Halo-Substituted Chalcones and Azachalcones-Inhibited, Lipopolysaccharited-Stimulated, Pro-Inflammatory Responses through the TLR4-Mediated Pathway

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题名:	Halo-Substituted Chalcones and Azachalcones-Inhibited, Lipopolysaccharited-Stimulated, Pro-Inflammatory Responses through the TLR4-Mediated Pathway
作者:	Shih,T.L;Liu, M.H;Li, C.W;Kuo,C.F
关键词:	anti-inflammation;azachalcones;chalcones;toll-like receptor 4
日期:	2018-03
上传时间:	2018-03-15 12:10:51 (UTC+8)
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.
關聯:	Molecules 23(3), p.597
DOI:	10.3390/molecules23030597
显示于类别:	[化學學系暨研究所] 期刊論文

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