Home General Physiology and Biophysics 2015 General Physiology and Biophysics Vol.34, No.2, p.209–216, 2015

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Quarterly, 80 pp. per issue
Founded: 1982
ISSN  1338-4325 (online)

Published in English

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General Physiology and Biophysics Vol.34, No.2, p.209–216, 2015

Title: Molecular pharmacology of antihistamines in inhibition of oxidative burst of professional phagocytes
Author: Radomír Nosáľ, Viera Jančinová, Katarína Drábiková, Tomáš Perečko

Abstract: Antihistamines of the H1 and H3/H4 groups interfere with oxidative burst of human professional phagocytes in vitro. In the concentration of 10 μM, H1 antihistamines of the 1st and 2nd generation inhibited oxidative burst of human neutrophils in the rank order of potency: dithiaden > loratadine > brompheniramine > chlorpheniramine > pheniramine. Of the H1 antihistamines, the most effective was dithiaden in suppressing oxidative burst of whole human blood and dose-dependently the chemiluminescence of isolated neutrophils at extra- and intracellular level. Inhibition of free oxygen radical generation in isolated neutrophils by dithiaden resulted from the inhibition of protein kinase C activation. The potentiation of recombinant caspase-3 by dithiaden is supportive of the antiinflammatory effect of dithiaden and suggestive of increasing the apoptosis of professional phagocytes. Of the H3/H4 antihistamines, the most effective was JNJ7777120 in decreasing chemiluminescence in whole blood and also at extra- and intracellular sites of isolated neutrophils. JNJ 10191584 and thioperamide were less effective and the latter significantly potentiated free oxygen radical generation intracellularly. The results demonstrated that, compared with the H3/H4 antihistamines investigated, H1 antihistamines were much more potent in inhibiting free oxygen radical generation in human professional phagocytes. This finding should be taken into account therapeutically.

Keywords: Professional phagocytes — Oxidative burst — Chemiluminescence — Antihistamines — Protein kinase C — Recombinant caspase-3
Year: 2015, Volume: 34, Issue: 2 Page From: 209, Page To: 216

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