Cheng T H, Shih N L, Chen S Y, Loh S H, Cheng P Y, Tsai C S, Liu S H, Wang D L, Chen J J
Institute of Biomedical Sciences, Academia Sinica, Taipei, Taiwan, ROC.
J Mol Cell Cardiol. 2001 Oct;33(10):1805-14. doi: 10.1006/jmcc.2001.1444.
Endothelin-1 (Et-1) is a peptide synthesized by endothelial cells (ECs) both in culture and in vivo. Cyclic strain induces gene expression of Et-1, however, the molecular mechanisms remain unclear. Since cyclic strain induces a sustained increase in intracellular reactive oxygen species (ROS), we hypothesized that the ROS could be a modulator in strain-induced Et-1 gene expression. Human umbilical vein ECs (HUVECs) subjected to cyclic strain had increased Et-1 secretion. Pretreatment of HUVECs with antioxidants, catalase (300 U/ml) or 1,3-dimethyl-2-thiourea (DMTU, 0.1 mm), abolished the strain-induced Et-1 release. ECs strained for 6 h had elevated Et-1 mRNA levels. In contrast, ECs treated with catalase or DMTU did not have increase Et-1 mRNA levels stimulated by cyclic strain. Bovine aortic ECs (BAECs) transfected with fusion plasmid containing Et-1 5'-flanking sequence (4.4 kb) and chloramphenicol acetyltransferase reporter gene produced a maximal Et-1 promoter activity after undergoing strain for 6 h, whereas pretreatment with catalase decreased this activity. BAECs cotransfected with a dominant negative mutant of Ras (RasN17), Raf-1 (Raf301), or catalytically inactive mutant of extracellular signal-regulated kinase (mERK2) had inhibited strain-induced Et-1 promoter activity, indicating the Ras/Raf/ERK pathway was involved; moreover, ERK phosphorylation was induced in ECs which were strained. This strain-activated ERK phosphorylation was attenuated in the presence of catalase. Functional analysis of the Et-1 promoter with site-directed mutagenesis indicates that the activator protein-1 (AP-1) binding site had to be within 143 base-pairs upstream of transcription initiation site for strain-induced promoter activity. Pretreatment of ECs with catalase also decreased the strain-induced promoter activity in the minimal construct (-143 bp). Our data demonstrate that strain-induced Et-1 gene expression is modulated by ROS via Ras/Raf/ERK signaling pathway, and indicate the responsiveness of the AP-1 binding site for strain-induced Et-1 expression.
内皮素 -1(Et-1)是一种在内皮细胞(ECs)体外培养和体内均能合成的肽。循环应变可诱导Et-1的基因表达,然而其分子机制仍不清楚。由于循环应变可导致细胞内活性氧(ROS)持续增加,我们推测ROS可能是应变诱导Et-1基因表达的调节因子。经受循环应变的人脐静脉内皮细胞(HUVECs)的Et-1分泌增加。用抗氧化剂过氧化氢酶(300 U/ml)或1,3 - 二甲基 -2 - 硫脲(DMTU,0.1 mM)预处理HUVECs,可消除应变诱导的Et-1释放。应变6小时的内皮细胞Et-1 mRNA水平升高。相反,用过氧化氢酶或DMTU处理的内皮细胞,其由循环应变刺激的Et-1 mRNA水平并未增加。用含有Et-1 5'侧翼序列(4.4 kb)和氯霉素乙酰转移酶报告基因的融合质粒转染的牛主动脉内皮细胞(BAECs),在经受应变6小时后产生最大的Et-1启动子活性,而用过氧化氢酶预处理可降低该活性。与Ras(RasN17)、Raf-1(Raf301)的显性负突变体或细胞外信号调节激酶的催化失活突变体(mERK2)共转染的BAECs,其应变诱导的Et-1启动子活性受到抑制,表明Ras/Raf/ERK途径参与其中;此外,在经受应变的内皮细胞中诱导了ERK磷酸化。在过氧化氢酶存在的情况下,这种应变激活的ERK磷酸化减弱。用定点诱变对Et-1启动子进行功能分析表明,激活蛋白-1(AP-1)结合位点必须位于转录起始位点上游143个碱基对内,才能产生应变诱导的启动子活性。用过氧化氢酶预处理内皮细胞也降低了最小构建体(-143 bp)中应变诱导的启动子活性。我们的数据表明,应变诱导的Et-1基因表达受ROS通过Ras/Raf/ERK信号通路调节,并表明AP-1结合位点对应变诱导的Et-1表达具有反应性。