Ac-YVAD-cmk improves neurological function by inhibiting caspase-1-mediated inflammatory response in the intracerebral hemorrhage of rats

Int Immunopharmacol. 2019 Oct:75:105771. doi: 10.1016/j.intimp.2019.105771. Epub 2019 Jul 25.

Abstract

Objective: Intracerebral hemorrhage (ICH) is acknowledged as a serious clinical problem lacking effective treatments. And caspase-1-mediated inflammatory response happened during the progression of ICH. Therefore, we aimed to investigate the effects of caspase-1 inhibitor Ac-YVAD-cmk on ICH.

Materials and methods: Microglia cells were isolated and activated by thrombin for 24 h. Then the transcript and protein expressions of NLRP3 and inflammatory factors were assessed by RT-PCR and western blotting. Moreover, Ac-YVAD-cmk was injected into the ICH model. The mNSS and brain water content were tested at 24 h post-ICH. Finally, the pathological changes of microglia activation following ICH were discovered by the immunohistochemical and HE staining ways.

Results: Ac-YVAD-cmk inhibited the activation of pro-caspase-1 and decreased brain edema, in association with decreasing activated microglia and the expression of inflammation-related factors at 24 h post-ICH. Consequently, Ac-YVAD-cmk reduced the release of mature IL-1β/IL-18 in perihematoma, improved the behavioral performance, and alleviated microglia in perihematoma region in ICH rats.

Conclusions: These results indicate that caspase-1 could amplify the plural inflammatory responses in the ICH. Administration of Ac-YVAD-cmk has the potential to be a novel therapeutic strategy for ICH.

Keywords: Ac-YVAD-cmk; Caspase-1; Intracerebral hemorrhage; Microglia.

MeSH terms

  • Amino Acid Chloromethyl Ketones / pharmacology
  • Amino Acid Chloromethyl Ketones / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Behavior, Animal / drug effects
  • Brain / drug effects
  • Brain / pathology
  • Caspase 1 / immunology*
  • Caspase Inhibitors / pharmacology
  • Caspase Inhibitors / therapeutic use*
  • Cells, Cultured
  • Cerebral Hemorrhage / drug therapy*
  • Cerebral Hemorrhage / immunology
  • Cerebral Hemorrhage / pathology
  • Interleukin-18 / genetics
  • Interleukin-18 / immunology
  • Interleukin-1beta / genetics
  • Interleukin-1beta / immunology
  • Male
  • Microglia
  • NLR Family, Pyrin Domain-Containing 3 Protein / genetics
  • NLR Family, Pyrin Domain-Containing 3 Protein / immunology
  • Neuroprotective Agents / pharmacology
  • Neuroprotective Agents / therapeutic use*
  • Rats, Sprague-Dawley

Substances

  • Amino Acid Chloromethyl Ketones
  • Anti-Inflammatory Agents
  • Caspase Inhibitors
  • IL1B protein, rat
  • Interleukin-18
  • Interleukin-1beta
  • N-acetyl-tyrosyl-valyl-alanyl-aspartyl chloromethyl ketone
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • Neuroprotective Agents
  • Nlrp3 protein, rat
  • Caspase 1