lobolideaditerpeneblockadesthenfbpathwayandp38anderkmapkactivityinmacrophagesinvitro
文献类型：期刊论文
| 作者 | Lv Xiaofen; Chen Sihan; Li Jie; Fang Jianping; Guo Yuewei ; Ding Kan
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2012 |
| 卷号 | 033期号:010页码:1293 |
| 关键词 | 巨噬细胞 MAPK ERK p38 通路 二萜 封锁 活性 |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim： Recent studies have shown that constitutive activation of the nuclear factor κB （NF-κB） plays a key role in chronic inflammation and cancers. The aim of this study was to characterize lobolide, a cembrane diterpene, as a drug candidate targeting the NF-κB signaling pathway. Methods： A HEK 293/NF-κB-luc stable cell line was constructed to evaluate the effect of lobolide on NF-κB activation. THP-1 human monocytes and peripheral blood mononuclear cells （PBMCs） from healthy volunteers were tested. Lipopolysaccharide （LPS）-induced TNFα and IL-1β production and activation of the TAK1-IKK-NF-κB pathway were studied using ELISA and Western blot analysis.Results： In HEK 293/NF-κB-luc stable cells, lobolide （0.19–50 μmol/L） inhibited NF-κB activation in a concentration-dependent manner with an IC50 value of 4.2±0.3 μmol/L. Treatment with lobolide （2.5–10 μmol/L） significantly suppressed LPS-induced production of TNFα and IL-1β in both THP-1 cells and PBMCs. In THP-1 cells, the suppression was partially caused by blockade of the translocation of NF-κB from the cytoplasm to the nucleus via affecting the TAK1-IKK-NF-κB pathway and p38 and ERK MAPK activity.Conclusion： Lobolide is a potential inhibitor of the NF-κB pathway, which blocks the translocation of NF-κB from the cytoplasm to the nucleus. Lobolide inhibits LPS-stimulated TNFα and IL-1β release, suggesting that the compound might be an anti-inflammatory compound. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/286062]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Lv Xiaofen,Chen Sihan,Li Jie,et al. lobolideaditerpeneblockadesthenfbpathwayandp38anderkmapkactivityinmacrophagesinvitro[J]. actapharmacologicasinica,2012,033(010):1293. |
| APA | Lv Xiaofen,Chen Sihan,Li Jie,Fang Jianping,Guo Yuewei,&Ding Kan.(2012).lobolideaditerpeneblockadesthenfbpathwayandp38anderkmapkactivityinmacrophagesinvitro.actapharmacologicasinica,033(010),1293. |
| MLA | Lv Xiaofen,et al."lobolideaditerpeneblockadesthenfbpathwayandp38anderkmapkactivityinmacrophagesinvitro".actapharmacologicasinica 033.010(2012):1293. |
入库方式： OAI收割
来源：上海药物研究所
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