Zhuo Ming, Gorgun Murat F, Englander Ella W
Department of Surgery, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555, USA.
Department of Surgery, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555, USA.
Free Radic Biol Med. 2016 Oct;99:20-31. doi: 10.1016/j.freeradbiomed.2016.07.022. Epub 2016 Jul 22.
To meet energy demands, dorsal root ganglion (DRG) neurons harbor high mitochondrial content, which renders them acutely vulnerable to disruptions of energy homeostasis. While neurons typically rely on mitochondrial energy production and have not been associated with metabolic plasticity, new studies reveal that meclizine, a drug, recently linked to modulations of energy metabolism, protects neurons from insults that disrupt energy homeostasis. We show that meclizine rapidly enhances glycolysis in DRG neurons and that glycolytic metabolism is indispensable for meclizine-exerted protection of DRG neurons from hypoxic stress. We report that supplementation of meclizine during hypoxic exposure prevents ATP depletion, preserves NADPH and glutathione stores, curbs reactive oxygen species (ROS) and attenuates mitochondrial clustering in DRG neurites. Using extracellular flux analyzer, we show that in cultured DRG neurons meclizine mitigates hypoxia-induced loss of mitochondrial respiratory capacity. Respiratory capacity is a measure of mitochondrial fitness and cell ability to meet fluctuating energy demands and therefore, a key determinant of cellular fate. While meclizine is an 'old' drug with long record of clinical use, its ability to modulate energy metabolism has been uncovered only recently. Our findings documenting neuroprotection by meclizine in a setting of hypoxic stress reveal previously unappreciated metabolic plasticity of DRG neurons as well as potential for pharmacological harnessing of the newly discovered metabolic plasticity for protection of peripheral nervous system under mitochondria compromising conditions.
为了满足能量需求,背根神经节(DRG)神经元含有大量线粒体,这使得它们极易受到能量稳态破坏的影响。虽然神经元通常依赖线粒体产生能量,且与代谢可塑性无关,但新研究表明,美克洛嗪这种最近与能量代谢调节相关的药物,能保护神经元免受破坏能量稳态的损伤。我们发现美克洛嗪能迅速增强DRG神经元中的糖酵解,且糖酵解代谢对于美克洛嗪发挥保护DRG神经元免受缺氧应激的作用不可或缺。我们报告称,在缺氧暴露期间补充美克洛嗪可防止ATP耗竭,维持NADPH和谷胱甘肽储备,抑制活性氧(ROS)并减轻DRG神经突中的线粒体聚集。使用细胞外通量分析仪,我们表明在培养的DRG神经元中,美克洛嗪可减轻缺氧诱导的线粒体呼吸能力丧失。呼吸能力是线粒体健康状况和细胞满足波动能量需求能力的指标,因此是细胞命运的关键决定因素。虽然美克洛嗪是一种有长期临床使用记录的“老”药,但其调节能量代谢的能力直到最近才被发现。我们关于美克洛嗪在缺氧应激情况下具有神经保护作用的研究结果,揭示了DRG神经元此前未被认识到的代谢可塑性,以及在线粒体受损条件下利用新发现的代谢可塑性进行药理学保护外周神经系统的潜力。