Department of Chemistry, Jinan University, Guangzhou 510632, PR China.
Department of Chemistry, Jinan University, Guangzhou 510632, PR China; School of Pharmacy, Guangdong Medical College, Zhanjiang, 524023, PR China.
J Inorg Biochem. 2014 May;134:1-11. doi: 10.1016/j.jinorgbio.2013.12.005. Epub 2013 Dec 24.
Two ruthenium(II) complexes (Ru-complexes) were synthesized and characterized in this study. The selectivity and ability of the complexes to interact with bcl-2 DNA were investigated here. It turned out that Ru(ip)32·2H2O (complex 1, ip = 1H-iminazole [4,5-f][1,10] phenanthroline) could induce and stabilize the formations of G-quadruplexes more effectively than Ru(pip)32·2H2O (complex 2, pip = 2-phenylimidazo-[4,5-f][1,10]phenanthroline) did. Considering the important role of the Ru-complex ligand in inducing and stabilizing the formations of G-quadruplex in our previous studies, we speculate that the overlarge ligand of complex 2 may block its binding affinity for G-quadruplexes. Complex 1 also induced cell apoptosis in in vitro assays. In general, this study provided potentially important information for further development of the Ru-complexes as good inducers and stabilizers of bcl-2 G-quadruplex DNA for cancer treatment.
本研究合成并表征了两种钌（II）配合物（Ru-complexes）。在此研究了配合物与 bcl-2 DNA 相互作用的选择性和能力。结果表明，Ru(ip)32·2H2O（配合物 1，ip = 1H-咪唑[4,5-f][1,10]菲咯啉）比Ru(pip)32·2H2O（配合物 2，pip = 2-苯基咪唑[4,5-f][1,10]菲咯啉）更有效地诱导和稳定 G-四链体的形成。考虑到 Ru-complex 配体在我们之前的研究中诱导和稳定 G-四链体形成的重要作用，我们推测配合物 2 过大的配体可能会阻碍其与 G-四链体的结合亲和力。配合物 1 也在体外实验中诱导了细胞凋亡。总的来说，本研究为进一步开发 Ru-complexes 作为治疗癌症的 bcl-2 G-四链体 DNA 的良好诱导剂和稳定剂提供了潜在的重要信息。
