The anticonvulsive Phenhydan® suppresses extrinsic cell death

Cell Death Differ. 2019 Sep;26(9):1631-1645. doi: 10.1038/s41418-018-0232-2. Epub 2018 Nov 15.

Abstract

Different forms of regulated cell death-like apoptosis and necroptosis contribute to the pathophysiology of clinical conditions including ischemia-reperfusion injury, myocardial infarction, sepsis, and multiple sclerosis. In particular, the kinase activity of the receptor-interacting serine/threonine protein kinase 1 (RIPK1) is crucial for cell fate in inflammation and cell death. However, despite its involvement in pathological conditions, no pharmacologic inhibitor of RIPK1-mediated cell death is currently in clinical use. Herein, we screened a collection of clinical compounds to assess their ability to modulate RIPK1-mediated cell death. Our small-scale screen identified the anti-epilepsy drug Phenhydan® as a potent inhibitor of death receptor-induced necroptosis and apoptosis. Accordingly, Phenhydan® blocked activation of necrosome formation/activation as well as death receptor-induced NF-κB signaling by influencing the membrane function of cells, such as lipid raft formation, thus exerting an inhibitory effect on pathophysiologic cell death processes. By targeting death receptor signaling, the already FDA-approved Phenhydan® may provide new therapeutic strategies for inflammation-driven diseases caused by aberrant cell death.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology
  • Apoptosis / drug effects*
  • Apoptosis / genetics
  • Cell Death / drug effects
  • Cell Death / genetics
  • HT29 Cells
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / genetics
  • Inflammation / pathology
  • Mice
  • Multiple Sclerosis / drug therapy
  • Multiple Sclerosis / genetics
  • Myocardial Infarction / drug therapy
  • Myocardial Infarction / genetics
  • NIH 3T3 Cells
  • Necroptosis / drug effects*
  • Necroptosis / genetics
  • Phenytoin / pharmacology*
  • Phenytoin / therapeutic use
  • Receptor-Interacting Protein Serine-Threonine Kinases / genetics
  • Receptors, Death Domain / antagonists & inhibitors
  • Receptors, Death Domain / genetics
  • Reperfusion Injury / drug therapy
  • Reperfusion Injury / genetics
  • Sepsis / drug therapy
  • Sepsis / genetics

Substances

  • Anticonvulsants
  • Receptors, Death Domain
  • Phenytoin
  • RIPK1 protein, human
  • Receptor-Interacting Protein Serine-Threonine Kinases