多肽Melittin-K1逆转人肝癌耐药细胞株BEL-7402/5-FU耐药性的研究  

Melittin-K1 reverses multidrug resistance of human hepatocellular carcinoma BEL-7402/5-FU cells

作　　者：董健[1,2] 赵诗迪 陈婷瑶 柯梦云 吕毅[1] Dong Jian;Zhao Shidi;Chen Tingyao;Ke Mengyun;Lyu Yi(National Local Joint Engineering Research Center for Precision Surgery&Regenerative Medicine,Shanxi Provincial Center for Regenerative Medicine and Surgical Engineering,First Affiliated Hospital of Xi′an Jiaotong University,Xi′an 710061,China;Department of Vascular Surgery,First Affiliated Hospital of Xi′an Jiaotong University,Xi′an 710061,China;School of Life Science and Technology,China Pharmaceutical University,Nanjing 210009,China)

机构地区：[1]西安交通大学第一附属医院精准外科与再生医学国家地方联合工程研究中心,陕西省再生医学与外科工程研究中心,710061 [2]西安交通大学第一附属医院血管外科,710061 [3]中国药科大学生命科学与技术学院,南京210009

出　　处：《中华普通外科杂志》2020年第11期882-886,共5页Chinese Journal of General Surgery

摘　　要：目的探讨蜂毒肽Melittin突变体Melittin-K1逆转人肝癌耐药细胞株BEL-7402/5-FU多药耐药性的作用及机制。方法采用CCK-8法检测细胞活率评价Melittin-K1对BEL-7402/5-FU细胞生长的影响以及Melittin-K1能否逆转BEL-7402/5-FU细胞的耐药性。实时荧光定量PCR技术对Melittin-K1处理后BEL-7402/5-FU细胞多药耐药基因MDR1表达的改变进行测定。流式细胞术检测细胞表面P-糖蛋白(P-glycoprotein,P-gp)的表达以及细胞内罗丹明-123的蓄积水平评价Melittin-K1对P-gp蛋白表达及其功能的影响。结果细胞体外增殖实验结果表明,Melittin-K1显著抑制BEL-7402/5-FU细胞生长。Melittin-K1下调BEL-7402/5-FU细胞MDR1基因的表达并抑制细胞膜表面P-gp的表达水平及功能。结论新型多肽Melittin-K1具有逆转肝癌耐药细胞株BEL-7402/5-FU多药耐药性的作用。Objective To investigate the mechanism by which Melittin-K1 reverses multidrug resistance of BEL-7402/5-FU cells.Methods CCK-8 assay was used to evaluate the effect of Melittin-K1 on the growth of BEL-7402/5-FU cells and to explore whether Melittin-K1 could reverse the drug resistance of BEL-7402/5-FU cells.The expression of MDR1 mRNA level was detected by real-time fluorescence quantitative PCR assay.The flow cytometry was used to measure the expression of P-glycoprotein(P-gp)on the cell membrane surface and the accumulation of rhodamine-123 in cells.Results Melittin-K1 significantly inhibited the growth of BEL-7402/5-FU cells in vitro in a time and dose-dependent manner.Melittin-K1 suppressed the level of MDR1 mRNA and inhibited the surface expression and function of P-gp in BEL-7402/5-FU cells.Conclusions Melittin-K1,a novel peptide,exhibited the activity of reversing multidrug resistance of liver cancer cells.

关 键 词：抗菌肽类 化学疗法 辅助 多药耐药 P-糖蛋白 

分 类 号：R96[医药卫生—药理学]