化学
NF-κB
立体化学
抑制性突触后电位
化学合成
体外
生物化学
脂多糖
生物活性
药理学
体内
作者
Dilidaer Ajiaikebaier,Li Zuopeng,TzuChun Lin,Sun Xinyu,Wang Bianlin,Jing-Ya Li
标识
DOI:10.1016/j.bmcl.2021.128042
摘要
Abstract In an effort to identify novel inhibitors of nuclear factor kappa B (NF-κB), twenty five pyranochalcone derivatives were synthesized and evaluated for their in vitro activities against TNF-α induced NF-κB inhibition in HEK293T cells. Among all of these derivatives, several displaying the same acrylate moiety on the B ring exhibited potent inhibition, with IC50 values ranging from 0.29 to 10.46 μM. A functional study of the most potent of these compounds, designated 6b, revealed that it significantly suppressed the transcriptional expression of inflammatory factor IL-1β in lipopolysaccharide-induced RAW 264.7 macrophages, and also mildly inhibited CCL2, IL6 and TNF-α. In addition, compound 6b was found to inhibit IL-1β released in LPS-induced BMDM cells. This study demonstrates that the inhibitory effect of 6b on LPS-stimulated inflammatory mediator production in the mouse macrophage cell line RAW 264.7 correlates with the suppression of the NF-κB and MAPK signaling pathways.
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