hefei Huang
    • Xuenong Zhang
    • Zhixiong Huang
    • Ye Zhang
    • Zhiyong Zhou

  • View Affiliations / Copyright

    Affiliations: Department of Pharmacy, Yichang Central People's Hospital, First Affiliated Hospital of China Three Gorges University, Yichang, Hubei 443002, P.R. China, Department of Pharmacy, Medical College of China Three Gorges University, Yichang, Hubei 443002, P.R. China
    Copyright: © Huang et al. This is an open access article distributed under the terms of Creative Commons Attribution License.
  • Pages: 437-442
    |
    Published online on: December 29, 2016
       https://doi.org/10.3892/etm.2016.4011
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Abstract

Geniposide is a water‑soluble iridoid glucoside with anti‑oxidant and anti‑inflammatory biological functions. It has been indicated that geniposide may increase doxorubicin (DOX) accumulation in drug‑resistant tumor cells. The present study aimed to investigate the resistance‑reversing effect of geniposide in DOX‑resistant cells and assess the underlying mechanisms of its action. The results revealed that geniposide itself weakly inhibited tumor cell growth. Furthermore, geniposide effectively reversed DOX resistance in a dose‑dependent manner in human osteosarcoma DOX‑resistant (MG63/DOX) cells. The action of geniposide was confirmed by increased accumulation of intracellular DOX detected in MG63/DOX cells. Notably, geniposide enhanced the efficacy of DOX against MG63/DOX cancer cell‑derived xenografts in nude mice. To study the mechanism, intracellular accumulation of rhodamine 123 was measured using flow cytometry. At concentrations that reversed multidrug resistance (MDR), geniposide significantly downregulated P‑glycoprotein (P‑gp) expression. Therefore, geniposide reverses P‑gp‑mediated MDR by reducing the expression of P‑gp and its transport function. The present study therefore indicated that geniposide may be administered in combination with conventional anti‑neoplastic drugs to prevent MDR.

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Copy and paste a formatted citation
Spandidos Publications style
Huang H, Zhang X, Huang Z, Zhang Y and Zhou Z: Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein. Exp Ther Med 13: 437-442, 2017.
APA
Huang, H., Zhang, X., Huang, Z., Zhang, Y., & Zhou, Z. (2017). Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein. Experimental and Therapeutic Medicine, 13, 437-442. https://doi.org/10.3892/etm.2016.4011
MLA
Huang, H., Zhang, X., Huang, Z., Zhang, Y., Zhou, Z."Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein". Experimental and Therapeutic Medicine 13.2 (2017): 437-442.
Chicago
Huang, H., Zhang, X., Huang, Z., Zhang, Y., Zhou, Z."Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein". Experimental and Therapeutic Medicine 13, no. 2 (2017): 437-442. https://doi.org/10.3892/etm.2016.4011
Copy and paste a formatted citation
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Spandidos Publications style
Huang H, Zhang X, Huang Z, Zhang Y and Zhou Z: Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein. Exp Ther Med 13: 437-442, 2017.
APA
Huang, H., Zhang, X., Huang, Z., Zhang, Y., & Zhou, Z. (2017). Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein. Experimental and Therapeutic Medicine, 13, 437-442. https://doi.org/10.3892/etm.2016.4011
MLA
Huang, H., Zhang, X., Huang, Z., Zhang, Y., Zhou, Z."Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein". Experimental and Therapeutic Medicine 13.2 (2017): 437-442.
Chicago
Huang, H., Zhang, X., Huang, Z., Zhang, Y., Zhou, Z."Geniposide reverses multidrug resistance in vitro and in vivo by inhibiting the efflux function and expression of P‑glycoprotein". Experimental and Therapeutic Medicine 13, no. 2 (2017): 437-442. https://doi.org/10.3892/etm.2016.4011
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