诺福素对MCF-7人乳腺癌细胞的体内外抗癌药效学研究  

Anti-cancer Evaluation of Epothilone B on Human Breast Cancer MCF-7

作　　者：于春芳[1] 杨德宣[1] 李琳娜[1] 张庆林[1] 袁守军[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《解放军药学学报》2011年第4期303-306,共4页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的研究评价诺福素在体内体外对MCF-7人乳腺癌细胞的生长抑制作用。方法按照抗癌药物临床前药效学评价原则,体外评价试验用MTT法,体内评价通过观察受试药物对MCF-7裸鼠移植瘤生长的影响,并与阳性药紫杉醇进行比较。结果两批体外MTT法显示,诺福素抑制MCF-7细胞生长的半效抑制浓度分别为1.7762 nmol/L和0.8578 nmol/L,实际检测的最大抑制率分别为72.24%、86.94%。而阳性药紫杉醇的半效抑制浓度分别为2.0627、1.9807 nmol/L,实际检测的紫杉醇最大抑制率分别为70.98%、86.86%。体内实验结果显示,诺福素可对人乳腺癌MCF-7裸鼠移植瘤的生长有较强的抑制效应,呈现剂量依赖性特点;第1次结果显示,诺福素单次给药8、6、4、2 mg/kg组的抑瘤率分别为85.8%、85.1%、83.7%、48.3%。第2次结果表明,诺福素单次给药6、4、2 mg/kg组的抑瘤率分别为86.9%、77.8%、37.5%。整个实验过程中,个别动物死亡,体质量一过性降低。阳性药物紫杉醇15 mg/kg多次给药的抑瘤率分别为98.9%、97.3%。结论诺福素对人乳腺癌MCF-7细胞在体内外生长均有较强的抑制效应。Objective To evaluate the anti-cancer activity of Epothilone B on human breast cancer MCF-7 both in vivo and in vitro.Methods According to Principles of Preclinical Evaluation,the anti-cancer activity of Epothilone B in vitro was inspected by MTT method,while the activity in vivo was evaluated by observing the growth inhibition of MCF-7 xenograft tumors.Results The replicated MTT inspection showed that the IC50 of Epothilone B was both 1.7762 nmol/L and 0.8578 nmol/L.The maximum growth inhibition rate was 72.24% and 86.94%.The IC50 of paclitaxel was 2.0627 nmol/L and 1.9807 nmol/L respectively and the maximum inhibition rate was 70.98% and 86.86% respectively.According to the observation of MCF-7 xenograft tumors,Epothilone B produced dose-dependent inhibition.The result of the first experiment showed the inhibition rate of Epothilone B with at a single dose of 8,6,4 mg/kg and 2 mg/kg was 85.8%,85.1%,83.7% and 48.3% respectively.The finding of the second experiment was that the inhibition rate of Epothilone B at a single dose of 6,4 mg/kg and 2 mg/kg was 86.9%,77.8% and 37.5% respectively.During the observation,a few of the nude mice died and had a transient weight reduction.Compared with Epothilone B,the inhibition rate of paclitaxel at a multiple dose of 15 mg/kg was 98.9% and 97.3%.Conclusion Epothilone B can efficiently inhibit the growth of human breast cancer MCF-7 both in vivo and in vitro.

关 键 词：诺福素 MCF-7 乳腺癌 抗瘤活性 

分 类 号：R965[医药卫生—药理学]