体内
一氧化氮
化学
一氧化氮合酶
MMP3型
肿瘤坏死因子α
药理学
消炎药
体外
维加维斯
促炎细胞因子
生物化学
炎症
生物
医学
免疫学
基因表达
病理
替代医学
生物技术
有机化学
中医药
基因
作者
Enjing Cui,Shihu Qian,Jiaming Li,Xueyang Jiang,Hongwei Wang,Shuaishuai Du,Le Du
标识
DOI:10.1021/acs.jnatprod.3c00309
摘要
Coixol, a derivative of 2-benzoxazolinone extracted from coix (Coix lachryma-jobi L. var. ma-yuen Stapf), has demonstrated promising anti-inflammatory activity and low cytotoxicity. In this study, 26 coixol derivatives were designed and synthesized by hybridization with cinnamic acid to identify new anti-inflammatory agents. The anti-inflammatory activities of the derivatives were screened using LPS-induced overexpression of nitric oxide (NO) in RAW264.7 macrophages. On the basis of the screening results, compounds containing furan (9c) or nitrofuran (9j) moieties displayed more pronounced activity than coixol and celecoxib. Mechanistic investigations revealed that 9c and 9j suppressed the expression of induced nitric oxide synthase (iNOS), tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β, which was associated with the inhibition of the nuclear factor (NF)-κB signaling pathway. In vivo studies confirmed the anti-inflammatory activity of 9c and 9j in a xylene-induced mice auricles edema model. The preliminary in vitro and in vivo research findings suggest that 9c and 9j have the potential to be developed as anti-inflammatory agents.
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