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  • Cetirizine  (1)
  • Copper niflumate  (1)
  • Immunomodulator  (1)
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  • 1
    ISSN: 0047-6374
    Keywords: Ageing ; Immunomodulator ; Migration ; Oxidative metabolism ; Polymorphonuclear leukocytes
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1420-908X
    Keywords: Pleurisy ; Burn ; Polymorphonuclear ; Copper niflumate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Antiinflammatory activities and modulations of PMNL responses produced by treatment with tetrakis-μ-2-[3-(trifluoromethyl)-phenyl] aminonicotinatodicopper (II) [Cu(II)2(niflumate)4] and niflumic acid were studied in isologous serum-induced rat pleurisy. Doses of 10 or 30 mg/kg (35 or 106 µmol/kg) of niflumic acid or Cu(II)2 (niflumate)4 (8 or 23 µmol/kg) caused significant (p 〈 0.01) reductions in pleural exudate and number of polymorphonuclear leukocytes (PMNLs) in the exudate. While both doses of Cu(II)2(niflumate)4 produced significant dose-related reductions in both parameters, only the higher dose of niflumic acid produced a significant dose-related reduction in both parameters. Boyden chamber measurements of N-formyl-methionyl-leucyl-phenylalanine (f-MLP) chemotaxis by PMNLs incubated with 10 or 30 µg/ml niflumic acid (35 or 106 nmol/ml) or Cu(II)2(niflumate)4 (8 or 23 nmol/ml) were significantly (p 〈 0.01 to p 〈 0.001) decreased in dose-related fashions. Chemotaxis of PMNLs from pleuritic rats treated orally with 10 or 30 mg/kg niflumic acid or Cu(II)2(niflumate)4 was significantly (p 〈 0.001) inhibited by the larger dose of niflumic acid and both doses of Cu(II)2(niflumate)4. Opsonized zymosan (OZ)-stimulated chemiluminescence (CL) of PMNLs from pleuritic rats treated orally with these same doses of niflumic acid or Cu(II)2(niflumate)4 was only significantly (p 〈 0.05 or p 〈 0.01 respectively) decreased by the larger doses. Superoxide (O 2 - ) production by these cells was significantly decreased by the larger dose of niflumic acid (p 〈 0.05) while both doses of Cu(II)2(niflumate)4 produced significant (p 〈 0.05 to p 〈 0.01) decreases. Recovery of the decreased PMNL response in burned rats was also studied following treatment with these two compounds. Oral treatment of non-burned rats with 1 mg/kg niflumic acid (4 µmol/kg) or Cu(II)2(niflumate)4 (1 µmol/kg) did not affect OZ-stimulated O 2 - production while decreased O 2 - production in non-treated scald-burned rats was reversed by oral treatment with either niflumic acid or Cu(II)2(niflumate)4. It is concluded that Cu(II)2(niflumate)4 is a more effective antiinflammatory agent than niflumic acid and more effective modulation of PMNL responsiveness may explain its beneficial antipleuritic and burn-injury recovery effects. Formation of the copper complex of niflumic acidin vivo may also account for its beneficial antiinflammatory effects and recovery of depressed PMNL responsiveness in burned rats.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1420-908X
    Keywords: Cetirizine ; Anti H1 ; PGE2 ; IL-1 ; Monocyte/macrophage
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Cetirizine was first described as a specific anti-H1 molecule displaying potent antiallergic activity. It was later found that its pharmacological properties extended to cellular actions as on eosinophil recruitment at inflammatory sites in allergic patients. Monocytes and macrophages participate in allergic mechanisms, particularly through high affinity H1 and H2 membrane receptors and generation of pro- and anti-inflammatory agents; among them histamine-induced factors, IL-1 and prostanoids are of importance. The aim of this work was to investigate the effect exerted by various concentrations of cetirizine (0.1–10 μg/ml) appliedin vitro to human monocytes and peritoneal rat macrophages cultured for 24 h. Peritoneal macrophages were collected either from normal or experimentally inflamed rats. Human monocytes, isolated from peripheral blood, were studied either in a resting state or after stimulation by LPS fromEscherichia coli (1 and 10 μg/ml). Cetirizine (10 μg/ml) significantly enhanced IL-1 release by human monocytes stimulated by a weak LPS concentration (1 μg/ml) but could not modify the maximal increase of IL-1 release induced by 10 μg/ml of LPS. It did not exert any effect on resting cells. Cetirizine (0.1–10 μg/ml) enhanced PGE2 release by resting human monocytes. Concentrations of 1 and 10 μg/ml enhanced PGE2 release by LPS-stimulated monocytes, and by healthy and inflamed rat macrophages. This effect was concentration-dependent. Our findings point to an anti-inflammatory action of cetirizine via PGE2 release and histamine H2 interactions. Cetirizine did not directly modify IL-1 generation by resting monocytes but the IL-1 production observed after LPS stimulation could promote the mechanisms by which PGE2 is released.
    Type of Medium: Electronic Resource
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