萘比拉霉素 A4 及其相关化合物，一种新型抗 PRV 剂及其抗菌活性，来自 WS-68302。
Napyradiomycin A4 and Its Relate Compounds, a New Anti-PRV Agent and Their Antibacterial Activities, from WS-68302.
机构信息
Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, No. 8, Nanhu Ave., Hongshan District, Wuhan 430064, China.
出版信息
Molecules. 2023 Jan 8;28(2):640. doi: 10.3390/molecules28020640.
Two new napyradiomycins derivatives, napyradiomycin A4 () and A80915 H (), along with five known ones, were isolated from the ethyl acetate extract of fermentation culture of WS-68302. Their structures were elucidated by extensive spectroscopic analysis, including HR-MS, 1D and 2D NMR, CD spectrum, as well as comparison with literature data. Compound exhibited significant antiviral activity against PRV (Pseudorabies virus) with an IC value of 2.056 μM and therapeutic ratio at 14.98, suggesting that it might have potential for development of an antiviral agent. Moreover, compound displayed the strongest inhibition against PRV protein among the tested napyradiomycins in the indirect immunofuorescence assay. Compounds and showed higher activities against swine pathogenic than the positive control penicillin G sodium salt, with MIC values of 3.125 and 6.25 μg/mL, respectively. Compounds and - exhibited moderate antibacterial activity against the swine pathogenic , with MIC values ranging from 25 to 50 μg/mL.
从 WS-68302 发酵培养物的乙酸乙酯提取物中分离得到两个新的纳比雷迪霉素衍生物，即纳比雷迪霉素 A4（）和 A80915 H（），以及五个已知化合物。通过广泛的光谱分析，包括高分辨质谱、1D 和 2D NMR、CD 光谱以及与文献数据的比较，确定了它们的结构。化合物 对 PRV（猪伪狂犬病病毒）表现出显著的抗病毒活性，IC 值为 2.056 μM，治疗比值为 14.98，表明它可能具有开发抗病毒药物的潜力。此外，在间接免疫荧光测定中，化合物 对测试的纳比雷迪霉素中对 PRV 蛋白的抑制作用最强。化合物 对猪致病性 的抑制活性高于阳性对照青霉素 G 钠盐，MIC 值分别为 3.125 和 6.25 μg/mL。化合物 对猪致病性 的抑制活性适中，MIC 值范围为 25 至 50 μg/mL。
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