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一种简化且易于使用的 HIP HOP 测定法提供了有关查尔酮抗真菌作用机制的深入见解。

A simplified and easy-to-use HIP HOP assay provides insights into chalcone antifungal mechanisms of action.

机构信息

Royal Botanic Gardens, Kew, Richmond, UK.

Unidad de Investigación, Hospital Universitario Ntra Sra de Candelaria, Santa Cruz de Tenerife, Spain.

出版信息

FEBS Lett. 2022 Dec;596(23):3087-3102. doi: 10.1002/1873-3468.14483. Epub 2022 Sep 9.

DOI:10.1002/1873-3468.14483
PMID:36053795
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10087691/
Abstract

Elucidating the mechanism of action of an antifungal or cytotoxic compound is a time-consuming process. Yeast chemogenomic profiling provides a compelling solution to the problem but is experimentally complex. Here, we demonstrate the use of a highly simplified yeast chemical genetic assay comprising just 89 yeast deletion strains, each diagnostic for a specific mechanism of action. We use the assay to investigate the mechanism of action of two antifungal chalcone compounds, trans-chalcone and 4'-hydroxychalcone, and narrow down the mechanism to transcriptional stress. Crucially, the assay eliminates mechanisms of action such as topoisomerase I inhibition and membrane disruption that have been suggested for related chalcone compounds. We propose this simplified assay as a useful tool to rapidly identify common off-target mechanisms.

摘要

阐明一种抗真菌或细胞毒性化合物的作用机制是一个耗时的过程。酵母化学基因组分析为解决这个问题提供了一个引人注目的解决方案，但实验复杂。在这里，我们展示了一种高度简化的酵母化学遗传测定方法，仅包含 89 种酵母缺失株，每种株都针对特定的作用机制进行诊断。我们使用该测定方法研究了两种抗真菌查尔酮化合物，反式查尔酮和 4'-羟基查尔酮的作用机制，并将机制缩小到转录应激。至关重要的是，该测定方法消除了与相关查尔酮化合物相关的作用机制，如拓扑异构酶 I 抑制和膜破裂。我们提出这种简化的测定方法作为一种快速识别常见的非靶向机制的有用工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/ac6a07a0f5e5/FEB2-596-3087-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/4fa7f016a9c8/FEB2-596-3087-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/96adfa121a80/FEB2-596-3087-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/8ac352d933c7/FEB2-596-3087-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/8c4080b44cac/FEB2-596-3087-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/e5d50c5b66bb/FEB2-596-3087-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/ac6a07a0f5e5/FEB2-596-3087-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/4fa7f016a9c8/FEB2-596-3087-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/96adfa121a80/FEB2-596-3087-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/8ac352d933c7/FEB2-596-3087-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/8c4080b44cac/FEB2-596-3087-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/e5d50c5b66bb/FEB2-596-3087-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aee0/10087691/ac6a07a0f5e5/FEB2-596-3087-g003.jpg

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本文引用的文献

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Compounds with Distinct Targets Present Diverse Antimicrobial and Antibiofilm Efficacy against and and Combinations of Compounds Potentiate Their Effect.具有不同靶点的化合物对[具体细菌名称1]和[具体细菌名称2]呈现出多样的抗菌和抗生物膜功效，且化合物组合可增强其效果。
J Fungi (Basel). 2021 Apr 28;7(5):340. doi: 10.3390/jof7050340.
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Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials.脱靶毒性是临床试验中癌症药物的常见作用机制。
Sci Transl Med. 2019 Sep 11;11(509). doi: 10.1126/scitranslmed.aaw8412.
3
Trans-chalcone activity against Trichophyton rubrum relies on an interplay between signaling pathways related to cell wall integrity and fatty acid metabolism.
反式查耳酮对红色毛癣菌的活性依赖于与细胞壁完整性和脂肪酸代谢相关的信号通路之间的相互作用。
BMC Genomics. 2019 May 22;20(1):411. doi: 10.1186/s12864-019-5792-0.
4
Oxidant-Sensing Pathways in the Responses of Fungal Pathogens to Chemical Stress Signals.真菌病原体对化学应激信号反应中的氧化还原感应途径。
Front Microbiol. 2019 Mar 19;10:567. doi: 10.3389/fmicb.2019.00567. eCollection 2019.
5
Yeast Chemogenomic Profiling Reveals Iron Chelation To Be the Principle Cell Inhibitory Mode of Action of Gossypol.酵母化学基因组学分析揭示棉酚的主要细胞抑制作用模式是铁螯合。
J Med Chem. 2018 Aug 23;61(16):7381-7386. doi: 10.1021/acs.jmedchem.8b00692. Epub 2018 Aug 6.
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Lawsone, Juglone, and β-Lapachone Derivatives with Enhanced Mitochondrial-Based Toxicity.lawsone、juglone 和β-拉帕醌衍生物具有增强的基于线粒体的毒性。
ACS Chem Biol. 2018 Aug 17;13(8):1950-1957. doi: 10.1021/acschembio.8b00306. Epub 2018 Jun 15.
7
A Mini HIP HOP Assay Uncovers a Central Role for Copper and Zinc in the Antifungal Mode of Action of Allicin.一种微型嘻哈测定法揭示了铜和锌在大蒜素抗真菌作用模式中的核心作用。
J Agric Food Chem. 2017 May 10;65(18):3659-3664. doi: 10.1021/acs.jafc.7b00250. Epub 2017 Apr 26.
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Cancer reproducibility project yields first results.癌症可重复性项目取得首批成果。
Nat Rev Drug Discov. 2017 Feb 2;16(2):77. doi: 10.1038/nrd.2017.19.
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Diverse Molecular Targets for Chalcones with Varied Bioactivities.具有多种生物活性的查耳酮的不同分子靶点。
Med Chem (Los Angeles). 2015 Aug;5(8):388-404. doi: 10.4172/2161-0444.1000291. Epub 2015 Aug 22.
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Anti-cancer activity of trans-chalcone in osteosarcoma: Involvement of Sp1 and p53.反式查尔酮在骨肉瘤中的抗癌活性：与Sp1和p53的关系。
Mol Carcinog. 2016 Oct;55(10):1438-48. doi: 10.1002/mc.22386. Epub 2015 Aug 21.