| 氨·二甲胺·羧酸根合铂(Ⅱ)类配合物的合成、抗肿瘤活性和与DNA的键合水平(英文) |
| Synthesis, Cytotoxicity and DNA-binding Levels of Ammine/Dimethylamine Platinum(Ⅱ) Complexes with Carboxylates |
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| 摘要: 本工作设计合成了6种新型混胺羧酸根合铂(Ⅱ)类配合物[Pt((?)NH)(NH3)X2](a～f){其中，X=CH3COO-(乙酸根)，CH3Cl COO-(氯乙酸根)，CHCl2COO-(二氯乙酸根)，C6H5-COO-(苯甲酸根)，p-CH3-C6H4-COO-(对甲基苯甲酸根)，p-CH3O-C6H4-COO-(对甲氧基苯甲酸根)}。通过元素分析、摩尔电导、差热分析、红外光谱、紫外光谱和 1H核磁共振谱对配合物进行了表征。通过MTT法研究了配合物的体外抗肿瘤活性，通过等离子体质谱研究了配合物与细胞DNA的键合量；体外抗肿瘤活性测试表明，配合物(a～f)对所测试的肿瘤细胞MCF-7、HCT-8和BGC-823没有表现出活性，但对EJ和HL-60两种肿瘤细胞表现出好的活性，而且配合物(d～f)对HL-60细胞的活性与顺铂相当。配合物(a～f)与HL-60细胞的DNA键合量与其作用浓度表现出一定的依赖性，从小到大的顺序为：cisplatin < c < b < a < f < e < d。 |
| 关键词: 混胺铂(Ⅱ)配合物 细胞毒性 经典构效关系 Pt-DNA键合 |
| 基金项目: |
| Abstract: Six new ammine/dimethylamine platinum(Ⅱ) complexes with carboxylates (a～f) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, and 1H NMR techniques. The cytotoxicity of the complexes was tested by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide)assay. The levels of total platinum bound to DNA were measured by ICP-MS. The results show that the complexes (a～f) have selectivity against tested carcinomas, have no cytotoxicity against HCT-8, BGC-823 and MCF-7, but have better cytotoxicity against EJ and HL-60, moreover, cytotoxicity of complexes (d～f) against HL-60 is similar to that of cisplatin. The levels of total platinum bound to DNA in HL-60 are increased with increasing concentrations，and the levels of total platinum bound to DNA increase in the following sequence: cisplatin < c < b < a < f < e < d. |
| Keywords: mixed amine platinum(Ⅱ) complexes cytotoxicity classical structure-activity relationships Pt-DNA binding |
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| 张金超,赵学军,申勇.氨·二甲胺·羧酸根合铂(Ⅱ)类配合物的合成、抗肿瘤活性和与DNA的键合水平(英文)[J].无机化学学报,2007,23(3):415-420. |
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