喹啉酮
化学
肿瘤坏死因子α
一氧化氮合酶
基因表达
对接(动物)
酶
一氧化氮
细胞培养
NF-κB
药理学
生物化学
分子生物学
基因
生物
信号转导
免疫学
立体化学
医学
护理部
有机化学
遗传学
作者
Sutthichat Kerdphon,Nopawit Khamto,Kittisak Buddhachat,Jatuporn Ngoenkam,Pussadee Paensuwan,Sutatip Pongcharoen,Thishana Singh,Puttinan Meepowpan,Jira Jongcharoenkamol
标识
DOI:10.1021/acsmedchemlett.3c00098
摘要
The quinazolinone scaffold is found in natural products and biologically active compounds, including inflammatory inhibitors. Major proteins or enzymes involved in the inflammation process are regulated by the amount of gene expression. Quinazolinone derivatives were investigated and developed against the inflammatory genes cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and inducible nitric oxide synthase (iNOS) in the lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cell line. The mRNA expressions were measured using a real-time quantitative polymerase chain reaction (RT-qPCR). Quinazolinone compounds at 62.5 μM demonstrated anti-COX-2 and anti-IL-1β mRNA expressions down to 0.50% and 3.10% gene expression, respectively, via inhibition of nuclear factor κB (NF-κB). Molecular docking was performed to explain the interaction between the binding site and the developed compounds as well as the structure–activity relationship of the quinazolinone moiety.
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