关键词: CysLT2受体, HAMI3379, 炎性反应, PKCα/NF-κB信号通路

Abstract: Objective To investigate the role and possible mechanism of CysLT2 receptor antagonist HAMI3379 on the inflammatory response of mouse microglia (BV-2) induced by LPS. Methods BV-2 cells were divided into control group, LPS (100 ng/mL) group, HAMI3379 (0.01, 0.1 and 1 μmol/mL) group and LPS+HAMI3379 group. The proliferation of BV-2 cells was detected by CCK-8 assay. The contents of cytokines IL-1β, TNF-α and IL-10 were measured by ELISA assay. Western blot was used to detect the expression of PKCα,IKBα,NF-κB p50 and p65 protein. Results LPS significantly induced the activation of BV-2 cells and promoted proliferation of cells(P＜0.05). The secretion of inflammatory factors IL-1β and TNF-α was significantly increased and the secretion of IL-10 was obviously reduced in cell supernatant(P＜0.05). The expression of PKCα, IKBα and p65 proteins were significantly up-regulated(P＜0.05). The CysLT2 receptor antagonist HAMI3379 was able to reduce these changes. Conclusions The CysLT2 receptor antagonist HAMI3379 may inhibit the activation of BV-2 cells induced by LPS and reduce the inflammatory response, and the possible mechanism is related to the inhibition of PKCα/NF-κB signaling pathway.

Key words: CysLT2 receptor, HAMI3379, inflammation, PKCα/NF-κB signaling pathway