Tianjin Key Laboratory of Structure and Performance for Functional Molecules, College of Chemistry, Tianjin Normal University, Tianjin 300387, China.
Beijing Key Laboratory of Flavor Chemistry, Beijing Technology and Business University (BTBU), Beijing 100048, China.
Molecules. 2022 Dec 2;27(23):8439. doi: 10.3390/molecules27238439.
Plant diseases caused by viruses and fungi have a serious impact on the quality and yield of crops, endangering food security. The use of new, green, and efficient pesticides is an important strategy to increase crop output and deal with the food crisis. Ideally, the best pesticide innovation strategy is to find and use active compounds from natural products. Here, we took the marine natural product hyrtinadine A as the lead compound, and designed, synthesized, and systematically investigated a series of its derivatives for their antiviral and antifungal activities. Compound was found to have excellent antiviral activity against the tobacco mosaic virus (TMV) (inactivation inhibitory effect of 55%/500 μg/mL and 19%/100 μg/mL, curative inhibitory effect of 52%/500 μg/mL and 22%/100 μg/mL, and protection inhibitory effect of 57%/500 μg/mL and 26%/100 μg/mL) and emerged as a novel antiviral candidate. These compound derivatives displayed broad-spectrum fungicidal activities against 14 kinds of phytopathogenic fungi at 50 μg/mL and the antifungal activities of compounds , , , and against are higher than that of the commercial fungicide chlorothalonil. Therefore, this study could lay a foundation for the application of hyrtinadine A derivatives in plant protection.
病毒和真菌引起的植物病害严重影响作物的质量和产量,危及粮食安全。使用新型、绿色、高效的农药是增加作物产量和应对粮食危机的重要策略。理想情况下,最佳的农药创新策略是从天然产物中寻找和利用具有活性的化合物。在这里,我们以海洋天然产物海兔毒素 A 为先导化合物,设计、合成并系统地研究了一系列衍生物的抗病毒和抗真菌活性。发现化合物 对烟草花叶病毒(TMV)具有优异的抗病毒活性(55%/500 μg/mL 和 19%/100 μg/mL 的失活抑制作用、52%/500 μg/mL 和 22%/100 μg/mL 的治疗抑制作用、57%/500 μg/mL 和 26%/100 μg/mL 的保护抑制作用),并成为一种新型的抗病毒候选药物。这些化合物衍生物在 50 μg/mL 时对 14 种植物病原菌表现出广谱杀菌活性,化合物 、 、 、 对 的抗真菌活性高于商业杀菌剂百菌清。因此,本研究可为海兔毒素 A 衍生物在植物保护中的应用奠定基础。