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

ABSTRACT: 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 ?g/mL of each compound for one hour before induction of inflammation by lipopolysaccharide (1 ?g/mL) for 6 h. Some halo-chalcones and -azachalcones suppressed expression of pro-inflammatory factors toll-like receptor 4 (TLR4), I?B-?, transcription factor p65, interleukine 1? (IL-1?), IL-6, tumor necrosis factor ? (TNF-?), 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.

SUBMITTER: Shih TL 

PROVIDER: S-EPMC6017711 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature