Department of Neurology and Neurological Sciences, Stanford University School of Medicine, Stanford, CA 94305, USA.
Neurosci Lett. 2011 Oct 31;504(3):185-90. doi: 10.1016/j.neulet.2011.09.005. Epub 2011 Sep 12.
Neonatal hypoxic-ischemic encephalopathy (HIE) is a leading cause of severe and permanent neurologic disability after birth. The inducible cyclooxygenase COX-2, which along with COX-1 catalyzes the first committed step in prostaglandin (PG) synthesis, elicits significant brain injury in models of cerebral ischemia; however its downstream PG receptor pathways trigger both toxic and paradoxically protective effects. Here, we investigated the function of PGE(2) E-prostanoid (EP) receptors in the acute outcome of hypoxic-ischemic (HI) injury in the neonatal rat. We determined the temporal and cellular expression patterns of the EP1-4 receptors before and after HIE and tested whether modulation of EP1-4 receptor function could protect against cerebral injury acutely after HIE. All four EP receptors were expressed in forebrain neurons and were induced in endothelial cells after HIE. Inhibition of EP1 signaling with the selective antagonist SC-51089 or co-activation of EP2-4 receptors with the agonist misoprostol significantly reduced HIE cerebral injury 24 h after injury. These receptor ligands also protected brain endothelial cells subjected to oxygen glucose deprivation, suggesting that activation of EP receptor signaling is directly cytoprotective. These data indicate that the G-protein coupled EP receptors may be amenable to pharmacologic targeting in the acute setting of neonatal HIE.
新生儿缺氧缺血性脑病(HIE)是出生后严重和永久性神经功能障碍的主要原因。诱导型环加氧酶 COX-2 与 COX-1 一起催化前列腺素(PG)合成的第一步,在脑缺血模型中引起明显的脑损伤;然而,其下游 PG 受体途径引发毒性和矛盾的保护作用。在这里,我们研究了 PGE(2)E-前列腺素(EP)受体在新生大鼠缺氧缺血(HI)损伤急性期的功能。我们在 HIE 前后确定了 EP1-4 受体的时间和细胞表达模式,并测试了 EP1-4 受体功能的调节是否可以在 HIE 后急性保护脑损伤。所有四个 EP 受体都在前脑神经元中表达,并在 HIE 后在内皮细胞中诱导。用选择性拮抗剂 SC-51089 抑制 EP1 信号或用激动剂米索前列醇共同激活 EP2-4 受体可显著减少 HIE 后 24 小时的脑损伤。这些受体配体还可保护氧葡萄糖剥夺的脑内皮细胞,表明 EP 受体信号的激活具有直接的细胞保护作用。这些数据表明,G 蛋白偶联的 EP 受体可能适合于新生儿 HIE 的急性治疗。