New mononuclear complexes [Mn(NO₃)(sac)(H₂O)(bzimpy)]·2DMF (Mn), [Fe(sac)₂(H₂O)(bzimpy)]·2H₂O (Fe), [Co(bzimpy)₂](sac)₂·2H₂O (Co), [Ni(bzimpy)₂](sac)₂·H₂O·i-PrOH (Ni) and [Cu(sac)₂(bzimpy)]·3DMF (Cu) (sac = saccharinate and bzimpy = 2,6-bis(2-benzimidazolyl)pyridine) were synthesized and structurally characterized by elemental analysis, UV–Vis, IR, ESI-MS and X-ray diffraction. The anticancer activity of the metal complexes against A549 (lung), MCF-7 (breast), HT29 (colon) cancer cells and MCF10A (normal human breast epithelial) cells was tested and compared with those of cisplatin and bzimpy. The complexes displayed potent cytotoxic activity especially in MCF-7 and A549 cell lines, but they were practically inactive against the normal cells. Mechanistic studies with Mn and Cu complexes on A549 cells indicated that the complexes induced G0/G1 arrest. Both complexes increased intracellular ROS (reactive oxygen species) levels and successfully caused both mitochondrial dysfunction and double-strand DNA breaks. The up-regulated Bax and down-regulated Bcl-2 expression levels, caspase-3/7 activation and reduced Fas expression indicated that Mn and Cu induced ROS-dependent mitochondria-mediated intrinsic apoptosis in A549 cells.

新的单核络合物[Mn（NO ₃）（sac）（H ₂ O）（bzimpy）]·2DMF（Mn），[Fe（sac）₂（H ₂ O）（bzimpy）]·2H ₂ O（Fe）， [Co（bzimpy）₂ ]（sac）₂ ·2H ₂ O（Co），[Ni（bzimpy）₂ ]（sac）₂ ·H ₂ O· i -PrOH（Ni）和[Cu（sac）₂（bzimpy） ）]·3DMF（铜）（sac =糖精，bzimpy = 2,6-双（2-苯并咪唑基）吡啶），并通过元素分析，UV-Vis，IR，ESI-MS和X射线衍射对其结构进行了表征。测试了金属配合物对A549（肺），MCF-7（乳腺癌），HT29（结肠）癌细胞和MCF10A（正常人乳腺上皮）细胞的抗癌活性，并将其与顺铂和bzimpy的抗癌活性进行了比较。该复合物显示出有效的细胞毒性活性，尤其是在MCF-7和A549细胞系中，但实际上对正常细胞无活性。锰和铜的力学研究A549细胞上的复合物表明该复合物诱导了G0 / G1停滞。两种复合物均会增加细胞内ROS（活性氧）的水平，并成功地导致线粒体功能障碍和双链DNA断裂。上调Bax和下调Bcl-2表达水平，caspase-3 / 7激活和Fas表达降低表明Mn和Cu诱导ROS依赖的线粒体介导的A549细胞内在凋亡。