苯并呋喃类考布他汀类似物抗乳腺癌和宫颈癌细胞增殖作用初步研究

Preliminary study on the inhibitory effect of benzofuran-based coubertin analogues on breast cancer and cervical cancer cells

目的研究含苯并呋喃类结构的考布他汀(CombretastatinA-4,CA-4)类似物(化合物I)的体外抗乳腺癌及宫颈癌细胞增殖的活性。方法分别将乳腺癌细胞(MCF-7)和宫颈癌细胞(SiHa)按照一定的接种密度分为药物组(分别加入0.1、1.0、5.0、15.0、50.0、100.0μmol/L的化合物I)、阴性对照组(不加化合物I)、阳性对照组(CA-4)、空白对照组(不加化合物I,不含细胞),置于37℃、5%CO_2环境下培养48h后,采用MTT法测定OD值,计算抑制率和IC_(50)值,Hoechst荧光染色法观察细胞形态变化;流式细胞技术检测细胞凋亡和生长周期;AutodockTools软件进行分子对接,并做单因素方差分析。结果与对照组相比,药物组OD值降低,抑制率升高,细胞凋亡率升高,差异有统计学意义(P <0.05)。结论化合物I具有抗乳腺癌及宫颈癌细胞增殖作用,其作用主要发生在G2期。

Objective To study the anti-cancer activity in vitro of the compound analogue combretastatinA-4(CA-4).Methods The experiment was designed and set as negative control group(no drugs),positive control group(CA-4),blank control group(no drugs and cells)and the drug group(0.1,1.0,5.0,15.0,50.0,100.0μmol/L of compound I).MTT assay was used to detect the OD value as well as the inhibition rate and IC(50)value were calculated,cell morphology was observed by Hoechst fluorescence staining,flow cytometry was used to detect apoptosis and cell cycle,moleculars were docked by the AutodockTools,single factor analysis of variance was done.Results Compared with the control group,OD value in the drug group decreased,apoptosis rate and inhibition rate increased,and the difference was statistically significant(P<0.05).Conclusion Compound I had anti-breast cancer and anti-cervical cancer in terms of proliferation,and its action mainly occurred in G2phase.