Xu Li, Zhong Nan-Jing, Huang Hong-Liang, Liang Zhen-Hua, Li Zheng-Zheng, Liu Yun-Jun
School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Zhongshan, PR China.
Nucleosides Nucleotides Nucleic Acids. 2012;31(8):575-91. doi: 10.1080/15257770.2012.704110.
Two new ruthenium(II) polypyridyl complexes Ru(dmb)(2)(HECIP)(2) (1) (HECIP = N-ethyl-4-[(1,10)-phenanthroline(5,6-f)imidazol-2-yl]carbazole, dmb = 4,4'-dimethyl-2,2'-bipyridine) and Ru(dmp)(2)(HECIP)(2) (2) (dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and characterized. The DNA-binding behaviors of the two complexes were investigated by absorption spectra, viscosity measurements, and photoactivated cleavage. The DNA-binding constants for complexes 1 and 2 were determined to be 8.03 (± 0.12) × 10(4) M(-1) (s = 1.62) and 2.97 (± 0.15) × 10(4) M(-1) (s = 1.82), respectively. The results suggest that these complexes interact with DNA through intercalative mode. The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 has been evaluated by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide)] method. Complex 1 shows higher anticancer potency than 2 against the four tumor cell lines. Apoptosis and cellular uptake were investigated. The antioxidant activities of the ligand and these complexes were also performed.
已合成并表征了两种新型钌（II）多吡啶配合物Ru(dmb)(2)(HECIP)(2)（1）（HECIP = N-乙基-4-[(1,10)-菲咯啉(5,6-f)咪唑-2-基]咔唑，dmb = 4,4'-二甲基-2,2'-联吡啶）和Ru(dmp)(2)(HECIP)(2)（2）（dmp = 2,9-二甲基-1,10-菲咯啉）。通过吸收光谱、粘度测量和光活化切割研究了这两种配合物与DNA的结合行为。配合物1和2的DNA结合常数分别测定为8.03（±0.12）×10(4) M(-1)（s = 1.62）和2.97（±0.15）×10(4) M(-1)（s = 1.82）。结果表明这些配合物通过插入模式与DNA相互作用。研究了Ru（II）配合物对pBR322 DNA的光切割。通过MTT [3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-四唑溴化物]法评估了配合物1和2的细胞毒性。配合物1对四种肿瘤细胞系显示出比2更高的抗癌效力。研究了细胞凋亡和细胞摄取。还进行了配体和这些配合物的抗氧化活性研究。
