National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, China.
Pest Manag Sci. 2023 Jul;79(7):2556-2570. doi: 10.1002/ps.7433. Epub 2023 Mar 14.
Plant pathogens have led to large yield and quality losses in crops worldwide. The discovery and study of novel agrochemical alternatives based on the chemical modification of bioactive natural products is a highly efficient approach. Here, two series of novel cinnamic acid derivatives incorporating diverse building blocks with alternative linking patterns were designed and synthesized to identify their antiviral capacity and antibacterial activity.
The bioassay results demonstrated that most cinnamic acid derivatives had excellent antiviral competence toward tobacco mosaic virus (TMV) in vivo, especially compound A (median effective concentration [EC ] = 287.7 μg mL ), which had a notable protective effect against TMV when compared with the commercial virucide ribavirin (EC = 622.0 μg mL ). In addition, compound A had a protective efficiency of 84.3% at 200 μg mL against Xac in plants. Given these outstanding results, the engineered title compounds could be regarded as promising leads for controlling plant virus and bacterial diseases. Preliminary mechanistic studies suggest that compound A could enhance the host's defense responses by increasing the activity of defense enzymes and upregulating defense genes, thereby suppressing phytopathogen invasion.
This research lays a foundation for the practical application of cinnamic acid derivatives containing diverse building blocks with alternative linking patterns in pesticide exploration. © 2023 Society of Chemical Industry.
植物病原体已导致全球农作物产量和品质的大量损失。基于生物活性天然产物的化学修饰,发现和研究新型农用化学品替代品是一种非常有效的方法。在这里,设计并合成了两个系列的新型肉桂酸衍生物,它们包含不同的构建基块和替代连接模式,以确定它们的抗病毒和抗菌活性。
生物测定结果表明,大多数肉桂酸衍生物在体内对烟草花叶病毒(TMV)具有优异的抗病毒能力,特别是化合物 A(半数有效浓度 [EC ] = 287.7μg/mL),与商业抗病毒剂利巴韦林(EC = 622.0μg/mL)相比,对 TMV 具有显著的保护作用。此外,化合物 A 在 200μg/mL 时对植物中的 Xac 具有 84.3%的保护效率。鉴于这些出色的结果,这些工程化的标题化合物可被视为防治植物病毒和细菌病害的有前途的先导化合物。初步的机制研究表明,化合物 A 可以通过提高防御酶的活性和上调防御基因来增强宿主的防御反应,从而抑制植物病原体的入侵。
本研究为含有不同构建基块和替代连接模式的肉桂酸衍生物在农药探索中的实际应用奠定了基础。 © 2023 化学工业协会。