水飞蓟宾
水飞蓟
p38丝裂原活化蛋白激酶
MAPK/ERK通路
一氧化氮
化学
免疫印迹
药理学
一氧化氮合酶
磷酸化
生物化学
细胞生物学
生物
医学
传统医学
基因
有机化学
作者
Cha Kyung Youn,Seon Joo Park,Min Young Lee,Man Tong Jin,Ok Hyeun Kim,Ho Jin You,In Youp Chang,Sang Pil Yoon,Young Jin Jeon
出处
期刊:Biomolecules & Therapeutics
[The Korean Society of Applied Pharmacology]
日期:2013-07-31
卷期号:21 (4): 258-263
被引量:56
标识
DOI:10.4062/biomolther.2013.044
摘要
We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR showed that silibinin inhibits iNOS, TNF-α, and IL1β. We also showed that silibinin strongly inhibits p38 MAPK phosphorylation, whereas the ERK1/2 and JNK pathways are not inhibited. The p38 MAPK inhibitor abrogated the LPS-induced nitrite production, whereas the MEK-1 inhibitor did not affect the nitrite production. A molecular modeling study proposed a binding pose for silibinin targeting the ATP binding site of p38 MAPK (1OUK). Collectively, this series of experiments indicates that silibinin inhibits macrophage activation by blocking p38 MAPK signaling.
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