Paecilosetin Derivatives as Potent Antimicrobial Agents from Isaria farinosa,Journal of Natural Products

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Paecilosetin Derivatives as Potent Antimicrobial Agents from Isaria farinosa
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-10-06 , DOI: 10.1021/acs.jnatprod.0c00444
Orianne Brel ₁ , Seindé Touré ₁ , Marceau Levasseur ₁ , Christian Lechat ₂ , Léonie Pellissier _{3,

4} , Jean-Luc Wolfender _{3,

4} , Elsa Van-Elslande ₁ , Marc Litaudon ₁ , Isabelle Dusfour _{5,

6} , Didier Stien ₇ , Véronique Eparvier ₁

Affiliation

Fifty-seven entomopathogenic microorganisms were screened against human pathogens and subjected to mass spectrometry molecular networking based dereplication. Isaria farinosa BSNB-1250, shown to produce potentially novel biologically active metabolites, was grown on a large scale on potato dextrose agar, and paecilosetin (1) and five new analogues (2–6) were subsequently isolated. The structures of the new compounds were elucidated using 1D and 2D NMR. The absolute configurations of compounds 1–6 were determined using Mosher ester derivatives (1, 3, 4), comparison of experimental and calculated ECD spectra (2–4 and 6), and single-crystal X-ray diffraction analysis (5). Compounds 1 and 5 exhibited strong antibacterial activity against MSSA and MRSA with MIC values of 1–2 μg/mL.

中文翻译：

Paecilosetin 衍生物作为来自 Isaria farinosa 的强效抗菌剂

针对人类病原体筛选了 57 种昆虫病原微生物，并进行了基于质谱分子网络的去复制。棒束孢farinosa BSNB-1250，显示产生潜在的新的生物活性代谢物，生长在马铃薯葡萄糖琼脂规模大，以及paecilosetin（1）和五个新类似物（2 - 6）随后分离。使用1D和2D NMR阐明了新化合物的结构。化合物1 – 6的绝对构型是使用 Mosher 酯衍生物 ( 1 , 3 , 4），实验的比较和计算的ECD谱（2 - 4和6），和单晶X射线衍射分析（5）。化合物1和5对 MSSA 和 MRSA 表现出很强的抗菌活性，MIC 值为 1-2 μg/mL。

更新日期：2020-10-26

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