Andrographolide inhibits PI3K/AKT-dependent NOX2 and iNOS expression protecting mice against hypoxia/ischemia-induced oxidative brain injury

Planta Med. 2011 Oct;77(15):1669-79. doi: 10.1055/s-0030-1271019. Epub 2011 Apr 21.

Abstract

This study aimed to explore the mechanisms by which andrographolide protects against hypoxia-induced oxidative/nitrosative brain injury provoked by cerebral ischemic/reperfusion (CI/R) injury in mice. Hypoxia IN VITRO was modeled using oxygen-glucose deprivation (OGD) followed by reoxygenation of BV-2 microglial cells. Our results showed that treatment of mice that have undergone CI/R injury with andrographolide (10-100 µg/kg, i. v.) at 1 h after hypoxia ameliorated CI/R-induced oxidative/nitrosative stress, brain infarction, and neurological deficits in the mice, and enhanced their survival rate. CI/R induced a remarkable production in the mouse brains of reactive oxygen species (ROS) and a significant increase in protein nitrosylation; this primarily resulted from enhanced expression of NADPH oxidase 2 (NOX2), inducible nitric oxide synthase (iNOS), and the infiltration of CD11b cells due to activation of nuclear factor-kappa B (NF- κB) and hypoxia-inducible factor 1-alpha (HIF-1 α). All these changes were significantly diminished by andrographolide. In BV-2 cells, OGD induced ROS and nitric oxide production by upregulating NOX2 and iNOS via the phosphatidylinositol-3-kinase (PI3K)/AKT-dependent NF- κB and HIF-1 α pathways, and these changes were suppressed by andrographolide and LY294002. Our results indicate that andrographolide reduces NOX2 and iNOS expression possibly by impairing PI3K/AKT-dependent NF- κB and HIF-1 α activation. This compromises microglial activation, which then, in turn, mediates andrographolide's protective effect in the CI/R mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Cell Line
  • Cerebral Infarction / complications
  • Cerebral Infarction / prevention & control
  • Disease Models, Animal
  • Diterpenes / pharmacology
  • Diterpenes / therapeutic use*
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Hypoxia-Ischemia, Brain / complications
  • Hypoxia-Ischemia, Brain / prevention & control*
  • Male
  • Mice
  • Mice, Inbred ICR
  • Microglia / metabolism
  • NADPH Oxidases / antagonists & inhibitors*
  • NADPH Oxidases / metabolism
  • NF-kappa B / metabolism
  • Nitric Oxide Synthase Type II / antagonists & inhibitors*
  • Nitric Oxide Synthase Type II / metabolism
  • Nitrosation / drug effects
  • Phosphatidylinositol 3-Kinase / metabolism
  • Reactive Oxygen Species / metabolism
  • Stroke / complications
  • Stroke / prevention & control*
  • Superoxides / metabolism
  • Tyrosine / analogs & derivatives
  • Tyrosine / metabolism
  • Up-Regulation

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Diterpenes
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • NF-kappa B
  • Reactive Oxygen Species
  • Superoxides
  • 3-nitrotyrosine
  • andrographolide
  • Tyrosine
  • Nitric Oxide Synthase Type II
  • NADPH Oxidases
  • Phosphatidylinositol 3-Kinase