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Structure-activity relationships for anti-inflammatory effect of flavonoids
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作者 PengZHANG judithcwmak +1 位作者 RickyYKMAN SusanWSLEUNG 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2015年第S1期110-110,共1页
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
关键词 FLAVONOIDS INTERLEUKIN-6 INTERLEUKIN-8 MONOCYTE CH
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