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

Objective Microglia play an important role in the neuroinflammation developed in response to various pathologies. In this study, we examined the anti-inflammatory effect of the new human histamine H 3 receptor (H 3 R) ligands with flavonoid structure in murine microglial BV-2 cells. Material and met...

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Bibliographic Details
Published in:Inflammation research 2023-02, Vol.72 (2), p.181-194
Main Authors: Honkisz-Orzechowska, Ewelina, Popiołek-Barczyk, Katarzyna, Linart, Zuzanna, Filipek-Gorzała, Jadwiga, Rudnicka, Anna, Siwek, Agata, Werner, Tobias, Stark, Holger, Chwastek, Jakub, Starowicz, Katarzyna, Kieć-Kononowicz, Katarzyna, Łażewska, Dorota
Format: Article
Language:English
Subjects:
Affinity
Allergology
Anti-inflammatory agents
Assaying
Biomedical and Life Sciences
Biomedicine
Cell viability
Cytokines
Cytotoxicity
Dermatology
Enzyme-linked immunosorbent assay
Evaluation
Flavonoids
Histamine
Histamine H3 receptors
Immunocytochemistry
Immunology
Inflammation
Interleukin 6
Ligands
Microglia
mRNA
Neurology
Original Research
Pharmacology/Toxicology
Receptors
Rheumatology
Toxicity
Tumor necrosis factor-α
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Summary:Objective Microglia play an important role in the neuroinflammation developed in response to various pathologies. In this study, we examined the anti-inflammatory effect of the new human histamine H 3 receptor (H 3 R) ligands with flavonoid structure in murine microglial BV-2 cells. Material and methods The affinity of flavonoids ( E243 -flavone and IIIa – IIIc —chalcones) for human H 3 R was evaluated in the radioligand binding assay. The cytotoxicity on BV-2 cell viability was investigated with the MTS assay. Preliminary evaluation of anti-inflammatory properties was screened by the Griess assay in an in vitro neuroinflammation model of LPS-treated BV-2 cells. The expression and secretion of pro-inflammatory cytokines were evaluated by real-time qPCR and ELISA, respectively. The expression of microglial cell markers were determined by immunocytochemistry. Results Chalcone derivatives showed high affinity at human H 3 R with K i values 
ISSN:1023-3830
1420-908X
DOI:10.1007/s00011-022-01658-z