Six new ellagitannins, brevipetins B-G ( and -), and a new phenolic glucoside, brevipetin A (), along with six known compounds were isolated from the traditional Chinese medicinal plant . Their structures and absolute configurations were determined by spectroscopic analyses, chemical methods, and TD-DFT-ECD calculations. Compounds - exhibited NO inhibitory effects with IC values of 1.9-8.2 μM, and showed the most potent inhibitory effect (IC: 1.9 μM). An in vivo anti-inflammatory assessment of showed that it exerts therapeutic effects in both the carrageenan-induced rat paw edema and collagen-induced arthritis (CIA) models at 50 mg/kg oral administration. The enhanced protein and mRNA expression levels of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2) in LPS-stimulated RAW 264.7 cells were dose-dependently suppressed by . An anti-inflammatory mechanistic study revealed that suppressed NF-κB activity by inhibiting IκBα phosphorylation and blocking translocation of p65 from the cytosol to the nucleus. Therefore, might have the potential to be developed as a lead compound for relieving rheumatoid arthritis.
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http://dx.doi.org/10.1021/acs.jnatprod.8b00984 | DOI Listing |
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