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与HERG相关的红霉素和司帕沙星联合抗肿瘤作用
引用本文:弓建华,尚伯杨,甄永苏. 与HERG相关的红霉素和司帕沙星联合抗肿瘤作用[J]. 医学研究杂志, 2011, 40(1): 54-59
作者姓名:弓建华  尚伯杨  甄永苏
作者单位:北京协和医学院/中国医学科学院医药生物技术研究所肿瘤室,100050
基金项目:国家重点基础研究发展计划(“973”计划)基金资助项目(2004CB518706)
摘    要:目的探讨与钾离子通道HERG相关的药物在肿瘤治疗中的靶向调节作用。方法采用Western blot检测相关蛋白的表达水平。采用MTT法观察SPFX-ERM对细胞增生的抑制作用;采用两药相互作用指数CDI评价是否存在协同作用。采用流式细胞术检测细胞周期。建立小鼠移植肝癌模型,观察连续灌胃给予SPFX-ERM的抑瘤效果。结果 HERG蛋白在人结肠癌细胞HCT116和HT-29中均高表达。MERG蛋白在小鼠肝癌H22细胞中也高表达。SPFX-ERM能明显抑制人结肠癌HCT116和HT-29细胞的增生,并且细胞对两药联合的敏感性要显著高于单用SPFX或ERM。高剂量的SPFX-ERM能抑制HERG蛋白的表达。SPFX-ERM可以引起G2期细胞阻滞。动物体内实验表明,SPFX-ERM能明显抑制小鼠移植性肝癌H22在体内的生长,协同作用显著,其CDI值均在0.7以下。结论联合SPFX-ERM作为与HERG有关的调节剂有显著的抗肿瘤作用。

关 键 词:HERG  司帕沙星  红霉素  抗肿瘤作用
收稿时间:2010-08-26
修稿时间:2010-12-05

Antitumor Efficacy of Erythromycin Combined with Sparfloxacin Related HERG
Gong Jianhua,Shang Boyang,Zhen Yongsu. Antitumor Efficacy of Erythromycin Combined with Sparfloxacin Related HERG[J]. Journal of Medical Research, 2011, 40(1): 54-59
Authors:Gong Jianhua  Shang Boyang  Zhen Yongsu
Affiliation:Gong Jianhua,Shang Boyang,Zhen Yongsu.Department of Oncology,Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China
Abstract:Objective To study the targeted modulation of the drugs targeted ion channel-HERG.Methods The protein expression level was detected by Western blot.MTT assay was used to detect the cytotoxicity.Flow cytometry was used to analyze cell cycle distribution.Transplantable murine hepatoma 22 model was used to evaluate the antitumor activity of drugs in vivo.Results HERG and MERG proteins were over-expressed in human colorectal cancer cells and mouse hepatoma cells respectively.The colon cancer cells were more sen...
Keywords:HERG  Sparfloxacin  Erythromycin  Antitumor efficacy  
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