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合成了2-乙基-3-(3-硝基苯基)喹唑啉-4-酮(ENPQO),用紫外光谱法、荧光光谱法、荧光偏振法、离子强度法及分子模拟法研究了ENPQO与小牛胸腺DNA(ct DNA)的相互作用。紫外光谱法显示ct DNA与ENPQO作用后,引起ENPQO紫外吸收光谱的增色效应;在以吖啶橙(AO)为荧光探针的实验中,随着ENPQO浓度的增加,ct DNA-AO体系的荧光被猝灭,其猝灭过程主要是静态猝灭,ENPQO对ct DNA-AO体系的荧光偏振基本无影响;不同浓度的Na Cl溶液未削弱ENPQO对ct DNA-AO的猝灭程度。以上结果均表明ENPQO与ct DNA之间的作用方式主要为沟槽结合。利用分子模拟对接技术预测了ENPQO与ct DNA的结合最优构象,与光谱实验结果一致。
Synthesis of 2-ethyl-3- (3-nitrophenyl) quinazolin-4-one (ENPQO) was studied by ultraviolet spectroscopy, fluorescence spectroscopy, fluorescence polarization, ionic strength and molecular modeling Interaction of ENPQO with calf thymus DNA (ct DNA). Ultraviolet spectroscopy showed that the effect of ct DNA and ENPQO induced the potentiation of ENPQO UV absorption spectrum. In the experiment of acridine orange (AO) as a fluorescent probe, the fluorescence of ct DNA-AO system increased with the increase of ENPQO concentration Quenching, the quenching process is mainly static quenching, while ENPQO has no effect on the fluorescence polarization of ct DNA-AO system. Different concentrations of NaCl solution do not weaken the quenching of ct DNA-AO by ENPQO. The above results indicate that the main mode of action between ENPQO and ct DNA is trench binding. The optimal conformation of ENPQO and ct DNA was predicted by molecular simulation docking technique, which was in good agreement with the experimental results.