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镧系金属(III)配合物的合成、表征、DNA 结合和抗增殖活性与 N-(氮杂环)去甲斑蝥酰亚胺酸。

Synthesis, characterization, DNA-binding and antiproliferative activity of Nd(III) complexes with N-(nitrogen heterocyclic) norcantharidin acylamide acid.

机构信息

Zhejiang Key Laboratory for Reaction Chemistry on Solid Surfaces, Zhejiang Normal University, Jinhua 321004, China.

出版信息

J Fluoresc. 2009 Sep;19(5):857-66. doi: 10.1007/s10895-009-0483-x. Epub 2009 Apr 25.

Abstract

Three novel complexes [Nd(L)(NO3)(H2O)2].NO(3).2H2O (HL1 = N-pyrimidine norcantharidin acylamide acid, C12H13N3O4; HL2 = N-pyridine norcantharidin acylamide acid, C13H14N2O4; HL3 = N-phenyl norcantharidin acylamide acid, C14H15NO4) were synthesized. HL1, HL2 and HL3 are the ligand of complex(1), complex(2) and complex(3), respectively. Their structures were characterized by elemental analysis, conductivity measurement, infrared spectra and thermogravimetric analysis. The DNA-binding properties of the complexes have been investigated by fluorescence spectroscopy and viscosity measurements. The results suggest that the complexes can bind to DNA by partial intercalation. The liner Stern-Volmer quenching constant Ksq values are 3.3(+/-0.21)(1), 1.7(+/-0.19)(2) and 0.9(+/-0.04)(3), respectively. Complex (1) and (2) have been found to cleave pBR322 plasmid DNA at physiological pH and temperature. The test of antiproliferation activity indicates that complex(1) has strong antiproliferative ability against the SMMC7721 (IC50 = 131.7 +/- 23.4 micromol x L(-1)) and A549 (IC50 = 128.4 +/- 19.9 micromol x L(-1)) cell lines. The inhibition rates of complex(2) (IC50 = 86.3 +/- 11.3 micromol x L(-1)) are much higher than that of NCTD (IC50 = 115.5 +/- 9.5 micromol x L(-1)) and HL2 (111.0 +/- 5.7 micromol x L(-1)) against SMMC7721 cell lines.

摘要

三种新型配合物[Nd(L)(NO3)(H2O)2].NO(3).2H2O(HL1=N-嘧啶诺卡他汀酰基酰胺酸,C12H13N3O4;HL2=N-吡啶诺卡他汀酰基酰胺酸,C13H14N2O4;HL3=N-苯甲酰基诺卡他汀酰基酰胺酸,C14H15NO4)被合成。HL1、HL2 和 HL3 分别是配合物(1)、(2)和(3)的配体。它们的结构通过元素分析、电导率测量、红外光谱和热重分析进行了表征。通过荧光光谱和粘度测量研究了配合物的 DNA 结合性质。结果表明,配合物可以通过部分嵌入与 DNA 结合。线性 Stern-Volmer 猝灭常数 Ksq 值分别为 3.3(+/-0.21)(1)、1.7(+/-0.19)(2)和 0.9(+/-0.04)(3)。配合物(1)和(2)在生理 pH 和温度下能够切割 pBR322 质粒 DNA。增殖活性测试表明,配合物(1)对 SMMC7721(IC50=131.7 +/- 23.4 micromol x L(-1))和 A549(IC50=128.4 +/- 19.9 micromol x L(-1))细胞系具有很强的增殖抑制能力。配合物(2)(IC50=86.3 +/- 11.3 micromol x L(-1))的抑制率远高于 NCTD(IC50=115.5 +/- 9.5 micromol x L(-1))和 HL2(111.0 +/- 5.7 micromol x L(-1))对 SMMC7721 细胞系的抑制率。

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