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一种VioA变体在异源宿主sp. OUC20 - O中激活抗生素链阳性菌素。

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

作者信息

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

机构信息

Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

State Key Laboratory of Photoelectric Conversion and Utilization of Solar Energy, Qingdao New Energy Shandong Laboratory, Shandong C1 Refinery Engineering Research Center, Qingdao Institute of Bioenergy and Bioprocess Technology, Chinese Academy of Sciences, Qingdao 266101, China.

出版信息

Mar Drugs. 2025 May 11;23(5):205. doi: 10.3390/md23050205.

Abstract

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

摘要

将vioA的G231L变体异源表达至16株海洋来源的菌株中,并结合生物活性追踪,导致在sp. OUC20 - O中激活了七种抗生素链阳性菌素(-)。其中,化合物,命名为林链阳性菌素,是一种具有不寻常线性链阳性菌素骨架的新化合物。基于广泛的质谱和核磁共振光谱分析以及电子圆二色性计算,确定了化合物的平面结构和立体化学。在抗菌活性评估中,化合物 - 对多重耐药的CCARM 5203表现出显著的生长抑制作用,MIC值为0.2 - 1.6 µg/mL,与阳性对照万古霉素相当。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94e7/12113368/2c99015945b3/marinedrugs-23-00205-g001.jpg

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