金属铜配合物Cu(Ⅱ)吨酮冠醚的体外抗肿瘤作用

目的探讨金属铜配合物Cu（Ⅱ）吨酮冠醚（XCE-Cu）的体外抗肿瘤作用。方法采用噻唑蓝比色法测定XCE—Cu对卵巢癌细胞3AO、食管鳞癌细胞ECA109、肺癌细胞GLC-82、胃癌细胞SGC一7901增殖的抑制作用;应用流式细胞仪检测药物对3AO细胞周期和凋亡的影响。结果XCE—Cu呈浓度依赖性的抑制3AO、ECAl09、GLC-82、SGC-7901细胞生长,作用72h的半抑制浓度依次为4．1、8．2、15．9、8．7ug／mL,其中对3AO的抑制作用最强。作用24、48、72hXCE-Cu呈浓度、时间依赖性的抑制3AO细胞生长,作用明显强于卡铂。12．5—50ug／mL使3AO细胞G1期减少而S期和G2期增加,并剂量依赖性的诱导细胞凋亡。结论XCE—Cu在体外具有抗肿瘤作用,对3AO细胞的选择性高,其机理为阻止细胞于S期和诱导细胞调亡。

Anti-tumor effects of CU complex with xanthone crown-ether in vitro

Objective To study the anti-tumor activity of Cu complex with xanthone crownether （XCE-Cu） in vitro and the effect on 3AO cell cycle and apoptosis. Methods Cell growth inhibition effect of tumor cells after treated with XCE-Cu was determined by 3-（4, 5-dimethylthiazol- 2-yl）-2, 5-diphenyl tetrazolium bromide in vitro. Cell cycle and apoptosis was determined by flow cytometry. Results XCE-Cu was inhibited 3AO, ECA109, GLC-82, SGC-7901 cells growth in a concentration dependent manner. After treatment with XCE-Cu 72 h, the 50% inhibiting concentration on 3AO, ECA109, GLC-82, SGC-7901 cells were 4.1, 8.2, 15.9 and 8.7 ug/mL respectively. The sensitivity of XCE-Cu on 3AO cell was the highest. The anti-tumor activity of XCE-Cu on 3AO cell was stronger in concentration and time dependence than that of carboplatin. 12.5-50 ug/mL XCE-Cu increased S and G2 phase but decreased G1 phase of 3AO cell. Meanwhile it also significantly induced 3AO cell apoptosis. Conclusion XCE-Cu has anti-tumor effect in vitro and the 3AO cell is the most selective and its mechanism may be to arrest cell in S phase and induce cell apoptosis.