Pond Brooks B, Galeffi Francesca, Ahrens Rebecca, Schwartz-Bloom Rochelle D
Department of Pharmacology and Cancer Biology, Duke University Medical Center, Box 3813, Durham, NC 27710, USA.
Neuropharmacology. 2004 Aug;47(2):253-62. doi: 10.1016/j.neuropharm.2004.04.002.
Cerebral ischemia in vivo or oxygen-glucose deprivation (OGD) in vitro are characterized by major disturbances in neuronal ionic homeostasis, including significant rises in intracellular Na(+), Ca(2+), and Cl(-) and extracellular K(+). Recently, considerable attention has been focused on the cation-chloride cotransporters Na-K-Cl cotransporter isoform I (NKCC-1) and K-Cl cotransporter isoform II (KCC2), as they may play an important role in the disruption of ion gradients and subsequent ischemic damage. In this study, we examined the ability of cation-chloride transport inhibitors to influence the biochemical (i.e. ATP) and histological recovery of neurons in adult hippocampal slices exposed to OGD. In the hippocampus, 7 min of OGD caused a loss of ATP that recovered partially (approximately 50%) during 3 h of reoxygenation. Furosemide, which inhibits the NKCC-1 and KCC2 cotransporters, and bumetanide, a more specific NKCC-1 inhibitor, enhanced ATP recovery when measured 3 h after OGD. Furosemide and bumetanide also attenuated area CA1 neuronal injury after OGD. However, higher concentrations of these compounds appear to have additional non-specific toxic effects, limiting ATP recovery following OGD and promoting neuronal injury. The KCC2 cotransporter inhibitor DIOA and the Cl(-) ATPase inhibitor ethacrynic acid caused neuronal death even in the absence of OGD and promoted cytochrome c release from isolated mitochondria, indicating non-specific toxicities of these compounds.
体内脑缺血或体外氧糖剥夺(OGD)的特征是神经元离子稳态出现重大紊乱,包括细胞内Na⁺、Ca²⁺和Cl⁻以及细胞外K⁺显著升高。最近,阳离子 - 氯离子共转运体钠 - 钾 - 氯共转运体同工型I(NKCC - 1)和钾 - 氯共转运体同工型II(KCC2)受到了相当多的关注,因为它们可能在离子梯度破坏及随后的缺血性损伤中起重要作用。在本研究中,我们检测了阳离子 - 氯离子转运抑制剂对暴露于OGD的成年海马切片中神经元的生化(即ATP)和组织学恢复的影响。在海马体中,7分钟的OGD导致ATP丢失,在复氧3小时期间部分恢复(约50%)。抑制NKCC - 1和KCC2共转运体的呋塞米以及更具特异性的NKCC - 1抑制剂布美他尼,在OGD后3小时测量时增强了ATP的恢复。呋塞米和布美他尼也减轻了OGD后CA1区神经元损伤。然而,这些化合物的较高浓度似乎具有额外的非特异性毒性作用,限制了OGD后的ATP恢复并促进了神经元损伤。KCC2共转运体抑制剂DIOA和Cl⁻ATP酶抑制剂依他尼酸即使在没有OGD的情况下也会导致神经元死亡,并促进细胞色素c从分离的线粒体中释放,表明这些化合物具有非特异性毒性。