High cytotoxicity of dihalo-substituted 8-quinolinolato-lanthanides

被引:55
作者
Chen, Zhen-Feng [1 ]
Song, Xiao-Yan [1 ]
Peng, Yan [1 ]
Hong, Xue [1 ]
Liu, Yan-Cheng [1 ]
Liang, Hong [1 ]
机构
[1] Guangxi Normal Univ, Sch Chem & Chem Engn, Key Lab Chem & Mol Engn Med Resources, Minist Educ China, Guilin 541004, Peoples R China
基金
中国国家自然科学基金;
关键词
DNA-BINDING PROPERTIES; NEUTRAL RED-DYE; X-RAY-STRUCTURE; BIOLOGICAL-ACTIVITY; METAL-COMPLEXES; RUTHENIUM(II) COMPLEXES; CIRCULAR-DICHROISM; ALZHEIMERS-DISEASE; LA(III) COMPLEX; ANTITUMOR;
D O I
10.1039/c0dt01310b
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Three new lanthanide complexes with dihalo-substituted 8-quinolinol: [Gd(BrQ)(3)(H2O)(2)]center dot 1.33EtOH center dot 0.33H(2)O (1), [Dy(ClQ)(3)(H2O)(2)]center dot 1.33EtOH center dot 0.33H(2)O (2), [Er(ClQ)(3)(H2O)(2)]center dot 1.33EtOH center dot 0.33H(2)O (3)(H-BrQ = 5,7-dibromo-8-quinolinol, H-ClQ = 5,7-dichloro-8-quinolinol)have been synthesized and characterized by elemental analysis, IR, ESI-MS, single-crystal X-ray diffraction and TGA. The single-crystal X-ray diffraction analyses reveal that complexes 1-3 are mononuclear and isostructural. Each metal centre is coordinated by three dihalo-substituted 8-quinolinol and two aqua ligands. The in vitro cytotoxicity of dihalo-substituted 8-quinolinol and complexes 1-3 against liver cancer BEL7404 was evaluated. The IC50 values of 1-3 to BEL7404 were 47.2 +/- 2.6, 18.3 +/- 1.0 and 31.5 +/- 1.2 nM, respectively. The lanthanide complexes 1-3 exhibited significantly enhanced cytotoxicity vs. free substituted 8-quinolinol. The binding properties of dihalo-substituted 8-quinolinol and complexes 1 and 2 to DNA were investigated by UV-vis, fluorescence, CD spectroscopy and viscosity measurements, as well as agarose gel electrophoresis experiments. Both complexes 1 and 2 interact more strongly with DNA than the free quinolinol ligand. Intercalation is the most probable binding mode for both the complexes and the quinolinol ligands.
引用
收藏
页码:1684 / 1692
页数:9
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