Yu Hao, Yang Yong, Li Qiaoyu, Ma Tieliang, Xu Jun, Zhu Taofeng, Xie Jing, Zhu Wenjiao, Cao Zhihong, Dong Kun, Huang Jiancui, Jia Lei
The Affiliated People 's Hospital of Jiangsu University, #8 Dianli Road, Zhenjiang, Jiangsu, 212000, China.
The Affiliated Yixing Hospital of Jiangsu University, #75 Tongzhenguan Road, Yixing, Jiangsu, 214200, China.
Chem Biol Drug Des. 2016 Mar;87(3):398-408. doi: 10.1111/cbdd.12669. Epub 2015 Nov 20.
A serial of mixed-ligand Cu(II) complexes of the type [Cu(phens)(H2 PDILeu)]H2 O (1-4) containing phens as 2,2'-bipyridyl (bpy, 1), 1,10-phenanthroline (phen, 2), dipyrido[3,2-d:2',3'-f]quinoxaline (dpq, 3), and dipyrido[3,2-a:2',3'-c]phenazine (dppz, 4) have been isolated and characterized. The interaction of the complexes with calf-thymus DNA has been explored by physical methods to propose modes of DNA binding of the complexes, which indicate that 4 interacts with DNA more strongly than all of the other complexes through intercalation interaction. Furthermore, cell apoptosis was detected by AnnexinV/PI flow cytometry and TUNEL assay and by Western blotting to detect the protein expression of p53, Bax, and Bcl-2. All the three copper complexes can effectively induce apoptosis of the three human tumor cells, which was accompanied with upregulation of the expression of p53 and Bax, while Bcl-2 decreased.
一系列通式为[Cu(phens)(H₂PDILeu)]H₂O (1 - 4)的混合配体铜(II)配合物已被分离和表征，其中phens分别为2,2'-联吡啶(bpy, 1)、1,10-菲咯啉(phen, 2)、二吡啶并[3,2 - d:2',3'-f]喹喔啉(dpq, 3)和二吡啶并[3,2 - a:2',3'-c]吩嗪(dppz, 4)。已通过物理方法探究了这些配合物与小牛胸腺DNA的相互作用，以提出配合物与DNA的结合模式，结果表明4通过嵌入相互作用与DNA的结合比其他所有配合物都更强。此外，通过AnnexinV/PI流式细胞术和TUNEL检测法检测细胞凋亡，并通过蛋白质印迹法检测p53、Bax和Bcl-2的蛋白表达。所有这三种铜配合物均可有效诱导三种人类肿瘤细胞凋亡，同时伴随着p53和Bax表达上调，而Bcl-2表达下降。
