Carbenoxolone prevents chemical eye ischemia-reperfusion-induced cell death via 11β-hydroxysteroid dehydrogenase type 1 inhibition

Pharmacol Res. 2017 Sep:123:62-72. doi: 10.1016/j.phrs.2017.07.002. Epub 2017 Jul 4.

Abstract

Glaucoma is one of the leading causes of preventable blindness diseases, affecting more than 2 million people in the United States. Recently, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors were found to exert preventive effects against glaucoma. Therefore, we investigated whether carbenoxolone (CBX), an 11β-HSD1 inhibitor, prevents chemical ischemia-reperfusion-induced cell death in human trabecular meshwork (HTM) cells. The present study demonstrated that CBX inhibited cell death caused by iodoacetic acid (IAA)-induced ischemia-reperfusion, and its effect was associated with the inhibition of 11β-HSD1 expression and activity. Furthermore, CBX reversed the IAA-induced structural damage on filamentous actin in HTM cells. In IAA-treated cells, the levels of 11β-HSD1 and the apoptosis-related factors Bax and FASL were increased throughout the reperfusion period, and CBX was able to attenuate the expression of 11β-HSD1 and the apoptosis-related factors. CBX also effectively suppressed IAA-induced intracellular ROS formation and cytochrome c release, which are involved in the mitochondrial apoptosis pathway. In addition, IAA-induced chemical ischemia-reperfusion stimulated TNF-α expression and NF-κB p65 phosphorylation, and these effects were attenuated by CBX. 11β-HSD1 RNAi also suppressed IAA-induced cell apoptosis via reduction of oxidative stress and inhibition of the pro-inflammatory pathway. Taken together, the present study demonstrated that the inhibition of 11β-HSD1 protected the TM against chemical ischemia-reperfusion injury, suggesting that the use of 11β-HSD1 inhibitors could be a useful strategy for glaucoma therapy.

Keywords: 11β-Hydroxysteroid dehydrogenase type 1; Apoptosis; Carbenoxolone; Carbenoxolone (PubChem CID: 636403); Glaucoma; Inflammation; Iodoacetic acid (PubChem CID: 5240).

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / metabolism
  • Carbenoxolone / pharmacology*
  • Cell Death / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cytochromes c / metabolism
  • Eye Injuries / chemically induced
  • Eye Injuries / metabolism
  • Eye Injuries / prevention & control*
  • Humans
  • Iodoacetic Acid
  • Protective Agents / pharmacology*
  • Reactive Oxygen Species / metabolism
  • Reperfusion Injury / chemically induced
  • Reperfusion Injury / metabolism
  • Reperfusion Injury / prevention & control*
  • Trabecular Meshwork / cytology
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Protective Agents
  • Reactive Oxygen Species
  • Tumor Necrosis Factor-alpha
  • Cytochromes c
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1
  • Carbenoxolone
  • Iodoacetic Acid