NF-κB抑制剂DHMEQ对小鼠小胶质细胞炎性细胞因子分泌的抑制作用

Inhibition of inflammatory cytokine secretion from mouse microglia cells by DHMEQ, an NF-kappaB inhibitor.

作者信息

Takatsuna H, Morita S, Nagatsu T, Sawada M, Umezawa K

机构信息

Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Yokohama 223-0061, Japan.

出版信息

Biomed Pharmacother. 2005 Jul;59(6):318-22. doi: 10.1016/j.biopha.2005.01.011.

DOI:10.1016/j.biopha.2005.01.011

PMID:15932789

Abstract

Activation of microglia has been implicated in various neurodegenerative disorders, and thus the inhibition of microglial activity may suppress these disorders. Earlier we designed and synthesized an NF-kappaB inhibitor, dehydroxymethylepoxyquinomicin (DHMEQ) that showed anti-inflammatory and anti-tumor activities in vivo. In the present research, we studied whether DHMEQ would inhibit the activation of mouse microglial cells. DHMEQ inhibited lipopolysaccharide (LPS)-induced activation of NF-kappaB in an electrophoresis mobility shift assay. It also inhibited LPS-induced secretions of TNF-alpha and IL-6 from mouse microglial cell line 6-1 cells.

摘要

小胶质细胞的激活与多种神经退行性疾病有关，因此抑制小胶质细胞活性可能会抑制这些疾病。此前我们设计并合成了一种NF-κB抑制剂——去羟甲基环氧喹霉素（DHMEQ），它在体内表现出抗炎和抗肿瘤活性。在本研究中，我们研究了DHMEQ是否会抑制小鼠小胶质细胞的激活。在电泳迁移率变动分析中，DHMEQ抑制了脂多糖（LPS）诱导的NF-κB激活。它还抑制了LPS诱导的小鼠小胶质细胞系6-1细胞分泌肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）。