天然产物药物发现：发现作为新型植物病毒抑制剂的Gramines。
Natural Products for Drug Discovery: Discovery of Gramines as Novel Agents against a Plant Virus.
机构信息
School of Chemical Engineering and Technology, Hebei Collaborative Innovation Center of Modern Marine Chemical Technology , Hebei University of Technology , Tianjin 300130 , China.
Tianjin Key Laboratory of Structure and Performance for Functional Molecules, MOE Key Laboratory of Inorganic-Organic Hybrid Functional Material Chemistry, College of Chemistry , Tianjin Normal University , Tianjin 300387 , China.
出版信息
J Agric Food Chem. 2019 Feb 27;67(8):2148-2156. doi: 10.1021/acs.jafc.8b06859. Epub 2019 Feb 15.
Plant viral diseases seriously affect crop yield and quality. The natural product gramine (1) and its simple structural analogues 2-35 were synthesized from indoles, amines, and aldehydes in one step. The antiviral effects of these alkaloids were evaluated systematically. Most of these compounds were found to have higher antiviral effects than commercial ribavirin for the first time. Especially compounds 22, 30, and 31 exhibited significantly higher effects than ningnanmycin, thereby emerging as novel antiviral leads for further optimization. The preliminary implementation indicated that these compounds likely inhibit the assembly of tobacco mosaic virus (TMV) by cross-linking TMV capsid protein. Gramine analogues were also found to have broad-spectrum fungicidal effects. Although gramine has been reported to have influence on germination and development of Erysiphe graminis, these compounds displayed no fungicidal effects against Blumeria graminis f. sp. tritici on wheat in our test. Some of these compounds also exhibited certain insecticidal activities.
植物病毒病严重影响作物的产量和质量。天然产物草菌碱（1）及其简单结构类似物 2-35 可由吲哚、胺和醛一步合成。系统评价了这些生物碱的抗病毒作用。这些化合物大多数首次被发现比商业利巴韦林具有更高的抗病毒活性。特别是化合物 22、30 和 31 表现出比宁南霉素更高的效果，因此成为进一步优化的新型抗病毒先导化合物。初步实施表明，这些化合物可能通过交联烟草花叶病毒（TMV）衣壳蛋白来抑制 TMV 的组装。草菌碱类似物还具有广谱的杀菌作用。尽管草菌碱已被报道对小麦白粉病菌的萌发和发育有影响，但在我们的测试中，这些化合物对小麦上的禾谷布氏白粉病菌没有杀菌作用。其中一些化合物还表现出一定的杀虫活性。
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