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基于化学生态学研究的 1T-2 对抗新型先导化合物的发现。

Novel Lead Compound Discovery from 1T-2 against Based on a Chemical Ecology Study.

机构信息

CAS and Shandong Province Key Laboratory of Experimental Marine Biology, Center for Ocean Mega-Science, Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.

Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology (Qingdao), No. 1 Wenhai Road, Qingdao 266237, China.

出版信息

J Agric Food Chem. 2022 Apr 20;70(15):4644-4657. doi: 10.1021/acs.jafc.1c08147. Epub 2022 Apr 11.

Abstract

To replace biohazardous nematicides, there is an ever-increasing need to identify natural product-based agents to contain root-knot nematodes (RKNs) in agriculture. In this chemical ecology study, an antagonistic fungus 1T-2, which could cause the formation of withering of the gut and vacuole-like structures in the nematode body, was isolated based on the gradually increased antagonistic interactions between the soil fungi and RKNs. Based on these typical morphological characteristics, a potent nematode-antagonistic compound 2-furoic acid, which had a simple structure, was successfully identified from 1T-2 fermentation broth by liquid chromatography-mass spectrometry (LC-MS). 2-Furoic acid showed effective mortality activity , of which the LC value to at 24 h was 37.75 μg/mL. 2-Furoic acid had similar mortality activity to the positive control fosthiazate at 30 μg/mL. Continuous 2-furoic acid exposure had obvious negative influences on both nematode vitality and egg hatchability. Notably, significant variations were observed in nematodes and eggs with 2-furoic acid treatment, which might be induced by novel nematocidal mechanisms. Furthermore, the 1T-2 fermentation broth and 2-furoic acid had significant control efficacy on under the greenhouse test-tube assay. Overall, these findings provide valuable insights into the use of 2-furoic acid with biocontrol potential as a preferable lead structure for the development of innovative nematicides.

摘要

为了替代生物危害性杀线虫剂,人们越来越需要从天然产物中寻找防治根结线虫的药剂。在这项化学生态学研究中,我们根据土壤真菌与根结线虫之间逐渐增强的拮抗相互作用,从一种拮抗真菌 1T-2 中分离出一种能够导致线虫肠道枯萎和空泡样结构形成的物质。基于这些典型的形态学特征,我们通过液相色谱-质谱联用技术(LC-MS)从 1T-2 发酵液中成功鉴定出一种具有简单结构的、活性很强的线虫拮抗化合物 2-糠酸。2-糠酸具有有效的致死活性,其 24 h 的 LC 值为 37.75 μg/mL。2-糠酸在 30 μg/mL 时的致死活性与阳性对照噻唑膦相当。连续暴露于 2-糠酸对线虫活力和卵孵化率均有明显的负面影响。值得注意的是,用 2-糠酸处理后线虫和卵出现了明显的形态变化,这可能是由新型杀线虫机制引起的。此外,在温室试管试验中,1T-2 发酵液和 2-糠酸对线虫的防治效果显著。总的来说,这些发现为利用具有生物防治潜力的 2-糠酸作为开发新型杀线虫剂的首选先导结构提供了有价值的见解。

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