Pien-Tze-Huang attenuates neuroinflammation in cerebral ischaemia-reperfusion injury in rats through the TLR4/NF-κB/MAPK pathway

Pharm Biol. 2021 Dec;59(1):828-839. doi: 10.1080/13880209.2021.1942926.

Abstract

Context: Pien-Tze-Huang (PTH) is traditionally applied to treat various inflammation-related diseases including stroke. However, literature regarding the anti-inflammatory effects and possible mechanisms of PTH in ischaemic stroke is unavailable.

Objective: This study investigates the anti-inflammatory effects and its underlying mechanism of PTH on ischaemic stroke.

Materials and methods: Cerebral ischaemia-reperfusion injury was induced through 2 h middle cerebral artery occlusion (MCAO) followed by 24 h reperfusion in male Sprague-Dawley (SD) rats receiving oral pre-treatment with PTH (180 mg/kg) for 4 days. TLR4 antagonist TAK-242 (3 mg/kg) was injected intraperitoneally at 1.5 h after MCAO. MRI, HE staining, qRT-PCR, western blot, and immunofluorescence methods were employed.

Results: PTH treatment markedly reduced cerebral infarct volume (by 51%), improved neurological function (by 33%), and ameliorated brain histopathological damage in MCAO rats. It also reduced the levels of four inflammatory mediators including IL-1β (by 70%), IL-6 (by 78%), TNF-α (by 60%) and MCP-1 (by 58%); inhibited microglia and astrocyte activation; and decreased protein expression of iNOS and COX-2 in injured brains. Moreover, PTH down-regulated the protein expressions of TLR4, MyD88, and TRAF6; reduced the expression and nuclear translocation of NF-κB; and lowered the protein expressions of p-ERK1/2, p-JNK, and p-p38. Similar effects were observed in MCAO rats with TAK-242 treatment. However, combined administration of PTH and TAK-242 did not significantly reinforce the anti-inflammatory effects of PTH.

Discussion and conclusion: PTH improved cerebral ischaemia-reperfusion injury by inhibiting neuroinflammation partly via the TLR4/NF-κB/MAPK signalling pathway, which will help guide its clinical application.

Keywords: Ischaemic stroke; neuroprotection; signalling pathways.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Brain Ischemia / drug therapy
  • Brain Ischemia / pathology
  • Disease Models, Animal
  • Drugs, Chinese Herbal / pharmacology*
  • Infarction, Middle Cerebral Artery
  • Ischemic Stroke / drug therapy*
  • Ischemic Stroke / pathology
  • MAP Kinase Signaling System / drug effects
  • Male
  • NF-kappa B / metabolism
  • Neuroinflammatory Diseases / drug therapy*
  • Neuroinflammatory Diseases / pathology
  • Rats
  • Rats, Sprague-Dawley
  • Reperfusion Injury / complications
  • Reperfusion Injury / drug therapy
  • Sulfonamides / pharmacology
  • Toll-Like Receptor 4 / metabolism

Substances

  • Anti-Inflammatory Agents
  • Drugs, Chinese Herbal
  • NF-kappa B
  • Sulfonamides
  • Tlr4 protein, rat
  • Toll-Like Receptor 4
  • ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
  • pien tze huang

Grants and funding

This study was supported by the National Natural Science Foundation of China [81973437], the Department of Technology and Science of Fujian Province [2019J01724], and the School Management Project of Fujian University of traditional Chinese Medicine [X2018013].