Carnosol as a Nrf2 Activator Improves Endothelial Barrier Function Through Antioxidative Mechanisms

Int J Mol Sci. 2019 Feb 18;20(4):880. doi: 10.3390/ijms20040880.

Abstract

Oxidative stress is the main pathogenesis of diabetic microangiopathy, which can cause microvascular endothelial cell damage and destroy vascular barrier. In this study, it is found that carnosol protects human microvascular endothelial cells (HMVEC) through antioxidative mechanisms. First, we measured the antioxidant activity of carnosol. We showed that carnosol pretreatment suppressed tert-butyl hydroperoxide (t-BHP)-induced cell viability, affected the production of lactate dehydrogenase (LDH) as well as reactive oxygen species (ROS), and increased the produce of nitric oxide (NO). Additionally, carnosol promotes the protein expression of vascular endothelial cadherin (VE-cadherin) to keep the integrity of intercellular junctions, which indicated that it protected microvascular barrier in oxidative stress. Meanwhile, we investigated that carnosol can interrupt Nrf2-Keap1 protein-protein interaction and stimulated antioxidant-responsive element (ARE)-driven luciferase activity in vitro. Mechanistically, we showed that carnosol promotes the expression of heme oxygenase 1(HO-1) and nuclear factor-erythroid 2 related factor 2(Nrf2). It can also promote the expression of endothelial nitric oxide synthase (eNOS). Collectively, our data support the notion that carnosol is a protective agent in HMVECs and has the potential for therapeutic use in the treatments of microvascular endothelial cell injury.

Keywords: HMVEC cells; antioxidant activity; carnosol; microvascular endothelial protection.

MeSH terms

  • Abietanes / chemistry
  • Abietanes / pharmacology*
  • Antigens, CD / metabolism
  • Antioxidants / pharmacology*
  • Benzothiazoles / metabolism
  • Cadherins / metabolism
  • Cell Line
  • Cytoprotection / drug effects
  • Cytoprotection / genetics
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism*
  • Free Radical Scavengers / metabolism
  • Humans
  • Microvessels / pathology
  • Molecular Docking Simulation
  • NF-E2-Related Factor 2 / metabolism*
  • Nitric Oxide / metabolism
  • Reactive Oxygen Species / metabolism
  • Sulfonic Acids / metabolism
  • tert-Butylhydroperoxide

Substances

  • Abietanes
  • Antigens, CD
  • Antioxidants
  • Benzothiazoles
  • Cadherins
  • Free Radical Scavengers
  • NF-E2-Related Factor 2
  • Reactive Oxygen Species
  • Sulfonic Acids
  • cadherin 5
  • 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid
  • Nitric Oxide
  • carnosol
  • tert-Butylhydroperoxide