Discovery of gamma-Lactam Alkaloid Derivatives as Potential Fungicidal Agents Targeting Steroid Biosynthesis

文献类型： 外文期刊

第一作者： Huang, Daye

作者： Huang, Daye;Huang, Wenbo;Ke, Shaoyong;Wang, Shuangshuang;Song, Di;Cao, Xiufang

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关键词： gamma-lactams; synthesis; bioassay; oomycetes; P. capsici; P. aphanidermatum; proteomic profile

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：5.279； 五年影响因子：5.269 ）

ISSN： 0021-8561

年卷期： 2020 年 68 卷 49 期

页码：

收录情况： SCI

摘要： Biological control of plant pathogens is considered as one of the green and effective technologies using beneficial microorganisms or microbial secondary metabolites against plant diseases, and so microbial natural products have played important roles in the research and development of new and green agrochemicals. To explore the potential applications for natural gamma-lactam alkaloids and their derivatives, 26 gamma-Iactams that have flexible substituent patterns were synthesized and characterized, and their in vitro antifungal activities against eight kinds of plant pathogens belonging to oomycetes, basidiomycetes, and deuteromycetes were fully evaluated. In addition, the high potential compounds were further tested using an in vivo assay against Phytophthora blight of pepper to verify a practical application for controlling oomycete diseases. The potential modes of action for compound DI against Phytophthora capsici were also investigated using microscopic technology (optical microscopy, scanning electron microscopy, and transmission electron microscopy) and label-free quantitative proteomics analysis. The results demonstrated that compound DI may be a potential novel fungicidal agent against oomycete diseases (EC50 = 4.9748 mu g-mL(-1) for P. capsici and EC50 = 5.1602 mu g.mL(-1) for Pythium aphanidermatum) that can act on steroid biosynthesis, which can provide a certain theoretical basis for the development of natural lactam derivatives as potential antifungal agents.

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