内生真菌拟盘多毛孢中新颖农药潜在先导结构的发现及活性筛选

It is vitually important in practice and strategy for discovering new pesticides with independent intellectual property rights from natural products. As one of large groups of endophytic fungi, Pestalotiopsis is rich, diverse and novel in metabolities, which provide possibility for discovering new pesticides of bioactive lead compounds.In the past several years, applicant focused mainly on the field of pesticides lead compounds from the fungi of unique ecological niches. During the course of screening the fungi strains with pesticide activities from Pestalotiopsis, more than 20 strains with high activity of pesticides were discoveried. This project is trying to find new compounds with pesticide activity from over 20 Pestalotiopsis strains by means of phytochemistry combined with bioassay method. These new compounds will be isolated and chemically characterized. They will be tested pesticide activity against phytopathogenic fungi,pests and weeds in vitro and in vivo. It can be expected that 20-30 new bioactive compounds will be isolated and identified with a combination of pesticide activity bioassay. In further research, 1-2 potential lead compounds will be evaluated as potential pesticide lead compounds.

从内生真菌中发现新奇结构的高活性农药活性分子对于创制我国具有自主知识产权的新型农药具有现实和战略意义。拟盘多毛孢作为内生真菌的大类群之一，次生代谢产物丰富多样且新颖，这为发现新的农药潜在先导结构提供了更大的可能性。申请者长期致力于真菌化学及农药先导结构的发现及活性评价研究，在对拟盘多毛孢内生真菌活性初筛过程中，发现20种(株)具有明显的杀虫、抑菌或除草活性。本项目以筛选的20种(株)拟盘多毛孢为研究对象，以粘虫、菜青虫为供试昆虫，10种植物病原菌为供试菌种，10种农田杂草为目标植物，采用常规发酵法和单菌多次级代谢产物(OSMAC)方法扩大培养，并优化培养发酵条件；采用生物活性和化学分离相结合的方法继续分离活性成分，并进行结构鉴定，发现结构新颖的活性物质20-30个；对所分离的化合物进行活性测试，评价其作为农药先导结构的可能性，争取发现1-2个值得进一步研究的潜在农药先导结构。

从内生真菌中发现新奇结构的高活性农药活性分子对于创制我国具有自主知识产权的新型农药具有现实和战略意义。拟盘多毛孢作为内生真菌的大类群之一，次生代谢产物丰富多样且新颖，这为发现新的农药潜在先导结构提供了更大的可能性。本项目以筛选的21种(株)拟盘多毛孢为研究对象，并优化培养发酵条件；采用生物活性和化学分离相结合的方法继续分离活性成分，并进行结构鉴定，分离鉴定了180个化合物，其中新结构化合物22个；在此基础上，对其进行活性测试和评价，发现了2个高活性的农药活性源头分子acetoxydehydroaustin A和pestalachloride C可作为新型农用抗生素的先导结构。