橙皮素
化学
炎症
药理学
一氧化氮
肿瘤坏死因子α
肝损伤
体内
脂多糖
一氧化氮合酶
活性氧
生物化学
立体化学
抗氧化剂
免疫学
类黄酮
医学
有机化学
生物
生物技术
作者
Yan Zheng,Yilong Zhang,Zeng Li,Wen Shi,Yongming Ji,Yahui Guo,Cheng Huang,Guangmin Sun,Jun Li
标识
DOI:10.1016/j.ejmech.2021.113162
摘要
Based on the previous research results of our research group, to further improve the anti-inflammatory activity of hesperetin, we substituted triazole at the 7-OH branch of hesperetin. We also evaluated the anti-inflammatory activity of 39 new hesperetin derivatives. All compounds showed inhibitory effects on nitric oxide (NO) and inflammatory factors in lipopolysaccharide-induced RAW264.7 cells. Compound d5 showed a strong inhibitory effect on NO (half maximal inhibitory concentration = 2.34 ± 0.7 μM) and tumor necrosis factor-α, interleukin (IL)-1β, and (IL-6). Structure–activity relationships indicate that 7-O-triazole is buried in a medium-sized hydrophobic cavity that binds to the receptor. Compound d5 can also reduce the reactive oxygen species production and significantly inhibit the expression of inducible NO synthase and cyclooxygenase-2 through the nuclear factor-κB signaling pathway. In vivo results indicate that d5 can reduce liver inflammation in mice with acute liver injury (ALI) induced by CCI4. In conclusion, d5 may be a candidate drug for treating inflammation associated with ALI.
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