OBJECTIVE The present study examined the potential of flavonoids in reducing airway inflammation and determined the structure activity relationships(SAR),if present,for their anti-inflammatory effects.METHODS Seventee...OBJECTIVE The present study examined the potential of flavonoids in reducing airway inflammation and determined the structure activity relationships(SAR),if present,for their anti-inflammatory effects.METHODS Seventeen flavonoids with different chemical structures were selected for the study.Inflammation was induced in human bronchial epithelial BEAS-2B cells with lipopolysaccharide(LPS).BEAS-2Bcells were incubated with or without different flavonoids(10μmol·L-1)1hbefore treatment with LPS(10μg·mL-1)for 24 h.The viability of the cells after exposure to LPS and/or flavonoids were determined by thiazolyl blue tetrazolium bromide(MTT)assay.The amount of the inflammatory mediators,interleukin(IL)-6,IL-8 and monocyte chemoattractant protein-1(MCP-1),were measured in the supernatants byenzyme-linked immunosorbent assay(ELISA).RESULTS Flavonoids(1to 10μmol·L-1)and LPS(1 to 10μg·mL-1)did not affect the viability of BEAS-2B cells.LPS(10μg·mL-1)significantly stimulated the release of IL-6,IL-8 and MCP-1 in BEAS-2B cells.Among the flavonoids tested,only apigenin,luteolin and genistein(10μmol·L-1)significantly inhibited the release of the inflammatory mediators.CONCLUSION These findings suggested that a hydroxy group at C5 and C7 positions in the A ring,a double bond between C2 and C3 and acarbonyl group at the C4 position in the C ring of the flavonoid might play an important role for their anti-inflammatory effect.The presence of a hydroxy group at C3 position or glycosylation at C3 or C7 position reduces the effectiveness of a flavonoid as an anti-inflammatory agent.展开更多
基金The project supported by the Health and Medical Research Fund of the Food and Health Bureau of Hong Kong SAR(11123011)
文摘OBJECTIVE The present study examined the potential of flavonoids in reducing airway inflammation and determined the structure activity relationships(SAR),if present,for their anti-inflammatory effects.METHODS Seventeen flavonoids with different chemical structures were selected for the study.Inflammation was induced in human bronchial epithelial BEAS-2B cells with lipopolysaccharide(LPS).BEAS-2Bcells were incubated with or without different flavonoids(10μmol·L-1)1hbefore treatment with LPS(10μg·mL-1)for 24 h.The viability of the cells after exposure to LPS and/or flavonoids were determined by thiazolyl blue tetrazolium bromide(MTT)assay.The amount of the inflammatory mediators,interleukin(IL)-6,IL-8 and monocyte chemoattractant protein-1(MCP-1),were measured in the supernatants byenzyme-linked immunosorbent assay(ELISA).RESULTS Flavonoids(1to 10μmol·L-1)and LPS(1 to 10μg·mL-1)did not affect the viability of BEAS-2B cells.LPS(10μg·mL-1)significantly stimulated the release of IL-6,IL-8 and MCP-1 in BEAS-2B cells.Among the flavonoids tested,only apigenin,luteolin and genistein(10μmol·L-1)significantly inhibited the release of the inflammatory mediators.CONCLUSION These findings suggested that a hydroxy group at C5 and C7 positions in the A ring,a double bond between C2 and C3 and acarbonyl group at the C4 position in the C ring of the flavonoid might play an important role for their anti-inflammatory effect.The presence of a hydroxy group at C3 position or glycosylation at C3 or C7 position reduces the effectiveness of a flavonoid as an anti-inflammatory agent.