Halo-substituted chalcones and azachalcones-inhibited, lipopolysaccharited-stimulated, pro-inflammatory responses through the TLR4-mediated pathway

Tzenge Lien Shih, Ming Hwa Liu, Chia Wai Li, Chia Feng Kuo*

*此作品的通信作者

研究成果: 期刊稿件文章同行評審

20 引文 斯高帕斯(Scopus)

摘要

A series of B-ring, halo-substituted chalcones and azachalcones were synthesized to evaluate and compare their anti-inflammatory activity. Mouse BALB/c macrophage RAW 264.7 were pre-treated with 10 μg/mL of each compound for one hour before induction of inflammation by lipopolysaccharide (1 μg/mL) for 6 h. Some halo-chalcones and -azachalcones suppressed expression of pro-inflammatory factors toll-like receptor 4 (TLR4), IκB-α, transcription factor p65, interleukine 1β (IL-1β), IL-6, tumor necrosis factor α (TNF-α), and cyclooxygenase 2 (COX-2). The present results showed that the synthetic halo-azachalcones exhibited more significant inhibition than halo-chalcones. Therefore, the nitrogen atom in this series of azachalcones must play a more crucial role than the corresponding C-2 hydroxyl group of chalcones in biological activity. Our findings will lay the background for the future development of anti-inflammatory nutraceuticals.

原文英語
文章編號597
期刊Molecules
23
發行號3
DOIs
出版狀態已出版 - 2018
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© 2018 by the authors.

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