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筛选受天然产物启发的文库以寻找抗活动。

Screening a Natural Product-Inspired Library for Anti- Activities.

机构信息

Department of Microbiology and Immunology, University of Otago, Dunedin 9054, New Zealand.

School of Biological Sciences, Victoria University of Wellington, Wellington 6140, New Zealand.

出版信息

Molecules. 2021 Mar 24;26(7):1819. doi: 10.3390/molecules26071819.

DOI:10.3390/molecules26071819
PMID:33804938
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8037946/
Abstract

is a genus of microorganisms that cause devastating dieback and root-rot diseases in thousands of plant hosts worldwide. The economic impact of diseases on crops and native ecosystems is estimated to be billions of dollars per annum. These invasive pathogens are extremely difficult to control using existing chemical means, and the effectiveness of the few treatments available is being jeopardized by increasing rates of resistance. There is an urgent need to identify new chemical treatments that are effective against diseases. Natural products have long been regarded as "Nature's medicine chest", providing invaluable leads for developing front-line drugs and agrochemical agents. Here, we have screened a natural product-inspired library of 328 chemicals against two key species: and . The library was initially screened for inhibition of zoospore germination. From these screens, we identified twenty-one hits that inhibited germination of one or both species. These hits were further tested in mycelial growth inhibition studies to determine their half-maximal inhibitory concentrations (ICs). Four compounds had IC values of approximately 10 µM or less, and our best hit had ICs of approximately 3 µM against both species tested. Overall, these hits may serve as promising leads for the development of new anti- agrochemicals.

摘要

是一类微生物,它们会在全球成千上万种植物宿主中引发毁灭性的枯萎病和根腐病。这些病害每年给农作物和原生生态系统造成的经济损失估计达数十亿美元。使用现有的化学手段来控制这些入侵性病原体极其困难,而少数可用的处理方法的有效性正受到抗性不断增加的威胁。迫切需要找到新的、对 病害有效的化学处理方法。天然产物长期以来一直被视为“大自然的药箱”,为开发一线药物和农用化学品提供了宝贵的线索。在这里,我们针对两种关键的 物种: 和 ,筛选了一个受天然产物启发的 328 种化学物质的文库。该文库最初是针对游动孢子萌发的抑制作用进行筛选的。从这些筛选中,我们确定了 21 个能抑制一个或两个物种萌发的命中化合物。这些命中化合物进一步在菌丝生长抑制研究中进行测试,以确定它们的半最大抑制浓度 (IC)。四种化合物的 IC 值约为 10 µM 或更低,而我们最好的命中化合物对两种测试的 物种的 IC 值约为 3 µM。总的来说,这些命中化合物可能成为开发新的抗农化剂的有希望的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40c4/8037946/19d7b327a84c/molecules-26-01819-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40c4/8037946/19d7b327a84c/molecules-26-01819-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40c4/8037946/19d7b327a84c/molecules-26-01819-g001.jpg

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Phosphonic acid: a long-standing and versatile crop protectant.膦酸:一种历史悠久且用途广泛的作物保护剂。
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Inhibitory Properties of Aldehydes and Related Compounds against -Identification of a New Lead.醛类及相关化合物的抑制特性——一种新先导化合物的鉴定
Pathogens. 2020 Jul 7;9(7):542. doi: 10.3390/pathogens9070542.
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