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
Objective: To examine the in vitro and in vivo anti-inflammatory effects of the alkaloid enriched extract(ELA) from the roots of Eurycoma longifolia. Methods: The in vitro antiinflammatory effects of ELA were evaluate...Objective: To examine the in vitro and in vivo anti-inflammatory effects of the alkaloid enriched extract(ELA) from the roots of Eurycoma longifolia. Methods: The in vitro antiinflammatory effects of ELA were evaluated by examining its inhibitory activities against nitric oxide(NO) production and inducible nitric oxide synthase(iN OS) and cyclooxygenase2(COX-2) expressions in lipopolysaccharide(LPS)-stimulated RAW264.7 cells. The level of NO produced in the culture media was determined by Griess method. The i NOS and COX-2 protein expressions were analyzed by Western blot. The in vivo effect of ELA was evaluated on LPS-induced septic shock in mice model. Mice mortality was monitored for5 days after injection of LPS. The chemical contents of the ELA were determined by using various chromatographic and spectroscopic techniques. Results: The ELA was found to exhibit a significant anti-inflammatory effect in both in vitro and in vivo models. The results demonstrated that ELA dose-dependently inhibited LPS-induced NO production as well as the protein iN OS and COX-2 expressions. In the septic shock model, ELA dose-dependently protected mice from LPS-induced mortality. Further study on the isolated components of ELA indicated that 9,10-dimethoxycanthin-6-one may contribute significantly to the antiinflammatory effects of the extract. Conclusions: These results suggest that ELA exhibits the anti-inflammatory activity via suppression of pro-inflammatory mediators such as NO, iN OS,and COX-2 and protects mice from LPS-induced mortality in septic shock model.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.
基金funded by Vietnam Academy of Science and Technology under grant number VAST04.03/17-18
文摘Objective: To examine the in vitro and in vivo anti-inflammatory effects of the alkaloid enriched extract(ELA) from the roots of Eurycoma longifolia. Methods: The in vitro antiinflammatory effects of ELA were evaluated by examining its inhibitory activities against nitric oxide(NO) production and inducible nitric oxide synthase(iN OS) and cyclooxygenase2(COX-2) expressions in lipopolysaccharide(LPS)-stimulated RAW264.7 cells. The level of NO produced in the culture media was determined by Griess method. The i NOS and COX-2 protein expressions were analyzed by Western blot. The in vivo effect of ELA was evaluated on LPS-induced septic shock in mice model. Mice mortality was monitored for5 days after injection of LPS. The chemical contents of the ELA were determined by using various chromatographic and spectroscopic techniques. Results: The ELA was found to exhibit a significant anti-inflammatory effect in both in vitro and in vivo models. The results demonstrated that ELA dose-dependently inhibited LPS-induced NO production as well as the protein iN OS and COX-2 expressions. In the septic shock model, ELA dose-dependently protected mice from LPS-induced mortality. Further study on the isolated components of ELA indicated that 9,10-dimethoxycanthin-6-one may contribute significantly to the antiinflammatory effects of the extract. Conclusions: These results suggest that ELA exhibits the anti-inflammatory activity via suppression of pro-inflammatory mediators such as NO, iN OS,and COX-2 and protects mice from LPS-induced mortality in septic shock model.