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赭曲霉花青苷,一种赭曲霉毒素-麦角固醇异二聚体,可抑制16D-1产生白细胞介素-6和一氧化氮。

Ochrasperfloroid, an ochratoxin-ergosteroid heterodimer with inhibition of IL-6 and NO production from 16D-1.

作者信息

Gu Bin-Bin, Jiao Fu-Rong, Wu Wei, Liu Lei, Jiao Wei-Hua, Sun Fan, Wang Shu-Ping, Yang Fan, Lin Hou-Wen

机构信息

Key Laboratory for Marine Drugs, Department of Pharmacy, State Key Laboratory of Oncogenes and Related Genes, Renji Hospital School of Medicine, Shanghai Jiao Tong University Shanghai 200127 China

出版信息

RSC Adv. 2019 Mar 4;9(13):7251-7256. doi: 10.1039/c8ra10539a. eCollection 2019 Mar 1.

Abstract

A novel ochratoxin-ergosteroid heterodimer, ochrasperfloroid (1), together with a known mycotoxin, ochratoxin A (2), were isolated from the sponge-derived fungus 16D-1. The structure of 1 was determined on the basis of 1D/2D NMR, HRESIMS/MS, and LC-UV/MS analysis of its alkaline hydrolyzates, quantum-chemical C NMR calculation, and comparison with literature data. Of note, the ergosteroid embedded in 1 is also a new structure. Ochrasperfloroid (1) showed potent inhibitory activity towards IL-6 production in lipopolysaccharide (LPS)-induced THP-1 cell line, with an IC value of 2.02 μM, and NO production in LPS-activated RAW264.7 macrophages, with an IC value of 1.11 μM.

摘要

从海绵来源的真菌16D-1中分离出一种新型的赭曲霉毒素-麦角甾醇异二聚体——赭曲asperfloroid(1),以及一种已知的霉菌毒素——赭曲霉毒素A(2)。通过对其碱性水解产物的一维/二维核磁共振、高分辨电喷雾电离质谱/质谱和液相色谱-紫外/质谱分析、量子化学碳核磁共振计算以及与文献数据的比较,确定了1的结构。值得注意的是,嵌入在1中的麦角甾醇也是一种新结构。赭曲asperfloroid(1)对脂多糖(LPS)诱导的THP-1细胞系中白细胞介素-6的产生显示出强效抑制活性,IC值为2.02 μM,对LPS激活的RAW264.7巨噬细胞中一氧化氮的产生也有抑制作用,IC值为1.11 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e380/9061062/d8b09351d3b3/c8ra10539a-f1.jpg

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