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从大青叶中分离出的四种天然化合物:晶体结构与抗菌活性

Four Natural Compounds Separated from Folium Isatidis: Crystal Structures and Antibacterial Activity.

作者信息

Liao Bei-Ling, Pan Yu-Jie, Zhang Wei, Pan Li-Wei

机构信息

School of Chemistry and Biological Engineering, Hechi University, Yizhou, 546300, P. R. China.

出版信息

Chem Biodivers. 2018 Jul;15(7):e1800152. doi: 10.1002/cbdv.201800152. Epub 2018 Jun 12.

Abstract

Four natural compounds were obtained by concentrating, separating and purifying from the Folium isatidis. These natural compounds have been characterized by elemental analysis, IR spectrum, NMR and single-crystal X-ray diffraction analysis. The results show that these natural compounds are 4(3H)-quinazolinone (I), 2,4(1H,3H)-quinazolinedione (II), methyl 3,4-dihydro-4-oxoquinazoline-2-carboxylate (III) and ethyl 3,4-dihydro-4-oxoquinazoline-2-carboxylate (IV). The antibacterial activity experiment showed that I and II had better activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis and Salmonella than III, IV and other multiple components, because III and IV have long branches and steric hindrance effect. Compounds I and II have planar structure, which can more easily combine with these bacteria and kill them. The above results have good guiding significance for studying the antibacterial activity for single components or mixtures from natural origin.

摘要

通过对大青叶进行浓缩、分离和纯化,得到了四种天然化合物。这些天然化合物已通过元素分析、红外光谱、核磁共振和单晶X射线衍射分析进行了表征。结果表明,这些天然化合物分别为4(3H)-喹唑啉酮(I)、2,4(1H,3H)-喹唑啉二酮(II)、3,4-二氢-4-氧代喹唑啉-2-羧酸甲酯(III)和3,4-二氢-4-氧代喹唑啉-2-羧酸乙酯(IV)。抗菌活性实验表明,与III、IV及其他多种成分相比,I和II对金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌和沙门氏菌具有更好的活性,因为III和IV具有较长的支链和空间位阻效应。化合物I和II具有平面结构,能够更轻松地与这些细菌结合并将其杀灭。上述结果对于研究天然来源的单一成分或混合物的抗菌活性具有良好的指导意义。

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