新木荷齐墩果烷型三萜皂甙结构修饰及其与抗稻瘟病菌活性的构效关系研究

项目名称： 新木荷齐墩果烷型三萜皂甙结构修饰及其与抗稻瘟病菌活性的构效关系研究

项目编号： No.21266010

项目类型： 地区科学基金项目

立项/批准年度： 2013

项目学科： 化学工业

项目作者： 霍光华

作者单位： 江西农业大学

项目金额： 50万元

中文摘要： 现行生产上防治水稻灾难性病害稻瘟病主要使用的化学药剂三环唑和富士一号，已经存在环境残留和病原抗药性，开发能减少对环境危害和有效控制病原生物的安全性新型天然产物农药已成为占领国际农药市场的一种发展趋势。 我们在前期研究中分离获得并鉴定出两种具有强抗稻瘟病菌活性的新的木荷齐墩果烷型三萜皂甙，并注意到以此类化合物为基础，进行结构修饰，对提高其抗稻瘟病菌活性和降低使用剂量较为有利。 基于此，本研究拟以木荷该类皂甙为起始物，有针对性地对其进行酶解、酸解、碱解，乙酰化、糖苷化等结构修饰，分离制取各衍生化次级皂甙单体，测定各单体抑制稻瘟病菌菌丝生长、孢子萌发和附着胞产生的活性，揭示其皂甙结构与抗稻瘟病菌活性的构效关系和规律，为开发皂甙类新型杀稻瘟剂奠定基础。

中文关键词： 齐墩果烷（酸）皂甙；糖基化及化学转化；抗稻瘟病菌活性；构效关系；先导物

英文摘要： Chemicals tricyclazole and Fuji-one (isoprothiolane) used on the production of rice as current prevention and treatment of catastrophic diseases in rice blast have already existed environmental residue and pathogen resistance. It has become a trend of occupation international pesticide market to develop safety new natural product fungicides with little environmental harm and effective control of pathogens. We acquired in preliminary studies and identified two new oleanane triterpenoid saponins of Schima superba with strong antifungal activity to rice blast pathogen, and noticed that structural modification on the basis of such compounds to improve its antifungal activity and lower doses is more favourable. Based on this, the research intends to carry out enzyme hydrolysis, acid hydrolysis, and alkali hydrolysis, acetylation and glycosidation of Schima superba saponins, separate derivative secondary saponin monomers, determine their activities in resisting blast mycelium growth, spores germination and appressorium formation. The overall objective of the study is to investigate the relationship and law between these saponin structures and resisting blast activities for development a new blasticide of saponins.

英文关键词： oleanane (oleanolic) saponin；glycosylation and chemical transformation；activities resisting M. oryzae；structure-activity relationship；lead compounds