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新型倍半萜茚满酮类似物作为强效抗炎剂的发现。

Discovery of novel sesquistilbene indanone analogues as potent anti-inflammatory agents.

作者信息

Tang Mei-Lin, Zhong Chen, Liu Zheng-Yu, Peng Peng, Liu Xin-Hua, Sun Xun

机构信息

Department of Natural Products Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.

Department of Pharmacology, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.

出版信息

Eur J Med Chem. 2016 May 4;113:63-74. doi: 10.1016/j.ejmech.2016.02.021. Epub 2016 Feb 8.

Abstract

To develop novel anti-inflammatory agents with improved pharmaceutical profiles, twenty-eight novel sesquistilbene indanone analogues were synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. Among these compounds, compound 11k was found to be one of the most potent analogues in inhibiting NO production in LPS-stimulated RAW264.7 cells. Furthermore, it could also significantly suppress LPS-induced iNOS and COX-2 expression and NO production through TLR4/JNK/NF-κB signaling pathway in a concentration dependent manner.

摘要

为了开发具有改善药学特性的新型抗炎剂,合成了28种新型倍半萜茚满酮类似物,并使用RAW264.7细胞评估其抗炎活性。在这些化合物中,化合物11k被发现是抑制LPS刺激的RAW264.7细胞中NO产生的最有效类似物之一。此外,它还可以通过TLR4/JNK/NF-κB信号通路以浓度依赖的方式显著抑制LPS诱导的iNOS和COX-2表达以及NO产生。

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