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Toad Alkaloid for Pesticide Discovery: Dehydrobufotenine Derivatives as Novel Agents against Plant Virus and Fungi
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-08-20 , DOI: 10.1021/acs.jafc.1c03714 Zhaoyong Tian 1 , Ancai Liao 2 , Jin Kang 2 , Yongyue Gao 2 , Aidang Lu 1 , Ziwen Wang 2 , Qingmin Wang 3
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-08-20 , DOI: 10.1021/acs.jafc.1c03714 Zhaoyong Tian 1 , Ancai Liao 2 , Jin Kang 2 , Yongyue Gao 2 , Aidang Lu 1 , Ziwen Wang 2 , Qingmin Wang 3
Affiliation
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Plant viruses and fungi are a serious threat to food security and natural ecosystems. The efficient and environment-friendly control methods are urgently needed to help safeguard such resources. Here, we achieved the efficient synthesis of toad alkaloid dehydrobufotenine in eight steps with an overall yield of 8% from 5-methoxyindole. A series of dehydrobufotenine derivatives were designed, synthesized, and evaluated for their antiviral and fungicidal activities systematically. It was found for the first time that these compounds have good anti-plant virus activities and anti-plant pathogen activities. The antiviral activities of 21 compounds were similar to or better than those of ribavirin. Compounds 12 and 17 displayed better antiviral activities than ningnanmycin which is perhaps the most effective anti-plant virus agent. The antiviral mechanism research study of 12 revealed that it could make 20S CP disk fusion and aggregation. Further molecular docking results showed that there are hydrogen bonds between compounds 12, 17, and tobacco mosaic virus CP. The docking results are consistent with the antiviral activity. These compounds also displayed broad-spectrum fungicidal activities against 14 kinds of fungi, especially for Sclerotinia sclerotiorum. In this work, the synthesis, structure optimization, structure–activity relationship studies, and mode of action research of dehydrobufotenine alkaloids were carried out. It provides a reference for the development of the anti-plant virus agent and anti-plant pathogen agent from toad alkaloids.
中文翻译：
用于农药发现的蟾蜍生物碱：脱氢蟾蜍精衍生物作为抗植物病毒和真菌的新型药剂
植物病毒和真菌对粮食安全和自然生态系统构成严重威胁。迫切需要有效和环境友好的控制方法来帮助保护这些资源。在这里，我们通过 8 个步骤实现了蟾蜍生物碱脱氢丁二烯的有效合成，5-甲氧基吲哚的总产率为 8%。系统地设计、合成了一系列脱氢丁二烯衍生物，并对其抗病毒和杀真菌活性进行了评估。首次发现这些化合物具有良好的抗植物病毒活性和抗植物病原体活性。21种化合物的抗病毒活性与利巴韦林相似或优于利巴韦林。化合物12和17显示出比宁南霉素更好的抗病毒活性，宁南霉素可能是最有效的抗植物病毒剂。12的抗病毒机制研究表明，它可以使20S CP磁盘融合和聚集。进一步的分子对接结果表明，有化合物之间的氢键12，17烟草花叶病毒CP和。对接结果与抗病毒活性一致。这些化合物还对14种真菌表现出广谱杀菌活性，尤其是对核盘菌（Sclerotinia sclerotiorum）. 在这项工作中，开展了脱氢丁二烯碱生物碱的合成、结构优化、构效关系研究和作用模式研究。为从蟾蜍生物碱中开发抗植物病毒剂和抗植物病原体剂提供了参考。
更新日期：2021-09-01
中文翻译：
用于农药发现的蟾蜍生物碱：脱氢蟾蜍精衍生物作为抗植物病毒和真菌的新型药剂
植物病毒和真菌对粮食安全和自然生态系统构成严重威胁。迫切需要有效和环境友好的控制方法来帮助保护这些资源。在这里，我们通过 8 个步骤实现了蟾蜍生物碱脱氢丁二烯的有效合成，5-甲氧基吲哚的总产率为 8%。系统地设计、合成了一系列脱氢丁二烯衍生物，并对其抗病毒和杀真菌活性进行了评估。首次发现这些化合物具有良好的抗植物病毒活性和抗植物病原体活性。21种化合物的抗病毒活性与利巴韦林相似或优于利巴韦林。化合物12和17显示出比宁南霉素更好的抗病毒活性，宁南霉素可能是最有效的抗植物病毒剂。12的抗病毒机制研究表明，它可以使20S CP磁盘融合和聚集。进一步的分子对接结果表明，有化合物之间的氢键12，17烟草花叶病毒CP和。对接结果与抗病毒活性一致。这些化合物还对14种真菌表现出广谱杀菌活性，尤其是对核盘菌（Sclerotinia sclerotiorum）. 在这项工作中，开展了脱氢丁二烯碱生物碱的合成、结构优化、构效关系研究和作用模式研究。为从蟾蜍生物碱中开发抗植物病毒剂和抗植物病原体剂提供了参考。
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