目的探讨野西瓜总生物碱(Capparisspinosa alkaloid,CSA)对人肝癌HepG2细胞的杀伤和诱导凋亡的作用机制。方法MTT法研究CSA对人肝癌HepG2的杀伤作用;荧光显微镜观察HepG2细胞形态;流式细胞仪研究CSA对HepG2细胞的凋亡诱导作用;激光共聚焦显微镜检测CSA对HepG2细胞内[Ca²⁺]i的影响。结果CSA对人肝癌HepG2有明显细胞毒性作用,并且有剂量依赖性,IC50为42.82μg/mL;HepG2细胞在CSA作用后出现特征性凋亡形态特征,凋亡细胞比率明显高于自然凋亡率;且阻断细胞由S期向G2期的移行,CSA明显升高HepG2细胞[Ca²⁺]i,并与药物质量浓度呈量效正相关。结论CSA对人肝癌HepG2有明显的杀伤和促凋亡作用,其机制可能与CSA造成肿瘤细胞内钙离子超载有关。

Objective To study the mechanism of killing and apoptosis-inducing effects of Capparis spinosa alkaloid (CSA) on human hepatocarcinoma cell line HepG2. Methods The killing effect of CSA on human hepatocarcinoma cell line HepG2 was studied by MTT method. Morphological observation of HepG2 cells was carried out by fluorescence microscope. Results The CSA had obvious cytotoxicity on the HepG2 in a dose-dependent manner and its IC50 value was 142.82 μg/mL. The HepG2 cells showed the characteristic morphologic changes of apoptosis by the function of CSA and the apoptosis percentage is higher than that of the natural one. The progress of cells cycle from S phase to G2 phase had been blocked by CSA. The intracellular Ca²⁺ level had been increased by the function of CSA, which was positively related with drug concentration. Conclusion CSA has obviously killing and apoptosis-inducing effects on human hepatocarcinoma cell line HepG2 and calcium overload might also be invovled in these events.

黑龙江省自然科学基金资助项目(C20060)