Department of Chemistry, Jinan University, Guangzhou 510632, PR China; GuangDong Dongguan Health School, Dongguan 523186, PR China.
J Inorg Biochem. 2014 Jan;130:122-9. doi: 10.1016/j.jinorgbio.2013.10.006. Epub 2013 Oct 12.
Two ruthenium(II) complexes Ru(IP)2(PIP)2·2H2O (1) and Ru(PIP)2(IP)2·2H2O (2) (IP=imidazole [4, 5-f] [1,10] phenanthroline, PIP=2-phenylimidazo-[4, 5-f][1,10] phenanthroline) have been synthesized and characterized. The quadruplex binding of the compounds was evaluated by emission spectrum, CD spectroscopy, Visual detection assay and FRET (fluorescence resonance energy transfer)-melting assay. The results show that both complexes can induce the stabilization of quadruplex DNA, while complex 1 is a better G-quadruplex binder than complex 2. Furthermore, polymerase chain reaction-stop assay, electrophoretic mobility shift assay, telomerase repeat amplification protocol and MTT (3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay demonstrate that complex 1 not only can stabilize dimer forms of the G-quadruplex at low concentrations but also exhibit better inhibitory activity for telomerase and cancer cells.
两种钌（II）配合物Ru(IP)2(PIP)2·2H2O（1）和Ru(PIP)2(IP)2·2H2O（2）（IP=咪唑[4,5-f][1,10]菲咯啉，PIP=2-苯基咪唑[4,5-f][1,10]菲咯啉）已被合成并表征。通过发射光谱、CD 光谱、目视检测法和 FRET（荧光共振能量转移）-融解法评估了化合物的四链体结合。结果表明，两种配合物都能诱导四链体 DNA 的稳定化，而配合物 1 是比配合物 2 更好的 G-四链体结合物。此外，聚合酶链反应停止法、电泳迁移率变动分析法、端粒酶重复扩增协议和 MTT（3-[4,5-二甲基噻唑-2-基]-2,5-二苯基四氮唑溴盐）分析法表明，配合物 1 不仅可以在低浓度下稳定 G-四链体的二聚体形式，而且对端粒酶和癌细胞也表现出更好的抑制活性。
