The membrane-active tri-block copolymer pluronic F-68 profoundly rescues rat hippocampal neurons from oxygen-glucose deprivation-induced death through early inhibition of apoptosis

J Neurosci. 2013 Jul 24;33(30):12287-99. doi: 10.1523/JNEUROSCI.5731-12.2013.

Abstract

Pluronic F-68, an 80% hydrophilic member of the Pluronic family of polyethylene-polypropylene-polyethylene tri-block copolymers, protects non-neuronal cells from traumatic injuries and rescues hippocampal neurons from excitotoxic and oxidative insults. F-68 interacts directly with lipid membranes and restores membrane function after direct membrane damage. Here, we demonstrate the efficacy of Pluronic F-68 in rescuing rat hippocampal neurons from apoptosis after oxygen-glucose deprivation (OGD). OGD progressively decreased neuronal survival over 48 h in a severity-dependent manner, the majority of cell death occurring after 12 h after OGD. Administration of F-68 for 48 h after OGD rescued neurons from death in a dose-dependent manner. At its optimal concentration (30 μm), F-68 rescued all neurons that would have died after the first hour after OGD. This level of rescue persisted when F-68 administration was delayed 12 h after OGD. F-68 did not alter electrophysiological parameters controlling excitability, NMDA receptor-activated currents, or NMDA-induced increases in cytosolic calcium concentrations. However, F-68 treatment prevented phosphatidylserine externalization, caspase activation, loss of mitochondrial membrane potential, and BAX translocation to mitochondria, indicating that F-68 alters apoptotic mechanisms early in the intrinsic pathway of apoptosis. The profound neuronal rescue provided by F-68 after OGD and the high level of efficacy with delayed administration indicate that Pluronic copolymers may provide a novel, membrane-targeted approach to rescuing neurons after brain ischemia. The ability of membrane-active agents to block apoptosis suggests that membranes or their lipid components play prominent roles in injury-induced apoptosis.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Animals
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Caspase 1 / metabolism
  • Caspase Inhibitors / pharmacology
  • Cell Hypoxia / drug effects
  • Cell Hypoxia / physiology
  • Cytochromes c / metabolism
  • Enzyme Activation / drug effects
  • Enzyme Activation / physiology
  • Female
  • Fetus / cytology
  • Glucose / metabolism
  • Glucose / pharmacology
  • Hippocampus / cytology*
  • Male
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Mitochondria / metabolism
  • Neurons / cytology*
  • Neurons / drug effects*
  • Neurons / physiology
  • Oxygen / metabolism
  • Oxygen / pharmacology
  • Patch-Clamp Techniques
  • Polyethylene Glycols / pharmacology*
  • Pregnancy
  • Primary Cell Culture
  • Propylene Glycols / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • bcl-2-Associated X Protein / metabolism

Substances

  • Amino Acid Chloromethyl Ketones
  • Caspase Inhibitors
  • PEO-PPO-PEO
  • Propylene Glycols
  • bcl-2-Associated X Protein
  • benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone
  • Polyethylene Glycols
  • Cytochromes c
  • Caspase 1
  • Glucose
  • Oxygen