一种丹皮酚衍生物的合成及其抗菌活性

一种丹皮酚衍生物的合成及其抗菌活性 Synthesis and Antimicrobial Activity of a Paeonol Derivative 赖普辉 LAI Puhui 1 first-author 田光辉 TIAN Guanghui 1 赵桦 ZHAO Hua 1 陕西理工学院化学与环境科学学院 陕西理工学院化学与环境科学学院 School of Chemistry and Environmental Sciences,Shaanxi University of Technology School of Chemistry and Environmental Sciences,Shaanxi University of Technology 用水蒸气蒸馏法从中药丹皮中提取丹皮酚进行精制,将其与间硝基苯甲醛在室温下发生羟醛缩合反应,合成出一种新型丹皮酚衍生物3-羟基-1-（2′-羟基-4′-甲氧基苯）-3-（3-硝基）苯-1-丙酮,产率可达75.1%.对其结构借助红外光谱、X-射线衍射分析、核磁共振谱、135°脉冲核磁共振碳谱和元素分析进行综合表征.抗菌实验研究表明,丹皮酚及其衍生物对所选实验菌株均有明显的抑制和灭活作用,其中对福氏志贺菌51065株的最小抑菌浓度（MIC）分别为0.10g/L和0.04g/L,对伤寒沙门菌50127株的MIC值分别为0.06g/L和0.02g/L,较其他菌株更为显著. Paeonol from traditional Chinese herb medicine of Paeonia Suff ruicosa was extracted by steam distillation,and then refined.A paeonol’s derivative named 3-hydroxy-1-（2’-hydroxy-4’-methoxyphenyl）-3-（3-nitrophenyl）propen-1-one was synthesized by aldol condensation reaction with paeonol and mnitro-benzaldehyde under room temperature,and its yield reached up to 75.1%.3-hydroxy-1-（2’-hydroxy4’-methoxyphenyl）-3-（3-nitrophenyl）propen-1-one had been identified by IR spectra,X-ray structure analysis,1 H NMR,13C NMR,135°DEPT（distortionless enhancement by polarization transfer）and elemental analyses.The results of the antimicrobial activities of paeonol and its derivative show that by inhibiting the growth of testing bacteria and sterilizing them,MICs on Shigella flexneri 51065were 0.10g/L and 0.04 g/L,MICs on Salmonella typhi 50127were 0.06g/L and 0.02g/L,respectively.So Paeonol and its derivative showed higher antimicrobial activity especially against Shigella flexneri 51065and Salmonella typhi 50127. 丹皮酚 合成 羟醛缩合反应 抗菌活性 paeonol synthesis aldol condensation reaction antimicrobial activity 10.14188/j.1671-8836.2010.05.010 TQ461 陕西省教育厅专项科研计划项目（04JK137）;陕西理工学院科技创新教改项目（XJG0726） 2010-05-01 2021-04-01 5 56