Structure-Activity Relationship and Molecular Docking of Quinazolinones Inhibiting Expression of COX-2, IL-1β, iNOS, and TNF-α through NF-κB Pathways.

ABSTRACT: 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 nuclea

SUBMITTER: Kerdphon S 

PROVIDER: S-EPMC10510524 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature