Recent studies suggest that several second-generation antihistamines can modulate various inflammatory reactions besides their H1-receptor antagonism. The antihistamine cetirizine is a racemic mixture of levocetirizine and dextrocetirizine. The aim of this study was to investigate the effects of these two antihistamines (cetirizine and levocetirizine) on granulocyte-macrophage colony-stimulating factor (GM-CSF) and interleukin (IL)-8 secretion in A549 human airway epithelial cells. A549 cells were preincubated with cetirizine (0.1, 1, 2.5, 5, and 10 M) or levocetirizine (0.1, 1, 2.5, 5, and 10 M) individually for 16 hours and were then stimulated with IL-1beta for 8 hours. The levels of GM-CSF and IL-8 in cultured supernatants were measured by enzyme-linked immunosorbent assay (ELISA). Our data showed that cetirizine (5 and 10 M) and levocetirizine (2.5, 5, and 10 M) significantly suppressed GM-CSF secretion from A549 cells stimulated with IL-1 (p < 0.05). Cetirizine (10 M) and levocetirizine (5 and 10 M) significantly suppressed IL-8 secretion after A549 was stimulated. The suppressive effect was comparable between levocetirizine, 2.5 M, and cetirizine, 5 M, as well as levocetirizine, 5 M, and cetirizine, 10 M. Moreover, levocetirizine, 5 M, was better than cetirizine, 5 M, on suppressing IL-8 secretion, but such a difference did not appear in other conditions. Our results suggest that cetirizine and levocetirizine at higher concentrations can reduce the release of GM-CSF and IL-8 from A549 cells stimulated with IL-1. These observations indicate that the two second-generation antihistamines may exert anti-inflammatory effects beyond histamine H1-receptor antagonist, and levocetirizine plays a major role in terms of this activity.
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granulocyte-macrophage colony-stimulating factor;
secondary generation antihistamines
Document Type: Research Article
From the Division of Immunology and Nephrology, Department of Pediatrics,
Division of Chest Medicine, Department of Internal Medicine, Taichung Veterans General Hospital, Taichung, Taiwan, and , Institute of Medicine, Chung Shan Medical University, Taichung, Taiwan
Publication date: 2008-09-01
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