PDF(Pubmed)
Abstract：
Natural products are a major source of biological molecules. The 3-methylfuran scaffold is found in a variety of plant secondary metabolite chemical elicitors that confer host-plant resistance against insect pests. Herein, the diversity-oriented synthesis of a natural-product-like library is reported, in which the 3-methylfuran core is fused in an angular attachment to six common natural product scaffolds-coumarin, chalcone, flavone, flavonol, isoflavone and isoquinolinone. The structural diversity of this library is assessed computationally using cheminformatic analysis. Phenotypic high-throughput screening of β-glucuronidase activity uncovers several hits. Further in vivo screening confirms that these hits can induce resistance in rice to nymphs of the brown planthopper Nilaparvata lugens. This work validates the combination of diversity-oriented synthesis and high-throughput screening of β-glucuronidase activity as a strategy for discovering new chemical elicitors.
摘要：
天然产物是生物分子的主要来源。3-甲基呋喃支架存在于多种植物次生代谢产物化学引发剂中,其赋予宿主植物对昆虫害虫的抗性。在这里，据报道，面向多样性的天然产物类库的合成，其中3-甲基呋喃核与六种常见的天然产物支架香豆素成角度地融合，查尔酮,黄酮,黄酮醇，异黄酮和异喹啉酮。使用化学信息学分析以计算方式评估该库的结构多样性。β-葡糖醛酸苷酶活性的表型高通量筛选揭示了几个命中。进一步的体内筛选证实，这些命中可以诱导水稻对褐飞虱Nilapavatalugens若虫的抗性。这项工作验证了以多样性为导向的合成与β-葡糖醛酸糖苷酶活性的高通量筛选相结合，作为发现新化学激发子的策略。
