姜黄素烷基化衍生物的合成及对朱砂叶螨的活性评价

姜黄素具有多种生物活性,结构修饰有利于提高其生物利用度及选择活性.实验以姜黄素与二溴乙烷反应,在其二酮结构的中间亚甲基位引入官能团,合成了3种化合物,其收率最高为53.00%,最低收率为5.50%.经室内毒力测定结果显示,3种化合物对朱砂叶螨均有一定的触杀效果,其中CM01在浓度为1.89 mg/mL时,其24 h、48 h对朱砂叶螨的校正死亡率分别为60.45%,80.45%,对应LC50为1.279 0 mg/mL、0.392 2 mg/mL;而姜黄素在浓度为5.0 mg/mL时,24 h、48 h对朱砂叶螨的死亡率分别为20.40%,50.8%,LC50依次为24.570 1 mg/mL和2.637 7 mg/mL. CM01对朱砂叶螨的杀螨活性较姜黄素有明显提高.

Abstract：

Curcumin has been reported to possess many bioactivities, and structure modification may help improve its bioavailability and selectivity. In the present study, 3 alkylation derivatives were synthesized in laboratory with the reaction between curcumin and bromoethane in the middle of its methylene-introduction of alkyl, their yields being in the range of 5.50%-53.00%. Bioassay in laboratory showed that all the four compounds had certain acaricidal activity. In treatments with the derivative CM01 at the concentration of 1.89 mg/mL for 24 h and 48 h, the corrected mortality against Tetranychus cinnabarinus was 60.45%and 80.45% and the LC50 was 1. 279 0 mg/mL and 0. 392 2 mg/mL, respectively. In contrast, treatments with curcumin at the concentration of 5.0 mg/mL for 24 and 48 h, the corrected mortality against T. cinnabarinus was 20.40% and 50.8% and the LC50 was 24. 570 1 mg/mL and 2. 637 7 mg/mL, respectively.It is thus concluded that the acaricidal activity of CM01 is markedly improved as compared with that of curcumin.

Synthesis of Three Alkylation Derivatives of Curcumin and Their Acaricidal Activity Evaluation