| 井冈羟胺A酯类衍生物的酶法合成及其生物活性 |
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| 引用本文： | 叶康,江瑞妮,苍涛,陆跃乐,陈小龙,范永仙.井冈羟胺A酯类衍生物的酶法合成及其生物活性[J].农药学学报,2021,23(5):869-876. |
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| 作者姓名： | 叶康 江瑞妮 苍涛 陆跃乐 陈小龙 范永仙 |
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| 作者单位： | 1.浙江工业大学 生物工程学院，杭州 310014 |
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| 基金项目： | 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) |
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| 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，EC50值为13.03 μmol/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。
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| 关 键 词： | 井冈羟胺A 酯类衍生物 脂肪酶催化 生物活性 |
| 收稿时间： | 2021-03-30 |
Enzymatic synthesis and biological activities of validoxylamine A ester derivatives |
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| Institution: | 1.College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, China2.College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China3.Institute of Agro-product Safety and Nutrition, Zhejiang Academy of Agricultural Sciences, Hangzhou 310021, China |
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| Abstract: | 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 by ⅠH NMR, 13C NMR and HRMS. The biological activities results showed that most of those compounds retained their inhibitory activity against Rhizoctonia solani. Compound Ⅰ had the best inhibitory effect, with the EC50 value of 13.03 μmol/L. Compound Ⅶ had 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. |
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