本文選題：聚乙二醇-伊立替康　切入點(diǎn)：拓?fù)洚悩?gòu)酶Ⅰ抑制劑　出處：《藥物分析雜志》2017年01期

【摘要】：目的:評(píng)價(jià)長(zhǎng)效拓?fù)洚悩?gòu)酶Ⅰ抑制劑聚乙二醇-伊立替康(YP-pegol)的體內(nèi)抗腫瘤活性。方法:將體外傳代培養(yǎng)后的人乳腺癌MCF-7細(xì)胞接種到裸鼠右前肢腋部皮下,建立裸鼠人乳腺癌移植瘤模型。待腫瘤體積增長(zhǎng)至滿足試驗(yàn)要求后,將裸鼠按腫瘤體積隨機(jī)分為6個(gè)組即4個(gè)YP-pegol劑量組,1個(gè)溶媒對(duì)照組和1個(gè)陽性對(duì)照組。每4天給藥1次,共給藥3次。每周測(cè)量裸鼠體重和瘤體積2~3次。計(jì)算出相對(duì)腫瘤體積(RTV)、相對(duì)腫瘤增殖率(T/C),并使用SPSS 13.0統(tǒng)計(jì)軟件對(duì)各組動(dòng)物體重、腫瘤體積結(jié)果進(jìn)行統(tǒng)計(jì)學(xué)處理。療效評(píng)價(jià)標(biāo)準(zhǔn):T/C40%為無效;T/C≤40%,并經(jīng)方差分析與陰性對(duì)照組比較,P0.05表示有效并具有統(tǒng)計(jì)學(xué)意義;用單因素方差分析的方法比較各組動(dòng)物體重?cái)?shù)據(jù),以P0.05表示有統(tǒng)計(jì)學(xué)意義;在毒性相當(dāng)(動(dòng)物死亡率和體重下降相當(dāng))的情況下,對(duì)供試品組和陽性對(duì)照組的T/C進(jìn)行比較。結(jié)果:YP-pegol各劑量組和陽性對(duì)照組的體重均值與溶媒對(duì)照組的體重?cái)?shù)據(jù)均值無顯著差異,YPpegol對(duì)裸鼠體重?zé)o明顯影響;給藥后第26天,供試品YP-pegol 20、40、60、90 mg·kg~(-1)劑量組、陽性對(duì)照組(伊立替康,60 mg·kg~(-1))與溶媒對(duì)照組比較,瘤體積(RTV)明顯小于溶媒對(duì)照組(P0.05),并且各治療組的T/C40%;與陽性對(duì)照組比較,YP-pegol高劑量組(90 mg·kg~(-1))腫瘤體積明顯低于陽性對(duì)照組(P0.05)。給藥后第62天,YP-pegol次高、高劑量組的相對(duì)腫瘤體積(RTV)與陽性對(duì)照組比較,明顯低于陽性對(duì)照組(P0.05)。結(jié)論:YP-pegol對(duì)裸鼠人乳腺癌移植瘤具有明顯的抑瘤作用并呈現(xiàn)一定的量效關(guān)系;YP-pegol較注射用伊立替康具有更好的療效。
[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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