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Anti-inflammatory Meroterpenoids from Baeckea frutescens
Journal of Natural Products ( IF 5.1 ) Pub Date : 2017-07-28 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00042
Ji-Qin Hou 1 , Cui Guo 1 , Jian-Juan Zhao 1 , Yang-Yang Dong 1 , Xiao-Long Hu 1 , Qi-Wei He 1 , Bao-Bao Zhang 1 , Ming Yan 1 , Hao Wang 1
Affiliation  

Frutescones H–R (111), new sesqui- or monoterpene-based meroterpenoids, were isolated from the aerial parts of Baeckea frutescens. Their structures and absolute configurations were established by means of spectroscopic analyses (HRESIMS, 1D and 2D NMR, and ECD), as well as single-crystal X-ray crystallography of 1, (−)-7, and 9. The anti-inflammatory activities of all isolates were evaluated by measuring their inhibitory effects on NO production in LPS-stimulated RAW 264.7 macrophages, and the structure–activity relationships of 111 are also discussed. Compound 8 exhibited anti-inflammatory activity with an IC50 value of 0.36 μM, which might be related to the regulation of the NF-κB signaling pathway via the suppression of p65 nuclear translocation and the consequent decrease of IL-6 and TNF-α.

中文翻译:

从抗炎Meroterpenoids岗松

Frutescones H–R(111)是新的基于倍半萜或单萜的类萜,是从Baeckea frutescens的地上部分中分离出来的。通过光谱分析(HRESIMS,1D和2D NMR和ECD)以及1,(-)- 79的单晶X射线晶体学,确定了它们的结构和绝对构型。所有分离物的抗炎活性是通过测量在LPS刺激的RAW 264.7巨噬细胞中它们对NO产生的抑制效果评价,结构-活性关系1 - 11进行了讨论。化合物8表现出抗炎活性,IC 50值为0.36μM,这可能与通过抑制p65核易位和随后降低IL-6和TNF-α调节NF-κB信号通路有关。
更新日期:2017-07-28
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