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Anti-inflammatory effects of new human histamine H3 receptor ligands with flavonoid structure on BV-2

Ewelina Honkisz-Orzechowska1, Katarzyna Popiołek-Barczyk2, Zuzanna Linart3

  • 1Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College in Kraków, Medyczna 9, 30-688, Kraków, Poland. ewelina.honkisz@uj.edu.pl.

Inflammation Research : Official Journal of the European Histamine Research Society ... [Et Al.]
|November 12, 2022
PubMed
Abstract

Insights

New chalcone derivatives targeting the histamine H3 receptor (H3R) show anti-inflammatory effects in microglia. Compound IIIc reduced inflammatory markers, suggesting potential therapeutic applications for neuroinflammation.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Immunology

Background:

  • Microglia are key players in neuroinflammation, a process implicated in various neurological diseases.
  • Histamine H3 receptor (H3R) ligands are being investigated for their therapeutic potential.
  • Flavonoids, a class of natural compounds, possess diverse biological activities.

Purpose of the Study:

  • To evaluate the anti-inflammatory effects of novel human H3R ligands with flavonoid structures.
  • To investigate the mechanism of action of these compounds in a microglial cell model.

Main Methods:

  • Radioligand binding assays were used to determine the affinity of flavonoids for human H3R.
  • Cytotoxicity was assessed using the MTS assay on BV-2 cells.
  • Anti-inflammatory activity was evaluated via Griess assay, real-time qPCR, ELISA, and immunocytochemistry.

Main Results:

  • Chalcone derivatives exhibited high affinity for human H3R (Ki < 25 nM).
  • Compound IIIc demonstrated significant anti-inflammatory effects, reducing nitrite levels and down-regulating pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) at both mRNA and protein levels.
  • Immunocytochemistry confirmed the expression of microglial markers (Iba1, CD68, CD206) in BV-2 cells.

Conclusions:

  • Novel chalcone derivatives targeting H3R possess significant anti-inflammatory properties in microglia.
  • Compound IIIc is a promising candidate for further investigation into its anti-inflammatory mechanisms.
  • These findings highlight the therapeutic potential of H3R ligands in managing neuroinflammation.
Keywords:
ChalconeHistamine H3 receptorMicrogliaNeuroinflammation

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