旋覆花来源的几种抗炎活性物质（英文）

【作者】 金美花； 陈曦； Eunkyung Lee； 孔德新；

【Author】 Eunkyung Lee;Research and Development Division,Korean Promotion Institute for Traditional Medicine Industry;

【机构】 天津医科大学药学院生物制药教研室、基础医学研究中心分子靶向药物研究室； Research and Development Division,Korean Promotion Institute for Traditional Medicine Industry；

【摘要】 Our previous study showed that the extract of Inula japonica Thunb(I.japonica)has anti-inflammatory and anti-asthmatic activities.Recently,we isolated1,6a-dihydroxy-4aH-1,10-secoeudesma-5(10),11(13)-dien-12,8b-olide(SE),6a-isobutyryloxy-1-hydroxy-4aH-1,10-secoeudesma-5(10),11(13)-dien-12,8b-olide(IBSE),and6a-isovaleryloxy-1-hydroxy-4aH-1,10-secoeudesma-5(10),11(13)-dien-12,8b-olide(IVSE),and investigated their inhibitory effects on nitric oxide(NO)production in LPS-stimulated RAW264.7 cells.Among them,IVSE displayed the most potent inhibition of NO production.Then we investigated the potential anti-inflammatory mechanism.IVSE dramatically decreased the expression of inducible nitric oxide synthase(i NOS),reduced the translocation of the Nuclear factorkB(NF-kB)subunit p65 into the nucleus by interrupting the phosphorylation and degradation of inhibitor kappa B(IkB)-a,and inhibited the activation of the upstream mediator Ik B kinase Ik B kinasea/b(IKKa/b).Furthermore,our results indicated that IVSE inhibited the phoshorylation of mitogen-activated protein kinases(MAPKs)including extracellular regulated kinases(ERK1/2),c-Jun N-terminal kinases(JNK)and p38.Taken together,our results showed that IVSE exhibited anti-inflammatory activity by inhibiting NO production,in which inactivation of NF-kB and MAPKs might be involved.更多还原

【Abstract】 Our previous study showed that the extract of Inula japonica Thunb(I.japonica) has anti-inflammatory and anti-asthmatic activities.Recently,we isolated1,6?-dihydroxy-4?H-1,10-secoeudesma-5(10),11(13)-dien-12,8?-olide(SE),6?-isobutyryloxy-1-hydroxy-4?H-1,10-secoeudesma-5(10),11(13)-dien-12,8?-olide(IBSE),and6?-isovaleryloxy-1-hydroxy-4?H-1,10-secoeudesma-5(10),11(13)-dien-12,8?-olide(IVSE),and investigated their inhibitory effects on nitric oxide(NO) production in LPS-stimulated RAW264.7 cells.Among them,IVSE displayed the most potent inhibition of NO production.Then we investigated the potential anti-inflammatory mechanism.IVSE dramatically decreased the expression of inducible nitric oxide synthase(i NOS),reduced the translocation of the Nuclear factor ?B(NF-?B) subunit p65 into the nucleus by interrupting the phosphorylation and degradation of inhibitor kappa B(I?B)-?,and inhibited the activation of the upstream mediator Ik B kinase Ik B kinase ???(IKK ???).Furthermore,our results indicated that IVSE inhibited the phoshorylation of mitogen-activated protein kinases(MAPKs) including extracellular regulated kinases(ERK1/2),c-Jun N-terminal kinases(JNK) and p38.Taken together,our results showed that IVSE exhibited anti-inflammatory activity by inhibiting NO production,in which inactivation of NF-?B and MAPKs might be involved.更多还原