K6PC-5 Activates SphK1-Nrf2 Signaling to Protect Neuronal Cells from Oxygen Glucose Deprivation/Re-Oxygenation

Cell Physiol Biochem. 2018;51(4):1908-1920. doi: 10.1159/000495716. Epub 2018 Nov 30.

Abstract

Background/aims: New strategies are required to combat neuronal ischemia-reperfusion injuries. K6PC-5 is a novel sphingosine kinase 1 (SphK1) activator whose potential activity in neuronal cells has not yet been tested.

Methods: Cell survival and necrosis were assessed with a Cell Counting Kit-8 assay and lactate dehydrogenase release assay, respectively. Mitochondrial depolarization was tested by a JC-1 dye assay. Expression levels of nuclear factor erythroid 2-related factor 2 (Nrf2) signaling components were examined by quantitative real-timePCR and western blotting.

Results: K6PC-5 protected SH-SY5Y neuronal cells and primary murine hippocampal neurons from oxygen glucose deprivation/re-oxygenation (OGDR). K6PC-5 activated SphK1, and SphK1 knockdown by targeted short hairpin RNA (shRNA) almost completely abolished K6PC-5-induced neuronal cell protection. Further work showed that K6PC-5 inhibited OGDR-induced programmed necrosis in neuronal cells. Importantly, K6PC-5 activated Nrf2 signaling, which is downstream of SphK1. Silencing of Nrf2 by targeted shRNA almost completely nullified K6PC-5-mediated neuronal cell protection against OGDR.

Conclusion: K6PC-5 activates SphK1-Nrf2 signaling to protect neuronal cells from OGDR. K6PC-5 might be a promising neuroprotective strategy for ischemia-reperfusion injuries.

Keywords: K6PC-5; Neuron; Nrf2; Oxidative stress; SphK1.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cell Line
  • Cell Survival / drug effects
  • Cells, Cultured
  • Enzyme Activators / pharmacology*
  • Glucose / metabolism
  • Humans
  • Mice
  • NF-E2-Related Factor 2 / metabolism*
  • Neurons / cytology
  • Neurons / drug effects*
  • Neurons / metabolism
  • Neuroprotective Agents / pharmacology*
  • Oxidative Stress / drug effects
  • Oxygen / metabolism
  • Phosphotransferases (Alcohol Group Acceptor) / metabolism*
  • Reperfusion Injury / drug therapy
  • Reperfusion Injury / metabolism
  • Signal Transduction / drug effects*

Substances

  • Enzyme Activators
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • Neuroprotective Agents
  • Phosphotransferases (Alcohol Group Acceptor)
  • sphingosine kinase
  • Glucose
  • Oxygen