Ergosterol reverses multidrug resistance in SGC7901/Adr cells

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Published on: November 15, 2013

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Xiaoxiao Hu, Danhong Jiang, Farong Li

    Die Pharmazie
    |May 27, 2014
    PubMed

    Insights

    Ergosterol (Erg) reverses multidrug resistance (MDR) in cancer cells by inhibiting P-glycoprotein (P-gp) expression. This study shows Ergosterol is a promising compound for overcoming chemotherapy resistance.

    Area of Science:

    • Oncology
    • Pharmacology
    • Molecular Biology

    Background:

    • Multidrug resistance (MDR) significantly hinders effective cancer chemotherapy.
    • Elevated P-glycoprotein (P-gp) expression is a primary mechanism driving MDR in tumor cells.
    • P-gp actively effluxes anticancer drugs, reducing their intracellular concentration and efficacy.

    Purpose of the Study:

    • To investigate the potential of ergosterol (Erg) in reversing adriamycin resistance in SGC7901/Adr cells.
    • To elucidate the underlying molecular mechanisms by which ergosterol affects P-gp expression and function.
    • To evaluate ergosterol as a potential lead compound for overcoming MDR in cancer treatment.

    Main Methods:

    • Utilized SGC7901/Adr cells, a model for adriamycin-resistant cancer cells.
    • Assessed the reversal effect of ergosterol at varying concentrations (1 microM and 5 microM) on adriamycin resistance.
    • Measured intracellular accumulation of adriamycin and Rhodamine 123 (Rh123) to evaluate P-gp activity.
    • Investigated the effect of ergosterol on MDR1 gene transcription and P-gp protein expression.

    Main Results:

    • Ergosterol significantly reversed adriamycin resistance in SGC7901/Adr cells, with fold reversals of 4.84 at 1 microM and 3.92 at 5 microM.
    • Ergosterol treatment led to increased intracellular accumulation of adriamycin and Rh123 in resistant cells.
    • Ergosterol inhibited the transcription of the MDR1 gene, consequently down-regulating P-gp expression.

    Conclusions:

    • Ergosterol effectively reverses multidrug resistance in SGC7901/Adr cells.
    • The mechanism involves the inhibition of MDR1 gene transcription and down-regulation of P-gp expression.
    • Ergosterol shows promise as a lead compound for developing novel strategies to combat cancer MDR.

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