RESUMO
A bioassay-guided phytochemical fractionation of the methanol extract of the Morus alba root barks led to the isolation of two chalcone-derived Diels-Alder adducts (1 and 2). Their structures were elucidated as kuwanon J 2,4,10â³-trimethyl ether (1) and kuwanon R (2) by means of spectroscopic methods. Both compounds strongly inhibited nuclear transcription factor.κB activity with the IC50 values of 4.65 and 7.38 µM, respectively.
Assuntos
Chalcona/isolamento & purificação , Morus/química , NF-kappa B/efeitos dos fármacos , Chalcona/química , Chalcona/farmacologia , Chalconas , Células HeLa , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Casca de Planta/química , Raízes de Plantas/química , VietnãRESUMO
OBJECTIVE@#To identify inhibitors of nitric oxide production and NF-κB activity from Chromolaena odorata (C. odorata).@*METHODS@#The compounds isolated from the aerial parts of C. odorata by bioassay-guided fractionation were investigated for their inhibitory effects on the NO production and NF-κB activity in LPS-stimulated RAW264.7 cells.@*RESULTS@#Six fatty acids (S)-coriolic acid (1), (S)-coriolic acid methyl ester (2), (S)-15,16-didehydrocoriolic acid (3), (S)-15,16-didehydrocoriolic acid methyl ester (4), linoleamide (5) and linolenamide (6) were isolated. All compounds inhibited the NO production at concentrations consistent with those required for NF-κB inhibition. Compound 2 was the most active with the IC(50) values of 5.22 and 5.73 μM. The addition of a double bond in the fatty chain decreased the inhibitory effects while the methyl esterification increased the activities.@*CONCLUSIONS@#The fatty acid components in C. odorata with NF-κB inhibitory activity could explain the anti-inflammation property of this plant in traditional medicine. This study could also contribute to the better use of C. odorata for human health care.
