Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 142036 - 142036
Опубликована: Март 1, 2025
Язык: Английский
Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 142036 - 142036
Опубликована: Март 1, 2025
Язык: Английский
Frontiers in Pharmacology, Год журнала: 2025, Номер 15
Опубликована: Янв. 20, 2025
Given the potent anti-inflammatory properties of 1,2,3-triazole structure and wide use 2H-1,4-benzoxazin-3(4H)-one in developing treatments for neurodegenerative diseases, a series derivatives were synthesized by introducing moiety. Screening activity microglial cells revealed that compounds e2, e16, e20 exhibited most promising effects without significant cytotoxicity. These effectively reduced LPS-induced NO production significantly decreased transcription levels pro-inflammatory cytokines IL-1β, IL-6, TNF-α. Furthermore, they downregulated protein inflammation-related enzymes iNOS COX-2 response to LPS stimulation. To further investigate mechanisms these microglia, intracellular ROS activation Nrf2-HO-1 signaling pathway analyzed. The results indicated activated pathway, production, alleviated inflammation. Molecular docking studies suggested could interact with Nrf2-related binding sites, preventing its degradation Keap1. Additionally, acute toxicity tests mice demonstrated compound e16 favorable safety.
Язык: Английский
Процитировано
1Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 142036 - 142036
Опубликована: Март 1, 2025
Язык: Английский
Процитировано
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