一个戊二烯酮化合物的合成及其杀菌抗癌活性  

Synthesis and Biological Activity of(1E,4E)-1,5-bis(2-hydroxyphenyl)penta-1,4-dien-3-one

作　　者：黄银久[1,2] 许瑞卿[2,3] 吴守伟[1] 赵莉[1] 

机构地区：[1]蚌埠医学院生物科学系,安徽蚌埠233030 [2]贵州大学精细化工研究开发中心,"绿色农药与生物工程"教育部重点实验室,贵州贵阳550025 [3]中国海洋石油总医院,贵州贵阳550025

出　　处：《生物技术》2009年第3期76-78,共3页Biotechnology

基　　金：安徽省教育厅自然科学研究项目(2006KJ124C)资助

摘　　要：目的:合成戊二烯酮类化合物(1E,4E)-1,5-二(2-羟基苯基)-1,4-戊二烯-3-酮,并进行杀菌和抗肿瘤活性测定。方法:水杨醛和丙酮反应得到目标产物;采用生长速率法和MTT比色法分别测定了该化合物的杀菌抗癌活性。结果:目标物结构经元素分析、红外光谱、核磁共振氢谱确证;该化合物在500μg/mL浓度下对小麦赤霉病原菌、辣椒枯萎病原菌、苹果腐烂病原菌的抑制率分别为73.0%±3.3%、70.4%±1.5%、79.2%±2.1%;在5.0μmol/L下对PC-3细胞的72h的体外抑制率为71.4%±2.7%。结论:该化合物有较好的杀菌抗癌活性,可以以它为先导进行结构优化,以期设计、合成出高效、选择性好的同类化合物。Objective：To synthesize （1E,4E） - 1,5 - bis（2 - hydroxyphenyl）penta- 1,4 - dien- 3 - one and evaluate its biological activity. Method：Title compound was synthesized by the reaction of salicylal, and propanone, and its fungicidal and antitumor activities were tested through growth rate method and MTT colorimetrie assay respectively. Result：The compound structure was confirmed by elemental analysis, IR, ^1H NMR. It displayed good fungicidal activity against Fusarium graminearum, Fusarium oxysporum, Cytospora mandshurica at the concentration of 500μg/mL with 73.0% ＋ 3.3%, 70.4% ＋ 1.5% and 79.2% ＋ 2.1% respectively and its in vitro inhibition rate toward PC - 3 cell at 5.0μmol/L within 72h was 71 .4% ＋ 2.7%. Conclusion：Title compound showed certain fungicidal and antitumor activities and could be used as lead compound for designing, synthesizing novel drug with significant biological activity.

关 键 词：(1E 4E)-1 5-二(2-羟基苯基)-1 4-戊二烯-3-酮 杀菌活性 抗肿瘤活性 

分 类 号：TQ460.1[化学工程—制药化工]