姜黄素双肟酯衍生物的合成与生物活性研究

Study of the Synthesis and the Biological Activity of Curcumin Dioxime Ester Derivatives

采用生物活性因子拼接的方法将活性基团肟酯引入植物源活性化合物姜黄素中对其结构进行修饰,通过肟化、酰化、最后酯化合成目标化合物姜黄素二苯甲肟酯和姜黄素二对氯苯甲肟酯,其结构经IR和^1H NMR确证.初步生物活性测试结果表明：姜黄素和目标化合物在浓度为500mg/L条件下对6种植物病原菌的抑菌活性都较小,分别在1.6%-11.1%和-0.5%-15.2%之间;在浓度为1250mg/L时,目标化合物对朱砂叶螨的触杀效果较姜黄素显著提高.药剂处理后48h时,姜黄素对朱砂叶螨的校正死亡率为12.5%,目标化合物的校正死亡率在48.5%-82.6%之间;72h时,姜黄素对朱砂叶螨的校正死亡率上升为19.3%,而目标化合物的校正死亡率则高达92.4%-97.0%.

Curcumin was modified by active functional group oxime ester with biologically active factor splicing. Two novel compounds were synthesized through oximic reaction, esterify reaction and acylic reaction. Their structures were confirmed by IR and ^1H NMR. The results of preliminary bioassay indicated that curcumin and the target compounds exhibited low antifungal activities to six plant pathogens at the concentration of 500 mg/L, their antifungal rate being 1.6%-11.1% and -0.5%-15.2%, respectively. At higher concentration （1 250 mg/L）, their antifungal increased significantly. The target compounds exhibited significantly higher contact activities than curcumin to Tetranychus cinnabrinus. The corrected mortality after 48 h was 12.5% in the curcumin treatment and 48.5%-82.6% in target compound treatment, and rose to 19.3% and 92.4G-97.0G, respectively, after 72 h.