一种VioA变异激活异源宿主链霉菌OUC20-O中的抗生素链脲蛋白。

IF 5.4 2区医学 Q1 CHEMISTRY, MEDICINAL

Marine Drugs Pub Date : 2025-05-11 DOI:10.3390/md23050205

Jie Shan, Liangguang Yue, Luyao Xu, Runyi Wang, Qingzhou Meng, Jun Feng, Joon-Hee Lee, Ming Lu, Huayue Li

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引用次数: 0

摘要

将VioA的G231L变体异源表达到16株海产链霉菌中，结合生物活性追踪，在Streptomyces sp. OUC20-O中激活了7种抗生素链霉菌蛋白（1-7）。其中，化合物1名为linstreptogramin，是一种具有不寻常的线性链脲蛋白骨架的新化合物。化合物1的平面结构和立体化学是通过广泛的质谱和核磁共振谱分析以及ECD计算确定的。抑菌活性评价中，化合物1 ~ 4对多重耐药屎肠球菌CCARM 5203有明显的生长抑制作用，MIC值为0.2 ~ 1.6µg/mL，与阳性对照万古霉素相当。

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A VioA Variant Activates Antibiotic Streptogramins in the Heterologous Host Streptomyces sp. OUC20-O.

Heterologous expression of the G231L variant of VioA into 16 strains of marine-derived Streptomyces, combined with bioactivity tracking, leads to the activation of seven antibiotic streptogramins (1-7) in Streptomyces sp. OUC20-O. Among these, compound 1, named linstreptogramin, is a new compound with an unusual linear streptogramin skeleton. The planar structure and stereochemistry of compound 1 were established based on extensive MS and NMR spectroscopic analyses, together with ECD calculations. In the antibacterial activity evaluation, compounds 1-4 showed significant growth inhibition against the multidrug-resistant Enterococcus faecium CCARM 5203 with MIC values of 0.2-1.6 µg/mL, which are comparable to the positive control vancomycin.

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来源期刊

Marine Drugs 医学-医药化学

CiteScore

9.60

自引率

14.80%

发文量

671

审稿时长

1 months

期刊介绍： Marine Drugs (ISSN 1660-3397) publishes reviews, regular research papers and short notes on the research, development and production of drugs from the sea. Our aim is to encourage scientists to publish their experimental and theoretical research in as much detail as possible, particularly synthetic procedures and characterization information for bioactive compounds. There is no restriction on the length of the experimental section.