Magro Fernando, Fraga Sónia, Soares-da-Silva Patrício
Faculty of Medicine, Institute of Pharmacology and Therapeutics, 4200-319 Porto, Portugal.
Br J Pharmacol. 2005 May;145(1):93-103. doi: 10.1038/sj.bjp.0706167.
The present study evaluated the effect of interferon-gamma (IFN-gamma) on intestinal Na+/H+ exchange (NHE) activity and the intracellular signaling pathways set into motion after IFN-gamma receptor activation. Caco-2 cells express endogenous NHE1, NHE2 and NHE3 proteins, as detected by immunoblotting. Short- (0.5 h) and long- (24 h) term exposure of Caco-2 cells to IFN-gamma resulted in a concentration-dependent decrease in NHE activity. Inhibition of NHE activity by IFN-gamma was absent in cariporide-treated cells, but not in cells treated with S-3226. The long-term exposure to IFN-gamma was accompanied by a 20% increase in surface NHE1 abundance and no changes in total NHE1 abundance. Inhibition of Raf1, mitogen-activated protein kinase kinase (MAPKK/MEK) and p38 MAPK with, respectively, GW 5074, PD 98059 and SB 203580 and downregulation of protein kinase C (PKC) with phorbol-12,13-dibutyrate (100 nM for 24 h) prevented inhibition of NHE activity by IFN-gamma (0.5 and 24 h exposure). The signal transducer and activator transcription factor 1 (STAT1) inhibitor epigallocatechin-3-gallate (EGCG) prevented inhibition of NHE activity by long- but not the short-term treatment with IFN-gamma. Treatment with IFN-gamma activated phospho-p38 MAPK, this effect being detected as early as 1 h, persisting over 3 h and decreasing after 24 h. IFN-gamma produced a sustained action of phospho-STAT1 that was prevented by EGCG and partially attenuated by SB 203580 and insensitive to downregulation of PKC. In conclusion, short- and long-term inhibition of NHE1 activity by IFN-gamma involves a complex signaling pathway that includes PKC activation and STAT1 phosphorylation, respectively, but is not accompanied by downregulation of NHE1.
本研究评估了γ-干扰素(IFN-γ)对肠道Na⁺/H⁺交换(NHE)活性以及IFN-γ受体激活后启动的细胞内信号通路的影响。通过免疫印迹检测发现,Caco-2细胞表达内源性NHE1、NHE2和NHE3蛋白。Caco-2细胞短期(0.5小时)和长期(24小时)暴露于IFN-γ会导致NHE活性呈浓度依赖性降低。在使用卡立泊来德处理的细胞中,IFN-γ对NHE活性的抑制作用不存在,但在使用S-3226处理的细胞中则存在。长期暴露于IFN-γ会伴随着表面NHE1丰度增加20%,而总NHE1丰度无变化。分别用GW 5074、PD 98059和SB 203580抑制Raf1、丝裂原活化蛋白激酶激酶(MAPKK/MEK)和p38 MAPK,并用佛波醇-12,13-二丁酸酯(100 nM,处理24小时)下调蛋白激酶C(PKC),可防止IFN-γ(暴露0.5和24小时)对NHE活性的抑制。信号转导和转录激活因子1(STAT1)抑制剂表没食子儿茶素-3-没食子酸酯(EGCG)可防止长期但不能防止短期IFN-γ处理对NHE活性的抑制。用IFN-γ处理可激活磷酸化p38 MAPK,这种效应最早在1小时即可检测到,持续超过3小时,并在24小时后降低。IFN-γ产生了磷酸化STAT1的持续作用,这种作用可被EGCG阻止,并被SB 203580部分减弱,且对PKC下调不敏感。总之,IFN-γ对NHE1活性的短期和长期抑制涉及复杂的信号通路,分别包括PKC激活和STAT1磷酸化,但不伴有NHE1的下调。