Synthesis compound XCR-7a ameliorates LPS-induced inflammatory response by inhibiting the phosphorylation of c-Fos

Biomedicine & Pharmacotherapy

Qianqian Di¹  Haimei Tang²  Jiazheng Quan²  Yue Xiao²  Zherui Wu²  Weilie Xiao²  Jiajing Zhao²  Xingyu Ma²  Prasanta Roy³  Weilin Chen³ 

[1] Development Center for Natural Products, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China;Department of Immunology, School of Basic Medical School, Health Science Center, Shenzhen University, Shenzhen 518060, China;;Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Research &

关键词: XCR-7a;    LPS;    Inflammation;    Macrophage;    C-Fos;   

DOI  :  

来源: DOAJ

【 摘 要 】

Inflammation is a biological process closely related to different kinds of diseases, such as cancer and metabolic diseases. Therefore, effective control of the occurrence and development of inflammation is of great significance for disease prevention and control. Recently, 2-substituted indoles have gradually become a research hotspot because of their stability and pharmacological activity. Here we synthesized a series of compound containing 2-substituted indoles and investigated XCR-7a’s role in inflammatory response. Our data show that XCR-7a can inhibit the production of inflammatory cytokines interleukin-1 beta (IL-1β), interleukin-6 (IL-6) and inflammatory mediator cyclooxygenase-2 (COX-2) induced by lipopolysaccharide (LPS) in mouse peritoneal macrophages. Also, XCR-7a has a protective effect on LPS-induced inflammatory response in mice. Mechanically, we found that XCR-7a could inhibit the phosphorylation of c-Fos induced by LPS, which suggested that the protective effect of XCR-7a on inflammation was related to its negative regulation to phosphorylation of c-Fos. Briefly, our results demonstrated that XCR-7a could be expected to be a potential drug for controlling inflammation.

【 授权许可】

Unknown