柚皮素对K562/A02细胞MDR1 mRNA/P-gp的影响及机制研究

被引：4

作者：

朱宏平 ^{[1
]}

靳高凤 ^{[1
]}

陈亚军 ^{[1
]}

李新华 ^{[2
]}

张红 ^{[1
]}

黄世博 ^{[1
]}

夏春华 ^{[1
]}

熊玉卿 ^{[1
]}

机构：

[1] 南昌大学临床药理研究所

[2] 南昌大学医院

来源：

中国临床药理学与治疗学 | 2016年 / 21卷 / 11期

关键词：

柚皮素; K562/A02细胞; MDR1 mRNA; P-糖蛋白; NF-κB;

D O I：

暂无

中图分类号：

R285 [中药药理学];

学科分类号：

100806 [中药药理学];

摘要：

目的:研究柚皮素对MDR1 mRNA与P-糖蛋白（P-gp）表达的影响及其分子生物学机制。方法:将不同浓度的柚皮素（50、100、250、500μmol/L）单独或联合阿霉素（5μmol/L）作用于K562/A02细胞48 h,RT-PCR法检测MDR1 mRNA的表达水平,Western-blot法检测P-gp的表达水平,并以NF-κB抑制剂吡咯烷二硫代氨基甲酸盐（PDTC）为对照,比较柚皮素与PDTC间的差异。结果:系列浓度柚皮素作用于K562/A02细胞48 h后能显著抑制MDR1 mRNA(IC50=460.3μmol/L)及P-gp的表达(IC50=286.3μmol/L),抑制作用随浓度的增加而增强;无毒剂量的柚皮素抑制强度与PDTC相近（P>0.05）;经阿霉素诱导后二者抑制效应仍然相仿（P>0.05）。结论:柚皮素明显抑制K562/A02细胞MDR1 mRNA及P-gp的表达,可能与PDTC的作用机制相同,即限制IκB-α磷酸化,阻抑NF-κB的活化,从而抑制MDR1的转录,导致MDR1 mRNA及P-gp的表达量下调,最终使得药物外排转运效应下降。

引用

页码：1209 / 1214

页数：6

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