The SIRT1 inhibitor EX-527 suppresses mTOR activation and alleviates acute lung injury in mice with endotoxiemia

Innate Immun. 2017 Nov;23(8):678-686. doi: 10.1177/1753425917733531. Epub 2017 Sep 27.

Abstract

It is generally regarded that Sirtuin 1 (SIRT1), a longevity factor in mammals, acts as a negative regulator of inflammation. However, recent studies also found that SIRT1 might be a detrimental factor under certain inflammatory circumstance. In this study, the potential pathophysiological roles and the underlying mechanisms of SIRT1 in a mouse model with endotoxemia-associated acute lung injury were investigated. The results indicated that treatment with the selective SIRT1 inhibitor EX-527 suppressed LPS-induced elevation of TNF-α and IL-6 in plasma. Treatment with EX-527 attenuated LPS-induced histological abnormalities in lung tissue, which was accompanied with decreased myeloperoxidase level and suppressed induction of tissue factor and plasminogen activator inhibitor-1. Treatment with EX-527 also suppressed LPS-induced phosphorylation of eukaryotic translation initiation factor-binding protein 1 (4E-BP1). Co-administration of a mammalian target of rapamycin (mTOR) activator 3-benzyl-5-[(2-nitrophenoxy) methyl]-dihydrofuran-2 (3H)-one (3BDO) abolished the inhibitory effects of EX-527 on 4E-BP1 phosphorylation. Meanwhile, the inhibitory effects of EX-527 on IL-6 induction and the beneficial effects of EX-527 on lung injury were partially reversed by 3BDO. This study suggests that selective inhibition of SIRT1 by EX-527 might alleviate endotoxemia-associated acute lung injury partially via suppression of mTOR, which implies that SIRT1 selective inhibitors might have potential value for the pharmacological intervention of inflammatory lung injury.

Keywords: Sirtuin 1; acute lung injury; inflammation; lipopolysaccharide; mTOR.

MeSH terms

  • 4-Butyrolactone / analogs & derivatives
  • 4-Butyrolactone / pharmacology
  • Acute Lung Injury / drug therapy*
  • Adaptor Proteins, Signal Transducing
  • Animals
  • Carbazoles / pharmacology*
  • Carrier Proteins / metabolism
  • Cell Cycle Proteins
  • Endotoxemia / drug therapy*
  • Eukaryotic Initiation Factors
  • Interleukin-6 / metabolism
  • Lipopolysaccharides / immunology
  • Lung / drug effects*
  • Lung / pathology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Phosphoproteins / metabolism
  • Phosphorylation
  • Plasminogen Activator Inhibitor 1 / metabolism
  • Sirtuin 1 / antagonists & inhibitors*
  • TOR Serine-Threonine Kinases / antagonists & inhibitors
  • Thromboplastin / genetics
  • Thromboplastin / metabolism
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • 3-benzyl-5-((2-nitrophenoxy)methyl)dihydrofuran-2(3H)-one
  • 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
  • Adaptor Proteins, Signal Transducing
  • Carbazoles
  • Carrier Proteins
  • Cell Cycle Proteins
  • Eif4ebp1 protein, mouse
  • Eukaryotic Initiation Factors
  • Interleukin-6
  • Lipopolysaccharides
  • Phosphoproteins
  • Plasminogen Activator Inhibitor 1
  • Tumor Necrosis Factor-alpha
  • Thromboplastin
  • TOR Serine-Threonine Kinases
  • Sirtuin 1
  • 4-Butyrolactone