کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1393807 | 1501103 | 2016 | 12 صفحه PDF | دانلود رایگان |
• Compound 11k was more effective than resveratrol.
• (±)-11k, (+)-11k and (−)-11k, do not have impacts on activity and toxicity.
• (±)-11k could suppress iNOS, COX-2 expression and NO production.
• The mechanism of (±)-11k was through TLR4/JNK/NF-κB signaling pathway.
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.
Sesquistilbene indanone analogue 11k was much more potent than resveratrol for its anti-inflammatory activity. 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.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 113, 4 May 2016, Pages 63–74