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Bioorg Med Chem Lett ; 26(18): 4417-4422, 2016 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-27542306

RESUMO

Five new flavonoids, griffinones A-E (1-5), a new biphenylneolignan, griffilignan A (6) and ten known compounds were isolated from the n-hexane and EtOAc extracts of Millettia griffithii. The structures of the new compounds were determined by 1D and 2D NMR, and by HRMS. The anti-inflammatory activity of the isolated compounds was evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells. Among the isolated compounds, compounds 1, 2 and 14 showed significant anti-inflammatory activity with IC50 values of 20.4, 2.1 and 35.7µM, respectively and no obvious toxicities were observed at 100µM. Western blot and PCR assay further showed that inhibition of nitric oxide production by compound 2 was associated with suppression of iNOS expression. Modeling studies suggested that the amino group, phenyl ring as well as the isopentenyl tails of compound 2 could help bind to iNOs.


Assuntos
Anti-Inflamatórios/farmacologia , Flavonoides/farmacologia , Lignanas/farmacologia , Millettia/química , Caules de Planta/química , Animais , Linhagem Celular , Lipopolissacarídeos/toxicidade , Espectroscopia de Ressonância Magnética , Camundongos , Espectrometria de Massas por Ionização por Electrospray
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