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Aspernigerin是从狗牙根内生菌Aspergillus niger IFB-E003的培养液中分离得到的天然产物,对癌细胞具有较强的活性.设计了一条全新的合成路线,以1,2,3,4-四氢喹啉和氯乙酰氯为主要原料,经过两步反应合成了Aspernigerin,总收率80.3%,较文献报道的合成路线的总收率提高了33%.首次对Aspernigerin进行农用生物活性测试,结果表明,Aspernigerin具有一定的杀菌、杀虫活性和除草活性,在600和200μg/mL的浓度下对小菜蛾的杀虫活性分别为100%和75%,在500μg/mL的浓度下对稗草、小麦、黄瓜的根、茎的生长抑制率都在90%以上.
Aspernigerin is a natural product isolated from the culture medium of Aspergillus niger IFB-E003, and has strong activity on cancer cells. A new synthetic route was designed, Hydroquinoline and chloroacetyl chloride as main raw materials, Aspernigerin was synthesized in two steps, the total yield was 80.3%, and the total yield was 33% higher than that reported in the literature.For the first time, Aspernigerin was tested for its agrobiological activity and the results The results showed that Aspernigerin had certain bactericidal, insecticidal and herbicidal activities. The insecticidal activities of Aspernigerin to Plutella xylostella were 100% and 75% respectively at 600 and 200μg / mL, The root and stem of wheat, cucumber growth inhibition rate of more than 90%.