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发现新型吩噻嗪衍生物作为治疗植物病毒病的新型农用化学品替代品。

Discovery of novel phenothiazine derivatives as new agrochemical alternatives for treating plant viral diseases.

作者信息

Shao Wu-Bin, Liao Yan-Mei, Luo Rong-Shuang, Ji Jin, Xiao Wan-Lin, Zhou Xiang, Liu Li-Wei, Yang Song

机构信息

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.

出版信息

Pest Manag Sci. 2023 Nov;79(11):4231-4243. doi: 10.1002/ps.7623. Epub 2023 Jul 5.

Abstract

BACKGROUND

Plant viral diseases, namely 'plant cancer', are extremely difficult to control. Even worse, few antiviral agents can effectively control and totally block viral infection. There is an urgent need to explore and discover novel agrochemicals with high activity and a unique mode of action to manage these refractory diseases.

RESULTS

Forty-one new phenothiazine derivatives were prepared and their inhibitory activity against tobacco mosaic virus (TMV) was assessed. Compound A had the highest protective activity against TMV, with a half-maximal effective concentration (EC ) of 115.67 μg/mL, which was significantly better than that of the positive controls ningnanmycin (271.28 μg/mL) and ribavirin (557.47 μg/mL). Biochemical assays demonstrated that compound A could inhibit TMV replication by disrupting TMV self-assembly, but also enabled the tobacco plant to enhance its defense potency by increasing the activities of various defense enzymes.

CONCLUSION

In this study, novel phenothiazine derivatives were elaborately fabricated and showed remarkable anti-TMV behavior that possessed the dual-action mechanisms of inhibiting TMV assembly and invoking the defense responses of tobacco plants. Moreover, new agrochemical alternatives based on phenothiazine were assessed for their antiviral activities and showed extended agricultural application. © 2023 Society of Chemical Industry.

摘要

背景

植物病毒病,即“植物癌症”,极难控制。更糟糕的是,很少有抗病毒剂能有效控制并完全阻断病毒感染。迫切需要探索和发现具有高活性和独特作用方式的新型农用化学品来应对这些难治性疾病。

结果

制备了41种新型吩噻嗪衍生物,并评估了它们对烟草花叶病毒(TMV)的抑制活性。化合物A对TMV具有最高的保护活性,其半数有效浓度(EC)为115.67μg/mL,显著优于阳性对照宁南霉素(271.28μg/mL)和利巴韦林(557.47μg/mL)。生化分析表明,化合物A可通过破坏TMV自组装来抑制TMV复制,还能通过提高各种防御酶的活性使烟草植株增强其防御能力。

结论

在本研究中,精心制备了新型吩噻嗪衍生物,其表现出显著的抗TMV行为,具有抑制TMV组装和激发烟草植株防御反应的双重作用机制。此外,基于吩噻嗪的新型农用化学品替代品的抗病毒活性得到评估,并显示出广阔的农业应用前景。©2023化学工业协会。

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