Neonatal Research Laboratory, Department of Pediatrics, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287, USA.
J Cereb Blood Flow Metab. 2011 Jan;31(1):178-89. doi: 10.1038/jcbfm.2010.72. Epub 2010 Jun 23.
Necrostatin-1 inhibits receptor-interacting protein (RIP)-1 kinase and programmed necrosis and is neuroprotective in adult rodent models. Owing to the prominence of necrosis and continuum cell death in neonatal hypoxia-ischemia (HI), we tested whether necrostatin was neuroprotective in the developing brain. Postnatal day (P)7 mice were exposed to HI and injected intracerebroventricularly with 0.1 μL of 80 μmol necrostatin, Nec-1, 5-(1H-Indol-3-ylmethyl)-(2-thio-3-methyl) hydantoin, or vehicle. Necrostatin significantly decreased injury in the forebrain and thalamus at P11 and P28. There was specific neuroprotection in necrostatin-treated males. Necrostatin treatment decreased necrotic cell death and increased apoptotic cell death. Hypoxia-ischemia enforced RIP1-RIP3 complex formation and inhibited RIP3-FADD (Fas-associated protein with death domain) interaction, and these effects were blocked by necrostatin. Necrostatin also decreased HI-induced oxidative damage to proteins and attenuated markers of inflammation coincidental with decreased nuclear factor-κB and caspase 1 activation, and FLIP ((Fas-associated death-domain-like IL-1β-converting enzyme)-inhibitory protein) gene and protein expression. In this model of severe neonatal brain injury, we find that cellular necrosis can be managed therapeutically by a single dose of necrostatin, administered after HI, possibly by interrupting RIP1-RIP3-driven oxidative injury and inflammation. The effects of necrostatin treatment after HI reflect the importance of necrosis in the delayed phases of neonatal brain injury and represent a new direction for therapy of neonatal HI.
Necrostatin-1 抑制受体相互作用蛋白 (RIP)-1 激酶和程序性细胞坏死,并在成年啮齿动物模型中具有神经保护作用。由于坏死和连续细胞死亡在新生儿缺氧缺血(HI)中较为突出,我们测试了 necrostatin 是否对发育中的大脑具有神经保护作用。出生后第 7 天(P)的小鼠暴露于 HI 中,并通过脑室内注射 0.1μL 的 80μmol necrostatin、Nec-1、5-(1H-吲哚-3-基甲基)-(2-硫代-3-甲基)海因或载体。Necrostatin 显著降低了 P11 和 P28 时前脑和丘脑的损伤。在接受 necrostatin 治疗的雄性小鼠中,存在特异性的神经保护作用。Necrostatin 治疗可减少坏死性细胞死亡并增加凋亡性细胞死亡。缺氧缺血导致 RIP1-RIP3 复合物形成,并抑制 RIP3-FADD(Fas 相关死亡结构域蛋白)相互作用,而这些作用被 necrostatin 阻断。Necrostatin 还降低了 HI 引起的蛋白质氧化损伤,并减轻了与核因子-κB 和 caspase 1 激活减少以及 FLIP(Fas 相关死亡结构域样 IL-1β 转化酶)抑制蛋白)基因和蛋白表达相关的炎症标志物。在这种严重的新生儿脑损伤模型中,我们发现,通过 HI 后单次给予 necrostatin 可以治疗细胞坏死,这可能是通过阻断 RIP1-RIP3 驱动的氧化损伤和炎症。HI 后 necrostatin 治疗的效果反映了坏死在新生儿脑损伤的延迟阶段的重要性,并为新生儿 HI 的治疗提供了新的方向。