新设计的含吡唑基单萜化合物增强对茄枯丝核菌的抗真菌效果

IF 6.2 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY
Haowen Huang, Cong Huang, Qingwen Fang, Yuhan Wu, Yuhuan Kuang, Ji Zhang, Guorong Fan, Zongde Wang, Shangxing Chen* and Dayong Peng*, 
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引用次数: 0

摘要

在农业和林业领域,存在与化学农药残留毒性和病原体耐药性相关的重大未知风险。为了解决这一问题,本研究通过有机合成高活性单萜天然产物获得了52个新的吡唑类单萜化合物,并对化合物5b的体外和体内抗真菌活性进行了评价和晶体结构分析。结果表明,化合物4g和8f对茄枯丝核菌具有较强的抑菌活性,EC50值分别为4.27和4.81 mg/L。同时,体内和体外试验结果表明,化合物4g和8f对水稻纹枯病均有较好的防治效果。通过扫描电镜、分子对接、酶活性测定和细胞毒性等方法初步探讨了这些化合物的抗真菌活性,表明这些化合物具有开发成低毒抗真菌药物的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Novel Design of Pyrazolyl-Containing Monoterpene Compounds to Enhance Antifungal Efficacy Against Rhizoctonia solani

Novel Design of Pyrazolyl-Containing Monoterpene Compounds to Enhance Antifungal Efficacy Against Rhizoctonia solani

In the fields of agriculture and forestry, there are major unknown risks associated with the toxicity of chemical pesticide residues and pathogen resistance. To address this issue, in this study, 52 novel pyrazole monoterpene compounds were obtained by organic synthesis of highly active monoterpene natural products and evaluated for their in vitro and in vivo antifungal activities and crystal structure analysis of compound 5b. The results showed that compounds 4g and 8f exhibited remarkable antifungal activities against Rhizoctonia solani, with the corresponding EC50 values reaching 4.27 and 4.81 mg/L. At the same time, the results of in vivo and in vitro experiments showed that both compounds 4g and 8f had good control effects against rice sheath blight. The antifungal activity of these compounds was preliminarily explored by scanning electron microscopy, molecular docking, enzyme activity determination, and cytotoxicity, indicating that these compounds have the potential for development into low-toxic antifungal drugs.

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来源期刊
Journal of Agricultural and Food Chemistry
Journal of Agricultural and Food Chemistry 农林科学-农业综合
CiteScore
9.90
自引率
8.20%
发文量
1375
审稿时长
2.3 months
期刊介绍: The Journal of Agricultural and Food Chemistry publishes high-quality, cutting edge original research representing complete studies and research advances dealing with the chemistry and biochemistry of agriculture and food. The Journal also encourages papers with chemistry and/or biochemistry as a major component combined with biological/sensory/nutritional/toxicological evaluation related to agriculture and/or food.
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