Abstract：
Four Ag(I) complexes with mefenamato and nitrogen heterocyclic ligands, [Ag(2-apy)(mef)]2 (1), [Ag(3-apy)(mef)] (2), [Ag2(tmpyz)(mef)2] (3), and {[Ag(4,4\'-bipy)(mef)]2(CH3CN)1.5(H2O)2}n (4), (mef = mefenamato, 2-apy = 2-aminopyridine, 3-apy = 3-aminopyridine, tmpyz = 2,3,5,6-tetramethylpyrazine, 4,4\'-bipy = 4,4\'-bipyridine), were synthesized and characterized. The interactions of these complexes with BSA were investigated by fluorescence spectroscopy, which indicated that these complexes quench the fluorescence of BSA by a static mechanism. The fluorescence data also indicated that the complexes showed good affinity for BSA, and one binding site on BSA was suitable for the complexes. The in vitro cytotoxicity of the four complexes against human cancer cell lines (MCF-7, HepG-2, A549, and MDA-MB-468) and one normal cell line (HTR-8) was evaluated by the MTT assay. Complex 1 displayed high cytotoxic activity against A549 cells. Further studies revealed that complex 1 could enhance the intracellular levels of ROS (reactive oxygen species) in A549 cells, cause cell cycle arrest in the G0/G1 phase, and induce apoptosis in A549 cells in a dose-dependent manner.
摘要：
四个Ag（I）配合物与甲胺和氮杂环配体，[Ag(2-apy)(mef)]2(1)，[Ag(3-apy)(mef)](2)，[Ag2(tmpyz)(mef)2](3)，和{[Ag(4,4'-bipy)(mef)]2(CH3CN)1.5(H2O)2}n(4),(mef=mefenamato,2-apy=2-氨基吡啶，3-apy=3-氨基吡啶，tmpyz=2,3,5,6-四甲基吡嗪,4,4'-bipy=4,4'-联吡啶)，进行了合成和表征。通过荧光光谱法研究了这些配合物与BSA的相互作用，这表明这些复合物通过静态机制猝灭BSA的荧光。荧光数据还表明，复合物对BSA显示出良好的亲和力，BSA上的一个结合位点适用于复合物。通过MTT测定评估了四种复合物对人癌细胞系（MCF-7，HepG-2，A549和MDA-MB-468）和一种正常细胞系（HTR-8）的体外细胞毒性。复合物1表现出对A549细胞的高细胞毒活性。进一步的研究表明，复合物1可以增强A549细胞中ROS（活性氧）的细胞内水平，导致细胞周期停滞在G0/G1期，并以剂量依赖的方式诱导A549细胞凋亡。
