【摘要】 目的研究新型钌(Ⅱ)多吡啶配合物[Ru(dmp)2Nadpip](Cl O4)2(Ru 1)对人骨肉瘤U-2 OS细胞增殖抑制及相关机制。方法 MTS法检测细胞增殖抑制情况,DAPI染色观察细胞吸收Ru1作用部位情况,Hoechst-33258染色观察Ru1作用后细胞核的形态变化,流式细胞仪检测细胞凋亡和细胞周期情况。结果 (6.25~100.00)μmol/L的Ru 1均能不同程度抑制骨肉瘤细胞增殖,其24、48、72 h半数抑制浓度(IC50)分别为113.26、45.52、41.00μmol/L,对骨肉瘤细胞增殖抑制作用呈时间-剂量依赖关系。细胞吸收结果显示Ru 1能进入细胞质,聚集并作用于细胞核内。药物处理后的细胞经Hoechst-33258染色,细胞核出现致密浓染,或呈碎块状致密浓染。100.0、50.0、25.0μmol/L Ru 1作用于细胞48 h后的凋亡率分别为(38.51±3.72)%、(21.13±2.03)%、(11.75±2.54)%,与对照组比较,差异均有统计学意义(P<0.05)。流式检测药物作用后的U-2 OS细胞呈现G0/G1期阻滞,并呈时间-剂量依赖效应。结论 Ru 1能抑制U-2 OS细胞增殖,诱导其发生凋亡并呈现G0/G1期阻滞,均与时间、剂量正相关。更多还原

【Abstract】 Objective To investigate the effects of ruthenium(Ⅱ) polypyfidyl complex [Ru(dmp)2Nadpip](Cl O4)2(Ru 1)on proliferation inhibition and the possible mechanism of human osteosarcoma cell line U-2OS in vitro.Methods MTS assay was used to detect the cytotoxicity of Ru 1 against U-2 OS cells; The cell uptake was investigated by DAPI staining.Nucleus morphological changes was evaluated by Hoechst 33258 staining method.Changes of apoptosis and cell cycle were analyzed by flow cytometry.Results(6.25-100.00) μmol / L of Ru1 could inhibit different percentages of osteosarcoma cell proliferation.The IC50 values of 24 h,48 h,72 h were 113.26 μmol / L,45.52 μmol / L,41.00 μmol / L,respectively.Significantly,the proliferation inhibition of Ru 1towards osteosarcoma cell was in a dose and time dependent manner.The cellular uptake showed that Ru 1 can enter into the cytoplasm,gather and act on the nucleus.Cell nucleus appeared dense stain,or showed fragmented dense stain after drug treatment of the cells by Hoechst 33258 staining.Flow cytometry detection showed that the percentages of apoptosis after the treatment with Ru 1at 100.0,50.0,25.0 μmol / L for 48 h were(38.51 ± 3.72)%,(21.13 ± 2.03)% and(11.75 ± 2.54)%,respectively.The data compared with the control group,the difference was statistically significant(P <0.05).After the treatment with Ru 1,the U-2 OS cells showed G0/ G1 phase arrest,and was in a dose and time dependent manner.Conclusion Ru 1 is able to inhibit cell proliferation and induce apoptosis in U-2 OS cells and showed G0/ G1 phase arrest,both with time and dose positive.更多还原