新型化合物吡啶衍生物的抗肿瘤活性研究

K. M.Y., D. O.N., Samishina E.A., Arutiunian K.K., Epishkina A.A.
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摘要

本文研究了一种新的吡啶衍生物LHT-13-19的抗肿瘤活性。为了确定有效的抑制浓度,采用人结肠癌HCT116培养。在10-9 ~ 10-7 m浓度的LHT-13-19存在下对肿瘤细胞进行孵育,MTT试验检测肿瘤细胞的存活情况。实验采用30只12周龄人源化BALB/c nu/nu雌性异种移植结直肠癌小鼠进行体内实验。将所有动物分为3组,每组10只,对照组每日腹腔注射0.5 ml PBS,第二组每日注射环磷酰胺,剂量为10 mg/kg,第三组每日注射LHT-13-19,剂量为3.7 mg/kg,连续10 d。评估动物的生存和抗肿瘤活性。估计肿瘤倍增时间、肝浅表转移数和生存时间。每天用LHT-13-19培养人结肠肿瘤细胞,伴随着该化合物的细胞毒性作用的形成。在人源化BALB/c nu/nu小鼠结肠腺癌异种移植模型中,3.7 mg/kg LHT-13-19 10天的疗程可通过增加肿瘤倍增时间、动物存活率和降低转移频率而形成抗肿瘤作用
本文章由计算机程序翻译,如有差异,请以英文原文为准。
ON ANTITUMOR ACTIVITY OF A NOVEL COMPOUND – A PYRIDINE DERIVATIVE
The work studied the antitumor activity of a new compound, a pyridine derivative LHT-13-19. To determine the effective inhibitory concentration, a culture of human colon cancer HCT116 was used. Incubation of tumor cells was carried out in the presence of LHT-13-19 in the concentration range from 10-9 to 10-7 M. The survival of tumor cells was determined in MTT test. In vivo experiments were performed on thirty athymic humanized 12-week-old female BALB/c nu/nu mice with xenograft colorectal adenocarcinoma. All animals were divided into 3 groups, 10 mice in each: animals of the control group were injected daily intraperitoneally with 0.5 ml of PBS, animals of the second group were treated with a cyclophosphamide at a dose of 10 mg/kg, mice of the third the groups received LHT-13-19 as experimental therapy at a daily dose of 3.7 mg/kg during 10 days. Animals’ survival and antitumor activity were assessed. Tumor-doubling time, the number of liver superficial metastases and survival time were estimated. Daily incubation of human colon tumor cells with LHT-13-19 is accompanied by the formation of the cytotoxic effect of the compound. On a xenograft model of colon adenocarcinoma in humanized BALB/c nu/nu mice, a 10-day course of 3.7 mg/kg LHT-13-19 leads to the formation of an antitumor effect due to increase in the time of tumor doubling, animal survival and a decrease in the frequency of metastasis
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