【摘要】 目的探讨西门木炔酸的抗结肠癌活性和相关机制。方法以}HCT116细胞为对象,用不同浓度和不同时间的西门木炔酸干预后,使用MTT法测细胞增殖活性、流式细胞仪测细胞凋亡和细胞周期情况,以及qPCR检测细胞周期相关因子的表达情况。结果西门木炔酸干预48h,显著抑制了HCT116的增殖活性(抑制浓度大于25μmol/L);干预72h,西门木炔酸25μmol/L时对HCT116细胞增殖的抑制率超过了50%。西门木炔酸也显著促进了HCT116晚期凋亡和坏死细胞的生成(25~100μmol/L)。西门木炔酸还显著阻滞HCT116细胞周期G1-S期的转变,表现为S期细胞显著下降(25~100μmol/L),并呈现时间和剂量依赖优势。此外,西门木炔酸干预下,HCT116细胞周期因子CCND3、CCNE1和CDK6的表达也显著下降(100μmol/L)。结论西门木炔酸显著抑制HCT116细胞增殖、促进细胞晚期凋亡和坏死,这与西门木炔酸抑制细胞周期因子表达进而阻滞HCT116细胞周期G1-S期的转变有关更多还原

【Abstract】 Objective To investigate the antitumor activity of ximenynic acid and its mechanism.Methods HCT116 cells were treated with ximenynic acid in vitro.MTT assay,flow cytometry and qPCR analyses were adopted to investigate the proliferation,apoptosis,cell cycle distribution and related genes expression of HCT116 cells.Results The proliferation of HCT116 cells was significantly suppressed by ximenynic acid(>25μmol/L) after 48 h incubation.The 50%inhibition was achieved with 25μmol/L ximenynic acid after 72 h incubation.The late stage and necrosis cells were significantly increased after ximenynic acid treatment(25-100μmol/L).Besides,ximenynic acid could block the transition of Gl to S phase of cell cycle,in which the S phase cells were remarkably diminished in dose and time dependent manner after ximenynic acid treatment.Moreover,the expression of related genes CCND3,CCNEl and CDK6 were marked decreased by ximenynic acid treatment(100μmol/L).Conclusion Ximenynic acid showed the anti-proliferation activity and promoted late apoptosis or necrosis on HCT116 cells.The effects of ximenynic acid on HCT116 cells may be associated with the blockage of cell cycle and inhibition of related genes expression.|更多还原