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新型的去甲斑蝥酸根合镨(Ⅲ)、钐(Ⅲ)配合物的晶体结构、与DNA和BSA的作用及抗增殖活性 被引量:4

Crystal Structure,Interaction with DNA and Protein and Antiproliferative Activities of Pr( Ⅲ) and Sm( Ⅲ) Novel Complexes of Demethylcantharate
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摘要 合成了两种2-氨甲基苯并咪唑(ambi)和去甲基斑蝥酸(H2DCA=7-氧杂二环[2.2.1]庚烷-2,3-二甲酸)与镨(Ⅲ)、钐(Ⅲ)的配合物。应用元素分析、摩尔电导、红外光谱及X射线单晶衍射法对配合物的组成和结构进行了表征,配合物的组成为:(Hambi)[Ln(DCA)2(H2O)3]·3H2O(Ln=Pr(III)(1),Sm(III))(2);Hambi为质子化的ambi。DCA离子的醚键和羧酸根的氧原子参与配位,为三齿配体,稀土离子的配位数为9。通过紫外光谱法、荧光光谱法和粘度法研究了配合物与DNA和牛血清白蛋白(BSA)的相互作用。结果表明:配合物能通过部分插入模式与DNA发生较强的结合作用(Kb:1.56×104(1)和1.85×104L·mol-1(2))。配合物能与BSA发生强烈的相互作用(KA:9.33×104L·mol-1(1)和1.52×106L·mol-1(2)),结合位点数为1。测试了配合物对人肝癌细胞(SMMC7721)的体外抗增殖活性。结果显示,配合物的抗癌活性较去甲基斑蝥素有明显提高。 Two novel complexes( Hambi) [Pr( DCA)2( H2O)3]·3H2O( 1) and( Hambi) [Sm( DCA)2( H2O)3]·3H2O( 2)( DCA = 7-oxabicyclo [2. 2. 1]heptane-2,3-dicarboxylate,demethylcantharate,C8H8O5; Hambi =protonated 2-aminomethylbenzimidazole,C8H10N3) were first synthesized and characterized by elemental analysis,infrared spectra and thermogravimetric analysis and X-ray diffraction. The rare earth ion was nine-coordinated by three oxygen atoms from three coordinated water,two bridging oxygen atoms and four oxygen atoms of carboxylate radical from two demethylcantharates. The DNA binding properties of the complexes were investigated by electronic absorption spectra,fluorescence spectra and viscosity measurements. The complexes could bind to DNA with moderate intensity via partial intercalation mode. Meanwhile,the binding intensity of complex with bovine serum albumin( BSA) was high. The experimental results showed that the complexes and BSA formed a 1∶ 1 compound with conformational changes in BSA. The antiproliferative activities of the complex Pr and Sm against human hepatoma cells( SMMC7721) were tested with MTT assay in vitro. The results showed that the antiproliferative activities of the complexes against the cells were more intense than Na2( DCA).
出处 《中国稀土学报》 CAS CSCD 北大核心 2014年第4期473-481,共9页 Journal of the Chinese Society of Rare Earths
关键词 苯并咪唑 去甲基斑蝥酸 稀土配合物 与DNA键合 与BSA相互作用 体外抗增殖活性 benzimidazole demethylcantharidin rare earth complexes DNA binding interaction with BSA antiproliferative activities
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