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

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.