Anticancer Activity for Targeting Telomeric G-Quadruplex and Antiangiogenesis of a Novel Ru(II)–Se Complex

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• 作者：Lijun Wang (1)
  Chuping Zheng (2)
  Yanyu Liu (2)
  Fangling Le (2)
  Fang Yang (2)
  Xiuying Qin (2)
  Chuan Wang (2)
  Jie Liu (2)
  
• 关键词：Ru(II)–Se complex ; Telomeric G ; quadruplex ; Anticancer activity ; Apoptosis ; Cell migration ; Antiangiogenesis
• 刊名：Biological Trace Element Research
• 出版年：2014
• 出版时间：February 2014
• 年：2014
• 卷：157
• 期：2
• 页码：175-182
• 全文大小：444 KB
• 作者单位：Lijun Wang (1)
  Chuping Zheng (2)
  Yanyu Liu (2)
  Fangling Le (2)
  Fang Yang (2)
  Xiuying Qin (2)
  Chuan Wang (2)
  Jie Liu (2)
  
  1. College of Chemistry and Biology, Beihua University, Jilin, 132013, People’s Republic of China
  2. Department of Chemistry, Jinan University, Guangzhou, 510632, People’s Republic of China
  
• ISSN：1559-0720

文摘

A new Ru(II)–Se complex, Ru(bpy)2L2Cl2 (bpy--,2-bipyridine, L--,10-phenanthrolineselenazole) (Ru-Se) has been synthesized and characterized. The G-quadruplex DNA-binding properties of the complex and its selenium ligand (Phen-Se) were evaluated by thermal denaturation study, polymerase chain reaction (PCR) stop assay, and telomerase repeat amplification protocol (TRAP). The results showed that the obtained complex could induce and stabilize G-quadruplex structure as well as exhibit potent inhibitory activity against telomerase. In vitro cytotoxicity studies showed that complex Ru-Se inhibited the cancer cell growth through apoptosis. However, the presence of the ligand Phen-Se did not appear to have a significant effect either on G-quadruplex binding or on biological activity. Furthermore, the cell migration assay and the tube formation assay also demonstrated that the complex Ru-Se significantly inhibited human umbilical vascular endothelial cell (HUVEC) proliferation, migration, and tube formation. These findings indicate that the Ru–Se complex may be a potential telomerase inhibitor and a viable drug candidate in antiangiogenesis for anticancer therapies.