Sukhoverkov Kirill V, Breese Karen J, Debowski Aleksandra W, Murcha Monika W, Stubbs Keith A, Mylne Joshua S
The University of Western Australia, School of Molecular Sciences 35 Stirling Highway Crawley Perth 6009 Australia
The ARC Centre of Excellence in Plant Energy Biology 35 Stirling Highway Crawley Perth 6009 Australia.
RSC Chem Biol. 2021 Nov 10;3(1):37-43. doi: 10.1039/d1cb00192b. eCollection 2022 Jan 5.
The rise in herbicide resistance over recent decades threatens global agriculture and food security and so discovery of new modes of action is increasingly important. Here we reveal linezolid, an oxazolidinone antibiotic that inhibits microbial translation, is also herbicidal. To validate the herbicidal mode of action of linezolid we confirmed its micromolar inhibition is specific to chloroplast translation and did not affect photosynthesis directly. To assess the herbicide potential of linezolid, testing against a range of weed and crop species found it effective pre- and post-emergence. Using structure-activity analysis we identified the critical elements for herbicidal activity, but importantly also show, using antimicrobial susceptibility assays, that separation of antibacterial and herbicidal activities was possible. Overall these results validate chloroplast translation as a viable herbicidal target.
近几十年来除草剂抗性的增加威胁着全球农业和粮食安全，因此发现新的作用模式变得越来越重要。在此我们揭示，恶唑烷酮类抗生素利奈唑胺虽能抑制微生物翻译，但也具有除草活性。为验证利奈唑胺的除草作用模式，我们证实其微摩尔级抑制作用对叶绿体翻译具有特异性，且不会直接影响光合作用。为评估利奈唑胺的除草潜力，我们对一系列杂草和作物品种进行了测试，发现它在芽前和芽后均有效。通过构效分析，我们确定了除草活性的关键要素，但重要的是，通过抗菌药敏试验我们还表明，抗菌活性和除草活性是可以分离的。总体而言，这些结果证实叶绿体翻译是一个可行的除草靶点。
