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 ...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）,（5）-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<sub>50</sub> values of 5.22 and 5.73μM. 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.展开更多
基金supported by the grant from the International Foundation for Science(No.F/4729-1)
文摘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）,（5）-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<sub>50</sub> values of 5.22 and 5.73μM. 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.
