| 镍(Ⅱ)、镉(Ⅱ)与去甲基斑蝥酸钠和咪唑配合物的结构、与DNA/BSA的作用及抗增殖活性 | |
| Structures, Interaction with DNA and BSA and Antiproliferative Activities of Ni(Ⅱ) and Cd(Ⅱ) Complexes Based on Demethylcantharate and Imidazole | |
| 摘要: 以2种配体去甲基斑蝥酸钠(Na2DCA=7-氧杂二环[2.2.1]庚烷-2,3-二甲酸钠)和咪唑(IM),分别与镍(Ⅱ)和镉(Ⅱ)的醋酸盐通过溶液法合成了2种配合物[Ni(IM)(DCA)(H2O)2]·2H2O (1),[Cd2(IM)4(DCA)2]·2H2O (2)。应用元素分析、热重分析、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1与2的中心离子分别与咪唑的亚胺氮原子、去甲基斑蝥酸根的羧基氧原子和醚键氧原子配位,配位数均为6,分别为单核(1)和双核(2)配合物。通过紫外光谱法、荧光光谱法和粘度法研究了配合 物与DNA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:5.51×103 (2)、1.01×103 (2) L·mol-1)。同时,利用荧光光谱法研究了配合物与牛血清白蛋白(BSA)的相互作用。配合物能与BSA发生强烈的相互作用(KA:1.91×105 (1)和6.17×105 (2) L·mol-1),结合位点数均为1。测试了配合物对人肝癌细胞(SMMC7721)和人乳腺癌(MCF-7)的体外抗增殖活性。结果显示,配合物对不同癌细胞具有选择性抑制作用。镍配合物(1)对SMMC7721的抗癌活性较去甲基斑蝥酸钠有明显提高。 | |
| 关键词: 咪唑 去甲基斑蝥酸钠 镍配合物 镉配合物 与DNA和BSA相互作用 体外抗增殖活性 | |
| 基金项目: 国家自然科学基金(No．)资助项目 | |
| Abstract: Two mixed-ligand complexes [Ni(IM)(DCA)(H2O)2]·2H2O (1) and [Cd2(IM)4(DCA)2]·2H2O (2) (DCA=demethylcantharate, 7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylate, C8H8O5; IM=imidazole, C3H4N2) were synthesized and characterized by elemental analysis, infrared spectra, thermogravimetric analysis, and X-ray diffraction. Complex 1 was a mononuclear molecule, with Ni(Ⅱ) ion six-coordinated by one nitrogen atom from imidazole, three oxygen atoms from DCA and two water molecules. The complex 1 crystallized in the monoclinic crystal system with P21/m. Complex 2 was a binuclear molecule, each Cd(Ⅱ) ion was six-coordinated by two nitrogen atoms from two imidazole, one ether oxygen atom and three oxygen atoms of carboxyl groups from DCA. The complex 2 crystallized in the triclinic crystal system with P1 space group. The DNA binding properties of the complexes were investigated by electronic absorption spectra, fluorescence spectra and viscosity measurements. These two complexes could bind to DNA with moderate intensity via partial intercalation. The binding constants Kb were 5.51×103 (1) and 1.01×103 L·mol-1 (2) at 298 K, respectively. Meanwhile, the binding intensity of complex with bovine serum albumin (BSA) is high, with binding constants KA equal to 1.91×105 (1) and 6.17×105 L·mol-1 (2), respectively. Experimental results showed that complexes and BSA formed a 1:1 compound with conforma-tional changes in BSA. The antiproliferative activities of the complex (1) against human hepatoma cells (SMMC7721) lines and human breast cancer cells (MCF-7) lines were tested with MTT assay in vitro. The results showed that the inhibition effect had selectivity against cancer cells after forming complexes. The antiproliferative activities of the complex (IC50=(86.8±6.1) μmol·L-1) against the human hepatoma cells lines was more intense than Na2(DCA) (IC50=(152.8±15.6) μmol·L-1), which suggests potential application in anti-cancer drug development. CCDC: 822330, 1; 822328, 2. | |
| Keywords: imidazole disodium demethylcantharate nickel complex cadmium complex interaction with DNA and BSA antiproliferative activity | |
| 投稿时间：2014-10-20 修订日期：2015-01-13 | |
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| 杜芳园,李士坤,林秋月,魏琼,汤宁宁.镍(Ⅱ)、镉(Ⅱ)与去甲基斑蝥酸钠和咪唑配合物的结构、与DNA/BSA的作用及抗增殖活性[J].无机化学学报,2015,31(4):813-823. | |
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