吡唑衍生物体外抗肿瘤活性研究

目的：研究吡唑衍生物对PC3、Bcap37、BGC8233种肿瘤细胞株生长的影响及其作用机制。方法：采用MTT比色法测定吡唑衍生物对3种肿瘤细胞生长的影响；AO／EB双染色，荧光显微镜观察细胞凋亡形态；利用Western Blot检测化合物对蛋白激酶磷酸化的影响。结果：吡唑衍生物对3种肿瘤细胞生长有一定的抑制作用，且具有浓度依赖性；吖啶橙／溴化乙锭（AO／EB）双染色可见吡唑衍生物F分别使PC3细胞变小、变圆，核染色质凝集，Bcap37细胞周围呈现亮绿色的荧光凋亡小体；Western Blot检测可知吡唑衍生物对EGF诱导的Erk1／2磷酸化没有抑制效果。结论：吡唑衍生物对3种肿瘤细胞生长有抑制作用，化合物F诱导PC3和Bcap37细胞凋亡，吡唑衍生物不能通过阻断Erk1／2磷酸化来抑制细胞增殖。

Anti-tumor activities of pyrazole derivatives in vitro

Objective:To investigate the anti-tumor activities of pyrazole derivatives against PC3,Bcap37 and BGC823 cells,and the mechanism of action.Methods:The inhibition effects of pyrazole derivatives on PC3,Bcap37 and BGC823 cells in vitro were tested through MTT colorimetric assay and the apoptotic morphology was observed by staining the PC3 cells with AO/EB.The inhibition effects of the compounds on the phosphorylation of Erk1/2 were determined by Western Blot analysis.Results:Pyrazole derivatives showed inhibition activities against PC3,Bcap37 and BGC823 cells in a concentration dependent manner;compound F could induce the apoptosis of PC3 and Bcap37 cells;Western Blot analysis showed that pyrazole derivatives could not inhibit the phosphorylation of Erk1/2 induced by EGF.Conclusions:Pyrazole derivatives can inhibit the activities of PC3,Bcap37 and BGC823 cells,and compound F may induce the apoptosis of PC3 and Bcap37 cells;pyrazole derivatives can not inhibit the proliferation of PC3 cell through Erk1/2 mediated signal pathway.