银杏黄素抑制IκB-α的降解缓解LPS诱导的巨噬细胞炎症损伤  

Ginkgetin alleviates LPS-induced inflammatory damage in macrophages of mouse model via inhibiting IκB-αdegradation

作　　者：刘倩[1] 兰钦 李敏[1] 郑旭勇 陈高帜 张秀华[2] LIU Qian;LAN Qin;LI Min;ZHENG Xu-yong;CHEN Gao-zhi;ZHANG Xiu-hua(First Clinical Medical College,School of Information and Engineering,Wenzhou Medical University,Wenzhou Zhejiang 325035,China;First Affiliated Hospital of Wenzhou Medical University,Wenzhou Zhejiang 325000,China;School of Pharmaceutical Sciences,Wenzhou Medical University,Wenzhou Zhejiang 325000,China)

机构地区：[1]温州医科大学第一临床医学院、信息与工程学院,浙江温州325035 [2]温州医科大学附属第一医院,浙江温州325000 [3]温州医科大学药学院,浙江温州325000

出　　处：《中国药理学通报》2021年第4期550-555,共6页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81703352);浙江省医药卫生科技计划项目(2019KY448)。

摘　　要：目的探究天然化合物银杏黄素(Ginkgetin)对脂多糖(LPS)诱导的小鼠腹腔原代巨噬细胞的抗炎作用及其机制,为临床候选药物的开发提供理论依据。方法应用MTT检测试剂盒检测银杏黄素对小鼠腹腔原代巨噬的细胞毒性;运用ELISA、RT-qPCR方法检测不同浓度银杏黄素对LPS诱导的细胞炎症损伤模型的抗炎效果;通过Western blot法检测银杏黄素的抗炎机制。结果与LPS刺激组相比,Ginkgetin治疗组产生了浓度依赖性的抗炎效果,表现于Ginkgetin能显著抑制LPS诱导的IκB-α的降解,而对于LPS诱导的另一经典炎症通路MAPKs信号通路没有影响。MTT结果也表明银杏黄素对小鼠腹腔原代巨噬细胞的毒性较小。结论银杏黄素通过抑制IκB-α的降解从而缓解LPS诱导的小鼠腹腔原代巨噬细胞炎症损伤,有望成为天然单体抗炎候选药物。Aim To explore the anti-inflammatory effect of natural compound Ginkgetin on lipopolysac-charide-induced mouse primary peritoneal macrophages and the underlying mechanism, in order to provide a theoretical basis for the development of clinical drug candidates. Methods MTT test kit was used to detect the cytotoxicity of Ginkgetin on mouse primary peritoneal macrophages;ELISA and RT-qPCR methods were used to detect the anti-inflammatory effect of different concentrations of Ginkgetin on LPS-induced cell inflammation injury model;Western blot was used to detect the anti-inflammatory mechanism of ginkgo flavonoids. Results Compared with LPS stimulation group, Ginkgetin treatment group produced a concentration-dependent anti-inflammatory effect, which could be attributed to the fact that Ginkgetin could inhibit LPS-induced activation of NF-κB signaling pathway. MTT results also showed that ginkgo flavonoids had little toxicity to mouse primary peritoneal macrophages. Conclusions Ginkgelin alleviates LPS-induced inflammatory injury of mouse primary peritoneal macrophages by inhibiting the activation of NF-κB signaling pathway. It is expected to be a natural monomer anti-inflammatory drug candidate.

关 键 词：银杏黄素 小鼠腹腔原代巨噬细胞 抗炎作用 脂多糖 MAPKS IΚB-Α 

分 类 号：R-332[医药卫生] R284.1