2-环戊氨基-5,8-二甲氧基-1,4-萘醌抑制LPS诱导的RAW264.7细胞内ROS水平与NO的分泌  

2-Cyclopentylamino-5,8-Dimethoxy-1,4-Naphthoquinone Inhibited the LPS Induced ROS and NO Production in RAW264.7 Cells

作　　者：刘磊[1] 申贵男 冯丽[1] 韩英浩[1] 罗英花[2] 金颖华[3] 金成浩[1] 崔玉东[1] 孙虎男[1] 

机构地区：[1]黑龙江八一农垦大学生命科学技术学院,大庆163319 [2]黑龙江八一农垦大学动物科学技术学院,大庆163319 [3]黑龙江八一农垦大学图书馆,大庆163319

出　　处：《中国细胞生物学学报》2015年第4期514-521,共8页Chinese Journal of Cell Biology

基　　金：黑龙江省教育厅科研基金(批准号:1251H010);国家教育部留学回国人员科研启动基金(第46批)资助的课题~~

摘　　要：炎症反应过程中有效控制巨噬细胞一氧化氮(niric oxide,NO)的过度分泌和细胞内活性氧(reactive oxygen species,ROS)水平,对抑制LPS诱导的巨噬细胞过度活化和巨噬细胞介导的急性炎症反应具有重要的临床意义。该研究检测了以5,8-二甲氧基-1,4-萘醌(5,8-dimethoxy-1,4-naphthoquinone,DMNQ)为中间体,通过有机合成反应获得的6种新萘醌类衍生物对LPS诱导的RAW264.7细胞NO分泌和细胞内ROS水平的抑制效果及其机理。结果显示,在6种新合成的化合物中,2-环戊氨基-5,8-二甲氧基-1,4-萘醌具有明显抑制RAW264.7细胞NO分泌和细胞内ROS水平的效果,同时不影响细胞的吞噬能力。另外,通过对细胞信号传导通路的分析发现,#6化合物能够有效地抑制ROS依赖性的ERK和JNK磷酸化水平,最终发挥降低LPS诱导的RAW264.7细胞NO分泌和i NOS蛋白质表达的作用。In inflammation processes, controlling the macrophage nitric oxide（NO） production and cellular reactive oxygen species（ROS） levels are the essential tools for inhibiting the LPS induced macrophage hyper-activation and macrophage mediated acute inflammation responses. In the present study, we examined the inhibitory effect of 5,8-dimethoxy-1,4-naphthoquinone（DMNQ） derivatives on LPS induced NO production and cellular ROS level in RAW264.7 macrophage cells. The results showed that among the six compounds, 2-Cyclopentylamino-5,8-dimethoxy-1,4-naphthoquinone significantly inhibited NO production and cellular ROS level in RAW264.7 cells, though it did not affect the cell phagocytosis. Furthermore, the signaling pathway studies showed that #6 compound significantly down-regulated the ROS dependent activation of ERK and JNK signaling pathway through inhibiting their phosphorylations, to decrease the NO production and inducible nitric oxide synthase（i NOS） protein expression.

关 键 词：萘醌类衍生物 一氧化氮 活性氧 炎症 

分 类 号：Q78[生物学—分子生物学]