Zhuang Shougang, Kinsey Gilbert R, Yan Yan, Han Jiahuai, Schnellmann Rick G
Department of Medicine Rhode Island Hospital, Middle House 301, 593 Eddy Street, Providence, RI 02903, USA.
J Pharmacol Exp Ther. 2008 Jun;325(3):732-40. doi: 10.1124/jpet.108.136358. Epub 2008 Mar 13.
Although tubular necrosis in acute renal failure is associated with excessive production of reactive oxygen species (ROS), such as hydrogen peroxide (H2O2), the mechanism of ROS-induced cell necrosis remains poorly understood. In this study, we examined the role of the extracellular signaling-regulated kinase (ERK) pathway in H2O2-induced necrosis of renal proximal tubular cells (RPTC) in primary culture. Exposure of 60 to 70% confluent RPTC to 1 mM H2O2 for 3 h resulted in 44% necrotic cell death, as measured by trypan blue uptake, and inactivation of mitogen-activated protein kinase kinase (MEK), the upstream activator of ERK, by either 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene (U0126) or 2-(2'-amino-3'-methoxyphenyl)-oxanaphthalen-4-one (PD98059) or overexpression of dominant-negative mutant of MEK1, inhibited cell death. In contrast, overexpression of active MEK1 enhanced H2O2-induced cell death. H2O2 treatment led to the loss of mitochondrial membrane potential (MMP) in RPTC, which was decreased by U0126 and PD98059. Furthermore, inhibition of the MEK/ERK pathway decreased oxidant-mediated ERK1/2 activation and mitochondrial swelling in isolated renal cortex mitochondria. However, treatment with cyclosporin A (CsA), a mitochondrial permeability transition blocker, did not suppress RPTC necrotic cell death, loss of MMP, and mitochondrial swelling. We suggest that ERK is a critical mediator of mitochondrial dysfunction and necrotic cell death of renal epithelial cells following oxidant injury. Oxidant-induced necrotic cell death was mediated by a CsA-insensitive loss of MMP that is regulated by the ERK pathway.
尽管急性肾衰竭中的肾小管坏死与活性氧(ROS)如过氧化氢(H2O2)的过量产生有关,但ROS诱导细胞坏死的机制仍知之甚少。在本研究中,我们检测了细胞外信号调节激酶(ERK)通路在原代培养的肾近端小管细胞(RPTC)中H2O2诱导的坏死中的作用。用锥虫蓝摄取法测定,将60%至70%汇合的RPTC暴露于1 mM H2O2 3小时,导致44%的坏死性细胞死亡,而通过1,4 - 二氨基 - 2,3 - 二氰基 - 1,4 - 双[2 - 氨基苯硫基]丁二烯(U0126)或2 - (2'-氨基 - 3'-甲氧基苯基) - 氧杂萘 - 4 - 酮(PD98059)或MEK1显性负性突变体的过表达来使ERK的上游激活剂丝裂原活化蛋白激酶激酶(MEK)失活,可抑制细胞死亡。相反,活性MEK1的过表达增强了H2O2诱导的细胞死亡。H2O2处理导致RPTC中线粒体膜电位(MMP)丧失,而U0126和PD98059可使其降低。此外,MEK/ERK通路的抑制减少了分离的肾皮质线粒体中氧化剂介导的ERK1/2激活和线粒体肿胀。然而,用线粒体通透性转换阻滞剂环孢素A(CsA)处理并不能抑制RPTC坏死性细胞死亡、MMP丧失和线粒体肿胀。我们认为ERK是氧化损伤后肾上皮细胞线粒体功能障碍和坏死性细胞死亡的关键介质。氧化剂诱导的坏死性细胞死亡是由ERK通路调节的、CsA不敏感的MMP丧失介导的。