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Molecules 2018, 23(3), 597; doi:10.3390/molecules23030597

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

Department of Chemistry, Tamkang University, Tamsui Dist., New Taipei City 251, Taiwan
Department of Food Science, Nutrition, and Nutraceutical Biotechnology, Shih Chien University, Zhongshan Dist., Taipei 104, Taiwan
Author to whom correspondence should be addressed.
Received: 4 February 2018 / Revised: 28 February 2018 / Accepted: 4 March 2018 / Published: 7 March 2018
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: azachalcones; chalcones; anti-inflammation; toll-like receptor 4 azachalcones; chalcones; anti-inflammation; toll-like receptor 4

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Shih, T.-L.; Liu, M.-H.; Li, C.-W.; Kuo, C.-F. Halo-Substituted Chalcones and Azachalcones Inhibited Lipopolysaccharited-Stimulated Pro-Inflammatory Responses through the TLR4-Mediated Pathway. Molecules 2018, 23, 597.

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