CAJ | 학술논문

本文以邻香草醛缩胡椒乙胺席夫碱(L)为配体,合成一种新的席夫碱-锌(Ⅱ)双核配合物[Zn2(L)2 Cl2](1),并通过谱学分析及 X 射线单晶衍射分析对配合物1进行结构表征,通过 MTT 法测试配合物1及 L 对6种人肿瘤细胞株和人正常肝细胞株 HL-7702的体外增殖抑制活性。结果显示,配合物1 对所有肿瘤株的增殖抑制率均高于配体,但低于顺铂；对 HL-7702,其细胞毒性也远低于顺铂,且略低于配体,表现出一定的细胞毒性选择性。在分子水平上,通过荧光光谱法和凝胶电泳实验研究配合物1 及 L 与 DNA 的作用机制。结果显示,配合物1 以经典插入方式与 DNA 结合,而 L 对 DNA 的插入作用弱,表明柔性配体 L 与锌(Ⅱ)配位后,芳香平面结构刚性增强,使配合物1 对 DNA 插入作用增强,从而能够通过阻碍肿瘤细胞 DNA复制而表现显著高于 L 的抗肿瘤活性。
본문이린향초철축호초을알석부감(L)위배체,합성일충신적석부감-자(Ⅱ)쌍핵배합물[Zn2(L)2 Cl2](1),병통과보학분석급 X 사선단정연사분석대배합물1진행결구표정,통과 MTT 법측시배합물1급 L 대6충인종류세포주화인정상간세포주 HL-7702적체외증식억제활성。결과현시,배합물1 대소유종류주적증식억제솔균고우배체,단저우순박；대 HL-7702,기세포독성야원저우순박,차략저우배체,표현출일정적세포독성선택성。재분자수평상,통과형광광보법화응효전영실험연구배합물1 급 L 여 DNA 적작용궤제。결과현시,배합물1 이경전삽입방식여 DNA 결합,이 L 대 DNA 적삽입작용약,표명유성배체 L 여자(Ⅱ)배위후,방향평면결구강성증강,사배합물1 대 DNA 삽입작용증강,종이능구통과조애종류세포 DNA복제이표현현저고우 L 적항종류활성。
2-(3,4-Methylenedioxyphenyl )ethylamine and 2-hydroxy-3-methoxybenzaldehyde were selected to synthesize a new Schiff base (L)as bioactive ligand.The reaction of L with ZnCl2 ??2 H 2 O af-forded the binuclear zinc(Ⅱ)complex (1),which was structurally characterized by IR,elemental analy-sis,ESI-MS,and single crystal X-ray diffraction analysis.The in vitro cytotoxicity of 1 against six hu-man tumor cell lines (A549,MDA-MB-231,HeLa229,MGC80-3,A375,BEL-7404)and HL-7702 nor-mal liver cell line was screened by MTT assay.The growth inhibition ratios of 1 were found to be higher than those of L against all the tumor cell lines,but lower than those of cisplatin.However,the cytotox-icity of 1 against HL-7702 was much lower than those of cisplatin,suggesting the cytotoxic selectivity of 1.On the molecular level,the DNA binding property of 1 as well as L was studied by fluorescence spec-troscopy and gel electrophoresis assay.The results indicated that complex 1 intercalatively bound with DNA,while the intercalative binding ability of L was very weak.It may be ascribed to the much more rigid aromatic planar structure of 1 than L,which will facilitate the intercalative binding of 1 with DNA to effectively block the DNA replications in tumor cells,and higher antitumor activity of 1 can be ob-tained than L.