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来自SCNU-F0046的具有抗菌和抗炎活性的苯并呋喃衍生物

Benzofuran Derivatives with Antimicrobial and Anti-Inflammatory Activities from SCNU-F0046.

作者信息

Chen Chen, Kang Jinbi, Zhang Ruiqi, Jia Hao, Lin Zirong, Liu Zhengming, Liu Rongrong, Zou Xinyi, Long Yuhua

机构信息

Guangzhou Key Laboratory of Analytical Chemistry for Biomedicine, School of Chemistry, South China Normal University, Guangzhou 510006, China.

出版信息

Int J Mol Sci. 2025 Aug 14;26(16):7861. doi: 10.3390/ijms26167861.

DOI:10.3390/ijms26167861
PMID:40869182
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12386745/
Abstract

A chemical investigation on the marine-derived fungus SCNU-F0046 resulted in the isolation and characterization of four new benzofurans (, , , ) and four known analogues (, , , ). Their structures were elucidated by a combination of mass, NMR spectroscopy, electronic circular dichroism (ECD) calculations and X-ray crystallographic analyses. The antimicrobial experiments disclosed compound exhibited moderate antibacterial activity, while compound showed antifungal activity. In addition, the anti-inflammatory activity of aza-benzofuran compounds (-) was also evaluated. Bioassays revealed that compounds and exhibited anti-inflammatory activity by inhibiting nitric oxide release without cytotoxicity in lipopolysaccharide (LPS)-stimulated RAW 264.7 mouse macrophages with IC values of 17.3 and 16.5 μM, respectively. The docking study revealed that compounds and exhibited an ideal fit within the active site of the murine inducible nitric oxide synthase (iNOS), establishing characteristic hydrogen bonds.

摘要

对源自海洋的真菌SCNU-F0046进行的化学研究,分离并鉴定了4种新的苯并呋喃(,,,)和4种已知类似物(,,,)。通过质谱、核磁共振光谱、电子圆二色性(ECD)计算和X射线晶体学分析相结合的方法阐明了它们的结构。抗菌实验表明化合物表现出中等抗菌活性,而化合物显示出抗真菌活性。此外,还评估了氮杂苯并呋喃化合物(-)的抗炎活性。生物测定显示,化合物和通过抑制一氧化氮释放表现出抗炎活性,在脂多糖(LPS)刺激的RAW 264.7小鼠巨噬细胞中无细胞毒性,IC值分别为17.3和16.5 μM。对接研究表明,化合物和在小鼠诱导型一氧化氮合酶(iNOS)的活性位点内表现出理想的契合,形成了特征性氢键。

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本文引用的文献

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