文献类型：期刊文献

中文题名：Sarsasapogenin-AA13 inhibits LPS-induced inflammatory responses in macrophage cells in vitro and relieves dimethylbenzene-induced ear edema in mice

英文题名：Sarsasapogenin-AA13 inhibits LPS-induced inflammatory responses in macrophage cells in vitro and relieves dimethylbenzene-induced ear edema in mice

作者：Dong, Dong[1];Zhou, Nan-nan[1];Liu, Rui-xuan[1];Xiong, Jia-wei[1];Pan, Hui[1];Sun, Si-qi[1];Ma, Lei[1];Wang, Rui[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2017

卷号：38

期号：5

起止页码：699

中文期刊名：Acta Pharmacologica Sinica

外文期刊名：ACTA PHARMACOLOGICA SINICA

收录：CSTPCD;;Scopus;WOS:【SCI-EXPANDED(收录号:WOS:000400566600009)】；CSCD:【CSCD2017_2018】；PubMed;

基金：This project was supported by grants (to Rui WANG) from the National Natural Science Foundation of China (No 81072627), the 111 Project (No B07023) from the Ministry of Education, the Pujiang talent project (No 11PJ1402300), the Shanghai Biomedical Technology Support Program (No 15401901100), Shanghai Pujiang Program (15PJD012), and the Key project from Shanghai Science and Technology Committee (No 12431900901).

语种：英文

中文关键词：sarsasapogenin; AA13; antifani; anti-inflammation; inflammatory factor; nuclear factor-KB; mitogen-activated proteinkinases; ear edema

外文关键词：sarsasapogenin; AA13; antifani; anti-inflammation; inflammatory factor; nuclear factor-kappa B; mitogen-activated protein kinases; ear edema

摘要：Sarsasapogenin-AA13 （AA13） is a novel synthetic derivative of sarsasapogenin extracted from the Chinese herb Rhizoma Anemarrhenae. In this study we investigated the effects of AA13 on lipopolysaccharide （LPS）-induced production of inflammatory factors in macrophage cells and the anti-inflammatory activity of AA13 in an inflammatory model of dimethylbenzene-induced ear edema. Macrophage cells （RAW264.7 ceils and mouse peritoneal macrophages） were exposed to LPS （1 pg/mL）; pretreatment with AA13 （5-20 pmol/L） dose-dependently inhibited LPS-induced production of NO, TNF-a and PGE2, and LPS-stimulated expression levels of COX-2 and iNOS. Furthermore, pretreatment with AA13 dose-dependently suppressed LPS-stimulated phosphorylation of p38 and JNK, but had no effect on ERK in RAW264.7 cells. Moreover, pretreatment with AA13 inhibited LPS-induced activation of the nuclear factor （NF）-KB in RAW264.7 cells. The in vivo anti-inflammatory activity of AA13 was demonstrated in a mouse inflammatory model： pre-treatment with either AA13 （20 mg.kg-1.d-1, ig） or a positive control antifani （10 mg-k-1.d-1, ig） for 3 d significantly relieved dimethylbenzene-induced ear edema. Our results demonstrate that AA13 effectively inhibit LPS-induced inflammatory responses in macrophage cells in vitro and relieve dimethylbenzene-induced ear edema in vivo.
Sarsasapogenin-AA13 (AA13) is a novel synthetic derivative of sarsasapogenin extracted from the Chinese herb Rhizoma Anemarrhenae. In this study we investigated the effects of AA13 on lipopolysaccharide (LPS)-induced production of inflammatory factors in macrophage cells and the anti-inflammatory activity of AA13 in an inflammatory model of dimethylbenzene-induced ear edema. Macrophage cells (RAW264.7 cells and mouse peritoneal macrophages) were exposed to LPS (1 ae g/mL); pretreatment with AA13 (5-20 mu mol/L) dose-dependently inhibited LPS-induced production of NO, TNF-alpha and PGE(2), and LPS-stimulated expression levels of COX-2 and iNOS. Furthermore, pretreatment with AA13 dose-dependently suppressed LPS-stimulated phosphorylation of p38 and JNK, but had no effect on ERK in RAW264.7 cells. Moreover, pretreatment with AA13 inhibited LPS-induced activation of the nuclear factor (NF)-kappa B in RAW264.7 cells. The in vivo anti-inflammatory activity of AA13 was demonstrated in a mouse inflammatory model: pre-treatment with either AA13 (20 mg.kg(-1).d(-1), ig) or a positive control antifani (10 mg.kg(-1).d(-1), ig) for 3 d significantly relieved dimethylbenzene-induced ear edema. Our results demonstrate that AA13 effectively inhibit LPS-induced inflammatory responses in macrophage cells in vitro and relieve dimethylbenzene-induced ear edema in vivo.