目的研究铁-氟尿嘧啶配合物对人胃癌细胞SGC-7901的细胞毒活性及对细胞凋亡的影响。方法采用MTT法检测配合物及其配体对SGC-7901的增殖抑制作用,流式细胞术检测配合物及其配体对SGC-7901细胞凋亡的影响,实时荧光定量PCR法检测配合物及其配体对凋亡相关因子Caspase-8基因表达的影响。结果配合物能明显抑制SGC-7901细胞的增殖,IC_(50)为35μM,抑制作用强于其配体氟尿嘧啶和邻菲罗啉。配合物在10、20、40μM浓度时能明显促进SGC-7901细胞凋亡,作用强于其配体5-Fu和Phen;配合物能使凋亡相关因子Caspase-8在mRNA水平的表达上调。结论铁-氟尿嘧啶配合物的合成使其配体间形成了协同作用,具有良好的体外抗肿瘤活性。铁-氟尿嘧啶配合物诱导细胞凋亡的作用可能与促凋亡因子Caspase-8的上调相关。
Objective In this study,we explored iron-fluorouracil complex cytotoxicity and effect to induce apoptosis on human cancer cells.Methods MTT method was used to detect inhibition rate of the complex on human gastric cancer cell SGC-7901;Flow cytometry(FCM)method was used to exhibit apoptosis of SGC-7901 induced by the complex;Quantitative real-time PCR was used to measure the mRNA expression of apoptosis related factor Caspase-8.Results The complex obviously inhibited the proliferation of SGC-7901 cell,IC_(50) value was 35μM.The results showed that the complex can remarkably promote SGC-7901 cell apoptosis than its ligand 5-Fu and Phen;The mRNA expression of Caspase-8was up-regulated.Conclusion The synthesis of Iron-Fluorouracil complex gave rise to synergistic antitumor effect of its ligands,and apoptosis induction effect of the complex on cancer cells may be caused by up regulation of Caspase-8.