GPER is involved in the anti-inflammatory effects of genistein in BV2 microglial cells
作者单位：Department of Physiology Shandong Provincial Key Laboratory of Pathogenesis and Prevention of Neurological Disorders Medical College of Qingdao University
会议名称：《中国神经科学学会第十二届全国学术会议》
会议日期：2017年
学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学]
关 键 词：genistein G protein-coupled estrogen receptor insulin-like growth factor 1 receptor microglia
摘 要：Objective Genistein is an isoflavonoid phytoestrogen extracted from leguminous plants exerting both estrogen agonist and antagonist activities. The present study hypothesized that the anti-inflammatory effects of genistein against lipopolysaccharide（LPS）-induced BV2 microglial activation might be mediated by membrane estrogen receptor（G-protein coupled estrogen receptor, GPER）. Methods The anti-inflammatory effects of genistein were investigated in LPS-induced microglial activation in murine BV2 cells. G1, the specific agonist of GPER, was used as a positive control. The pharmacological blockade and lentivirus-mediated si RNA knockdown of GPER were used to study the underlying mechanism. Results Genistein mimicked the effects of G1 treatment by inhibiting the LPS-induced gene expressions of inflammatory cytokines, including TNF-a, IL-1b, COX-2 and iNOS in BV2 microglial cells. Pretreatment with GPER antagonist G15 or si RNA knockdown of GPER could significantly block the anti-inflammatory effects of genistein and G1. Furthermore, pretreatment with G15 could also block the inhibitory effects of genistein on LPS-induced phosphorylation of JNK, p38, ERK and IkB. Conclusion Genistein exerts antin-inflammatory effects in BV2 microglial cells possibly by the activating GPER.