Anticancer activity of novel ruthenium complex with 1,10-phenanthrolineselenazole as potent telomeric G-quadruplex inhibitor

详细信息	查看全文 | 推荐本文 |

• 作者：Qian Li^a ; Dongdong Sun^a ; Yanhui Zhou^a ; Du Liu^a ; Qianling Zhang^b ; ^{qlzh98@yahoo.com.cn} ; Jie Liu^a ; ^{tliuliu@jnu.edu.cn}
• 关键词：Ru(II)&ndash ; selenium complex ; Spectral property ; G-quadruplex ; Telomerase ; Anticancer activity
• 刊名：Inorganic Chemistry Communications
• 出版年：2012
• 期刊代码：39_13877003
• 类别：ch
• 出版时间：June, 2012
• 卷：20
• 期：Complete
• 页码：142-146
• 文件大小：881 K

摘要

A novel Ru(II)-selenium complex [Ru(phen)₂L](ClO₄)₂ (phen = 1,10-phenanthroline, L = 1,10-phenanthrolineselenazole) has been synthesized and structurally characterized by elemental analysis, ESI-MS and ¹H NMR spectra, and the interaction between human telomeric G-quadruplex DNA (HTG21) and the new compound has been studied by emission spectra, visual detection assay, circular dichroism (CD) spectroscopy and fluorescence resonance energy transfer (FRET) melting assay. The results show that the complex has interaction with human telomeric G-quadruplex DNA which is visually detected, meanwhile it induces the guanine-rich single-strand oligomer d[G₃(T₂AG₃)₃] to form antiparallel G-quadruplex and has a moderate ability to stabilize G-quadruplex structures (螖T_m = 11.2 掳C). Furthermore, polymerase chain reaction-stop assay, telomerase repeat amplification protocol, and MTT assay demonstrate that the Ru-complex can exhibit well inhibitory activity for telomerase and cancer cells. The results suggest that Ru-complex may be a potential telomerase inhibitor for cancer chemotherapy.