化合物W3D通过调控TLR4-MyD88-NF-κB通路抑制LPS诱导的RAW264.7细胞炎症因子的释放

被引：18

作者：

罗捷然 ^{[1
]}

赵蓓 ^{[1
]}

唐莉 ^{[1
]}

葛睿 ^{[1
]}

李青山 ^{[1
,2
]}

机构：

[1] 山西医科大学药学院

[2] 山西中医药大学中药学院

来源：

中国药理学通报 | 2018年 / 34卷 / 07期

关键词：

苯并噁唑酮衍生物W3D; RAW264.7细胞; 炎症; TLR4; MyD88; NF-κB; 炎症因子;

D O I：

暂无

中图分类号：

R965 [实验药理学];

学科分类号：

100706 [药理学];

摘要：

目的建立脂多糖(LPS)诱导的小鼠单核巨噬细胞(RAW264.7)炎症模型,探究新型苯并噁唑酮衍生物4-(5'-二甲氨基)-萘磺酰氧基苯并噁唑酮(W3D)的抗炎活性及其对TLR4-MyD88-NF-κB通路的调控作用。方法 MTT法测定化合物W3D对细胞活力的影响;LPS与不同浓度的化合物W3D共同作用RAW264.7细胞后,ELISA法测定细胞上清液中TNF-α、IL-6、IL-1β、COX-2的含量,Western blot法检测IL-6、TLR4、MyD88、IRAK4、NF-κB的蛋白表达;实时荧光定量PCR法检测细胞中TLR4、MyD88、IL-6 mRNA的表达。结果化合物W3D对LPS诱导的RAW264.7细胞培养液中炎症因子TNF-α、IL-6、IL-1β的分泌有明显的抑制作用,但对COX-2无抑制活性;可明显下调TLR4、MyD88、IL-6的蛋白与mRNA的表达,抑制IRAK4磷酸化和NF-κB的入核活化。结论化合物W3D可通过调控TLR4-MyD88-IRAK4-NF-κB信号通路,抑制TNF-α、IL-6、IL-1β等炎症因子的释放而发挥抗炎活性。

引用

页码：977 / 982

页数：6

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