Alopecurone B逆转人乳腺癌细胞MCF-7阿霉素耐药株活性研究

Reversal Effect and Mechanism of Alopecurone B on MCF-7 Adriamycin-Resistant Subline

摘要: 目的研究黄酮化合物Alopecurone B（APB）对人乳腺癌细胞阿霉素耐药株MCF-7/ADR多药耐药的逆转活性及逆转机制。方法人乳腺癌细胞阿霉素耐药株MCF-7/ADR维持在含有250 ng/mL阿霉素的培养基中，使用MTT法、qPCR、Western blot和流式细胞术研究APB对耐药株P-糖蛋白(P-gp)功能和表达的影响。结果 APB能逆转MCF-7/ADR细胞多药耐药，抑制P-gp的功能，下调P-gp基因和蛋白的表达。结论 APB具有强效逆转人乳腺癌细胞MCF-7/ADR多药耐药的效果，其机制涉及对P-gp的调控。

Abstract: OBJECTIVE To study the reversal effect and the mechanism of APB on adriamycin (ADR)-induced multidrug-resistant human breast cancer MCF-7/ADR cells. METHODS ADR-resistant MCF-7 cells were maintained in RPMI-1640 culture medium containing 10%FBS and 250 ng/mL ADR. MTT assay， qPCR， Western blot and flow cytometry were used to determine the inhibitory effect of APB on P-gp levels and function in MCF-7 or MCF-7/ADR cells. RESULTS APB reversed MCF-7/ADR multidrug resistance at the concentration of 10 μmol/L. Treated with 0， 5， 10， 20 μmol/L of ABP， P-gp gene and protein levels were suppressed significantly in a concentration-dependent manner. Furthermore， APB in 10 μmol/L markedly inhibited the function of P-gp. CONCLUSION APB potent reversed the multidrug resistance in MCF-7 ADR-resistant subline. The mechanism referred to P-gp inhibition.