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Fang Liu1, Xiao Cao1, Tao Zhang1
1National 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 550025, China.
新的与pyrazole和piperazine环的myricetin衍生物显示出强大的抗菌和抗真菌活性. 化合物D1有效地保护,而D6和D16对植物病原体具有强烈的疗效.
科学领域:
- 药用化学 医学化学
- 农业科学 农业科学
- 植物病理学 植物病理学
背景情况:
- 瑞是一种天然产品,作为合成新生物活性化合物的支架.
- 皮拉和皮佩拉环是药物发现中的关键药.
- 开发针对植物病原菌和真菌的有效药物对于作物保护至关重要.
研究的目的:
- 合成和描述新型的myricetin衍生物,其中包括pyrazole和piperazine部分.
- 评估这些衍生物对关键植物病原体的抗菌和抗真菌活性.
- 为了研究强效化合物的作用机制.
主要方法:
- 通过胺基键形成合成myricetin衍生物.
- 使用NMR光谱学和高分辨率质谱学阐明结构.
- 在体外生物试验中检测抗菌活性对抗Xanthomonas axonopodis pv. 树, 伪虫注射器 pv. 它们包括Actinidiae和Xanthomonas oryzae pv. 米. 这是一种米.
- 对十种植物病原菌的抗真菌活性查.
- 在收获后的桃上进行了体外疗效测试.
- 作用研究的机制,包括SDH活动评估,分子对接和含量分析.
- 扫描电子显微镜用于菌体形态观测.
主要成果:
- 化合物D6对Xanthomonas oryzae pv.表现出显著的抗菌活性. 米 (EC50 = 18.8 微克/毫升).
- 化合物D1对Phomopsis sp.表现出强大的抗真菌活性. (EC50 = 16.9μg/mL) 并且对果有治愈性 (60.6%) 和保护性 (74.9%) 的作用.
- 化合物D16表现出对Phytophthora capsici (EC50 = 11.3μg/mL) 的优越活性,SEM揭示了细胞损伤.
- 机制研究表明,D1增加了甲水平,损害了真菌细胞膜.
结论:
- 合成的myricetin衍生物具有有前途的抗菌和抗真菌特性.
- 化合物D1,D6和D16对特定的植物病原体有效,并显示出农业应用的潜力.
- 对这些衍生物的进一步研究可能会导致新的作物保护剂.
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