Apigenin protects blood-brain barrier and ameliorates early brain injury by inhibiting TLR4-mediated inflammatory pathway in subarachnoid hemorrhage rats

Int Immunopharmacol. 2015 Sep;28(1):79-87. doi: 10.1016/j.intimp.2015.05.024. Epub 2015 May 28.

Abstract

Early brain injury (EBI) following subarachnoid hemorrhage (SAH) is associated with high morbidity and mortality. Inflammation has been considered as the major contributor to brain damage after SAH. SAH induces a systemic increase in pro-inflammatory cytokines and chemokines. Disruption of blood-brain barrier (BBB) facilitates the influx of inflammatory cells. It has been reported that the activation of toll-like receptor 4 (TLR4)/NF-κB signaling pathway plays a vital role in the central nervous system diseases. Apigenin, a common plant flavonoid, possesses anti-inflammation effect. In this study, we focused on the effects of apigenin on EBI following SAH and its anti-inflammation mechanism. Our results showed that apigenin (20mg/kg) administration significantly attenuated EBI (including brain edema, BBB disruption, neurological deficient, severity of SAH, and cell apoptosis) after SAH in rats by suppressing the expression of TLR4, NF-κB and their downstream pro-inflammatory cytokines in the cortex and by up-regulating the expression of tight junction proteins of BBB. Double immunofluorescence staining demonstrated that TLR4 was activated following SAH in neurons, microglia cells, and endothelial cells but not in astrocytes. Apigenin could suppress the activation of TLR4 induced by SAH and inhibit apoptosis of cells in the cortex. These results suggested that apigenin could attenuate EBI after SAH in rats by suppressing TLR4-mediated inflammation and protecting against BBB disruption.

Keywords: Apigenin; Early brain injury; Inflammation; Neuroprotective effect; Subarachnoid hemorrhage; Tight junction proteins.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Apigenin / pharmacology*
  • Apoptosis / drug effects
  • Blood-Brain Barrier / drug effects*
  • Brain Injury, Chronic / drug therapy*
  • Brain Injury, Chronic / pathology
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Cytokines / metabolism
  • Disease Progression
  • Male
  • NF-kappa B / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction / drug effects*
  • Subarachnoid Hemorrhage / drug therapy*
  • Subarachnoid Hemorrhage / pathology
  • Tight Junction Proteins / metabolism
  • Toll-Like Receptor 4 / antagonists & inhibitors*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cytokines
  • NF-kappa B
  • Tight Junction Proteins
  • Tlr4 protein, rat
  • Toll-Like Receptor 4
  • Apigenin