AI Article Synopsis
- A study focused on 24 derivatives of natural pyranochalcones was conducted to evaluate their ability to inhibit nitric oxide production in LPS-stimulated RAW264.7 cells.
- Four compounds (5b, 5d, 5f, and 5h) were identified as being more effective than indomethacin in inhibiting iNOS activity and NO production.
- Compound 5b showed promising results in reducing hind paw edema and arthritis symptoms, demonstrating its potential as an iNOS inhibitor through docking studies.
Article Abstract
24 derivatives (5a-x) derived from natural pyranochalcones (I and II) were designed and evaluated for their inhibitory potency on the production of nitric oxide (NO) in LPS-stimulated RAW264.7 cells. Among them, four compounds (5b, 5d, 5f, and 5h) exhibited more potent inhibitory effects on iNOS activity and iNOS-mediated NO production than a positive control indomethacin. Furthermore, 5b could significantly suppress the progression of carrageenan-induced hind paw edema compared to indomethacin at a dosage of 10 mg/kg/day, and dose-dependently ameliorated the development of adjuvant-induced arthritis (AIA) validated by arthritic scores and H&E staining of joints. In addition, docking study confirmed that 5b was an iNOS inhibitor with binding to the active site of murine iNOS.
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| http://dx.doi.org/10.1016/j.ejmech.2012.05.005 | DOI Listing |
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