植物多酚类化合物逆转肿瘤多药耐药的筛选

Studies of several polyphenolses on multidrug resistances

目的:研究槲皮素、小檗碱、黄芩甙、芦丁、牛蒡子甙逆转肿瘤多药耐药(MDR)的作用及机制。方法:MTT法检测槲皮素、小檗碱、黄芩甙、芦丁、牛蒡子甙的细胞毒性作用及耐药逆转效果。流式细胞术检测槲皮素作用前后MCF-7/ADR细胞P-糖蛋白(Pgp)表达的变化。结果:小檗碱能显著抑制MCF-7/ADR及MCF-7细胞的增殖,槲皮素、黄岑甙、芦丁能显著抑制MCF-7细胞增殖。槲皮素能提高MCF-7/ADR细胞对阿霉素的敏感性,逆转倍数为3.19,并能降低MCF-7/ADR细胞Pgp的表达。结论:槲皮素能够部分逆转多药耐药,其逆转机制与下调Pgp表达有关。

Objective:To investigate the activity and mechanism of quercetin,berberine,bacalin,rutin and arctiin in the reversal of tumor multidrug resistance(MDR).Methods:The cytotoxicity of quercetin,berberine,bacalin,rutin,arctiin and MDR reversion to MCF-7and MCF-7/ADR cells were de-termined with MTT assay.The expression of P-glycoprotein(Pgp)in MCF-7/ADR cells after72h of expo-sure to quercetin were observed with Flow cytometry analysis.Results:Berberine could significantly inhibit the proliferation of MCF-7and MCF-7/ADR cells.Quercetin,bacalin,rutin and arctiin could all inhibit the proliferation of MCF-7cells significantly.Quercetin could obviously enhance the sensitivity of MCF-7/ADR cells to adrimary,fold reversal(FR)was3.19.Positivity of P-glycoprotein was decreased after exposed to quercetin.Conclusion:Quercetin can partially reverse MDR in MCF-7/ADR cells,and its reversal mecha-nism was related with the decrease of the expression of P-glycoprotein.