聚乙二醇-伊立替康对裸鼠人乳腺癌移瘤模型的药效学研究

发布时间：2018-03-28 20:23

  本文选题：聚乙二醇-伊立替康　切入点：拓扑异构酶Ⅰ抑制剂　出处：《药物分析杂志》2017年01期

【摘要】：目的:评价长效拓扑异构酶Ⅰ抑制剂聚乙二醇-伊立替康(YP-pegol)的体内抗肿瘤活性。方法:将体外传代培养后的人乳腺癌MCF-7细胞接种到裸鼠右前肢腋部皮下,建立裸鼠人乳腺癌移植瘤模型。待肿瘤体积增长至满足试验要求后,将裸鼠按肿瘤体积随机分为6个组即4个YP-pegol剂量组,1个溶媒对照组和1个阳性对照组。每4天给药1次,共给药3次。每周测量裸鼠体重和瘤体积2~3次。计算出相对肿瘤体积(RTV)、相对肿瘤增殖率(T/C),并使用SPSS 13.0统计软件对各组动物体重、肿瘤体积结果进行统计学处理。疗效评价标准:T/C40%为无效;T/C≤40%,并经方差分析与阴性对照组比较,P0.05表示有效并具有统计学意义;用单因素方差分析的方法比较各组动物体重数据,以P0.05表示有统计学意义;在毒性相当(动物死亡率和体重下降相当)的情况下,对供试品组和阳性对照组的T/C进行比较。结果:YP-pegol各剂量组和阳性对照组的体重均值与溶媒对照组的体重数据均值无显著差异,YPpegol对裸鼠体重无明显影响;给药后第26天,供试品YP-pegol 20、40、60、90 mg·kg~(-1)剂量组、阳性对照组(伊立替康,60 mg·kg~(-1))与溶媒对照组比较,瘤体积(RTV)明显小于溶媒对照组(P0.05),并且各治疗组的T/C40%;与阳性对照组比较,YP-pegol高剂量组(90 mg·kg~(-1))肿瘤体积明显低于阳性对照组(P0.05)。给药后第62天,YP-pegol次高、高剂量组的相对肿瘤体积(RTV)与阳性对照组比较,明显低于阳性对照组(P0.05)。结论:YP-pegol对裸鼠人乳腺癌移植瘤具有明显的抑瘤作用并呈现一定的量效关系;YP-pegol较注射用伊立替康具有更好的疗效。
[Abstract]:Objective: to evaluate the in vivo antitumor activity of long acting topoisomerase I inhibitor, polyethylene glycol (PEG-Iritekam) YP-pegol.Methods: the cultured human breast cancer MCF-7 cells were subcutaneously inoculated into the armpit of the right forelimb of nude mice. Human breast cancer transplanted tumor model was established in nude mice. After tumor volume was increased to meet the test requirements, nude mice were randomly divided into 6 groups according to tumor volume: 4 YP-pegol dosage group, 1 solvent control group and 1 positive control group. The body weight and tumor volume of nude mice were measured 23 times a week. The relative tumor volume and the relative tumor proliferation rate were calculated. The weight of each group was measured by SPSS 13.0 statistical software. The tumor volume results were statistically processed. The curative effect evaluation standard: t / C 40% was invalid T / C 鈮，

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