井冈羟胺A酯类衍生物的酶法合成及其生物活性  

Enzymatic synthesis and biological activities of validoxylamine A ester derivatives

作　　者：叶康 江瑞妮 苍涛[3] 陆跃乐 陈小龙[1] 范永仙 YE Kang;JIANG Ruini;CANG Tao;LU Yuele;CHEN Xiaolong;FAN Yongxian(College of Biotechnology and Bioengineering,Zhejiang University of Technology,Hangzhou 310014,China;College of Chemical Engineering,Zhejiang University of Technology,Hangzhou 310014,China;Institute of Agro-product Safety and Nutrition,Zhejiang Academy of Agricultural Sciences,Hangzhou 310021,China)

机构地区：[1]浙江工业大学生物工程学院,杭州310014 [2]浙江工业大学化学工程学院,杭州310014 [3]浙江省农业科学院农产品质量安全与营养研究所,杭州310021

出　　处：《农药学学报》2021年第5期869-876,共8页Chinese Journal of Pesticide Science

基　　金：浙江省重点研发计划项目(2019C02088);浙江省自然科学基金项目(LY19B060008);国家自然科学基金项目(21572206).

摘　　要：井冈羟胺A(validoxylamine A)作为重要的生物农药中间体具有抑菌和杀虫活性。为开发新型绿色农药,以井冈羟胺A作为先导化合物,通过脂肪酶催化酯化反应,合成了9个未见文献报道的井冈羟胺A酯类衍生物,通过核磁共振氢谱、碳谱以及高分辨质谱对其结构进行了表征。生物活性测定结果表明:大部分目标化合物对立枯丝核菌Rhizoctonia solani具有抑制活性,其中化合物Ⅰ的抑制效果最好,EC_(50)值为13.03μmol/L;化合物Ⅶ在500 mg/L下对豆蚜Aphis craccivora的致死率为64.60%。该类衍生物具有一定的抑菌、杀虫活性,有进一步研究的价值。Validoxylamine A is an important biopesticide intermediate with bacteriostatic and insecticidal activities.To discover new green pesticides,9 novel compounds were synthesized by lipase esterification reaction using validoxylamine A as the lead compound.Their structures were characterized byⅠH NMR,^(13)C NMR and HRMS.The biological activities results showed that most of those compounds retained their inhibitory activity against Rhizoctonia solani.CompoundⅠhad the best inhibitory effect,with the EC_(50) value of 13.03μmol/L.CompoundⅦhad a lethality of 64.60%to Aphis craccivora at 500 mg/L.This class of derivatives has fungicidal and insecticidal activities and is worthy of further study.

关 键 词：井冈羟胺A 酯类衍生物 脂肪酶催化 生物活性 

分 类 号：TQ450.1[化学工程—农药化工] O624.3[理学—有机化学]