多酸基复合物的设计合成及生物活性研究

发布时间：2018-05-29 10:17

本文选题：多酸 + 吡哌酸　；参考：《佳木斯大学》2014年硕士论文

【摘要】：目的设计合成出新型的多酸基复合物，对其进行结构表征及生物进行研究。探索复合物的合成规律，研究其构效关系。方法复合物的合成采用水热合成法；通过X-射线单晶衍射、X-射线粉粉末衍射、元素分析、差热-热重和红外光谱等方法对晶体进行结构表征。利用紫外光谱法研究复合物与DNA的相互作用；采用药敏纸片法研究复合物抗菌活性；利用MTT法研究新型复合物的体外抗肿瘤活性。结果合成出4个新的有机活性分子修饰的多酸复合物；复合物能够与DNA发生相互作用，得到了配合物与DNA的作用模式和相应的结合常数；复合物有一定的抗菌活性和抗肿瘤活性。结论本论文选择喹诺酮类药物分子吡哌酸和唑类杂环分子作为有机配体，在过渡金属阳离子存在下，借助配位键或分子间相互作用来剪切、修饰或者桥连多酸基本单元，进而构建新型的多酸基复合物。研究这类新型复合物的合成规律，探索其微观结构与宏观性质之间的联系。制备并表征了4种新型的多酸基复合物，确定分子式如下： {[Cu（PPA）2]2[H3PMo12O40]}·8H2O （1）； {[Zn（PPA）2][H3PMo12O40]}·[HPPA]·3H2O （2）； {[Zn（HPPA）2H2O]2[H2ZnW12O40]}.9H2O （3）； [Ag3（pytz）2（H2O）]2·[HAgGeMo12O40]·H2O （4）。复合物与DNA相互作用的实验结果表明，复合物1-3与DNA具有强的作用力，紫外光谱实验证明他们与DNA的结合模式为嵌插结合。体外抗肿瘤实验发现药物配体自身的性质，，多酸自身的构型和配位模式，复合物的结构等许多因素都可能影响复合物的抗肿瘤活性，即多酸和药物分子之间的协同作用调节了抗肿瘤活性，其中金属离子对于电子在多酸与金属配合物的转移起到了关键作用。抗菌实验结果表明复合物1-4对金黄葡萄球菌和大肠杆菌有明显的抑制作用，其抑菌活性来源与金属离子Ag和药物吡哌酸分子。由于复合物不溶于水可以作为新型固体抗菌材料。
[Abstract]:Objective to design and synthesize a novel polyacid complex and study its structure and biology. To explore the synthesis law of the complex and study its structure-activity relationship. Methods the complex was synthesized by hydrothermal method, and the crystal structure was characterized by X-ray single crystal diffraction powder diffraction, elemental analysis, differential thermogravimetry and infrared spectroscopy. The interaction between the complex and DNA was studied by ultraviolet spectroscopy, the antibacterial activity of the complex was studied by drug sensitive disk method, and the antitumor activity of the new complex was studied by MTT in vitro. Results four new organic active molecular modified polyacid complexes were synthesized, which could interact with DNA, and the interaction mode and binding constants of the complexes with DNA were obtained. The complex has certain antibacterial activity and anti-tumor activity. Conclusion Quinolones were selected as organic ligands. In the presence of transition metal cations, the basic units of polyacids were cut, modified or bridged by coordination bonds or intermolecular interactions. Then a new polyacid complex was constructed. The synthesis law of this kind of new complex is studied, and the relation between its microstructure and macroscopic properties is explored. Four novel polyacid-group complexes were prepared and characterized, and the molecular formula was as follows: {[Cu(PPA)2] 2 [H3PMo12O40]} 8H2O 1; {[Zn(PPA)2] [H3PMo12O40]} [HPPA] 3H2O; {[Zn(HPPA)2H2O] 2 [H2ZnW12O40]}. [Ag3PYTZZZZZZZZZHZ H _ 2O] _ 2 [HAgGeMo12O40] H _ 2O _ (4) H _ 2O _ 4. The experimental results of interaction between complex and DNA show that complex 1-3 has strong interaction with DNA. UV spectra show that their binding mode with DNA is intercalation binding. In vitro antitumor experiments showed that many factors, such as the properties of drug ligands, the configuration and coordination pattern of polyacids, the structure of complexes and so on, may affect the antitumor activity of the complexes. The synergistic action between polyacid and drug molecules regulates the antitumor activity of which metal ions play a key role in the transfer of electrons in polyacid and metal complexes. The results of antibacterial test showed that complex 1-4 had obvious inhibitory effect on Staphylococcus aureus and Escherichia coli, and its antibacterial activity was derived from metal ion Ag and pyrrolidic acid molecule. Because the complex is insoluble in water, it can be used as a new solid antibacterial material.
【学位授予单位】：佳木斯大学
【学位级别】：硕士
【学位授予年份】：2014
【分类号】：R914.5;R96

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