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基于从内生真菌中分离出的天然吡唑的新型介离子化合物的设计、合成、抗菌活性及作用机制。

Design, Synthesis, Antibacterial Activity, and Mechanism of Novel Mesoionic Compounds Based on Natural Pyrazole Isolated from an Endophytic Fungus .

机构信息

National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.

Guizhou Institute of Soil and Fertilizer/Agricultural Resources and Environment, Guizhou Academy of Agricultural Sciences, Huaxi District, Guiyang 550025, P. R. China.

出版信息

J Agric Food Chem. 2023 Jul 5;71(26):10018-10027. doi: 10.1021/acs.jafc.3c02908. Epub 2023 Jun 20.

Abstract

pv. () is a type of bacteria that causes bacterial leaf blight disease in rice plants. This disease is substantially harmful, and the current prevention and control measures are facing challenges. This study has investigated the effectiveness of the control activity that the endophytic fungus NS7 fermented from possessed against . Twenty-eight novel mesoionic compounds were designed and synthesized based on the natural compound . These compounds displayed moderate to excellent anti- activity . Notably, compound exhibited prominent anti- activity with an EC value of 40.3 mg/L, which was better than that of the positive control thiodiazole copper (TC)(71.2 mg/L) and the lead compound (108.1 mg/L). pot experiments on showed that compound exhibited protective and curative activities of 39.4 and 30.4%, respectively, which were better than those of TC (35.7 and 28.8%, respectively). Further, a preliminary mechanism study indicated that compound could enhance the activity of defense enzymes to improve the ability for anti-. Meanwhile, compound could also regulate the carbon fixation in photosynthetic organisms, which might be related to the enhanced immune function of rice. This study offers a new strategy for discovering antibacterial agents based on natural products.

摘要

(PV)是一种引起水稻细菌性叶枯病的细菌。这种疾病危害极大,目前的防控措施面临挑战。本研究调查了从内生真菌 NS7 发酵得到的对 PV 的控制活性的效果。基于天然化合物,设计和合成了 28 种新型介离子化合物。这些化合物表现出中等至优异的抗 PV 活性。值得注意的是,化合物 表现出突出的抗 PV 活性,EC 值为 40.3mg/L,优于阳性对照噻二唑铜(TC)(71.2mg/L)和先导化合物 (108.1mg/L)。对 进行的盆栽试验表明,化合物 表现出 39.4%和 30.4%的保护和治疗活性,分别优于 TC(35.7%和 28.8%)。此外,初步的机制研究表明,化合物 可以增强防御酶的活性,提高抗 PV 的能力。同时,化合物 还可以调节光合生物中的碳固定,这可能与水稻增强的免疫功能有关。本研究为基于天然产物发现抗菌剂提供了一种新策略。

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