PMID- 11878205 OWN - NLM STAT- MEDLINE DCOM- 20020327 LR - 20220408 IS - 0004-4172 (Print) IS - 0004-4172 (Linking) VI - 52 IP - 2 DP - 2002 TI - Effects of antihistamines on leukotriene and cytokine release from dispersed nasal polyp cells. PG - 97-102 AB - In this study the effects of antihistamines on the release of eicosanoids and the pro-inflammatory cytokine tumor necrosis factor alpha (TNF alpha) were compared. Enzymatically dispersed cells from human nasal polyps served as an in vitro model of chronic respiratory mucosal inflammation. Nasal polyp cells (2 x 10(5)/ml) were sensitized with human IgE pre-incubated azelastine (CAS 58581-89-8), terfenadine (CAS 50679-08-8), levocabastine (CAS 79516-68-0) or cetirizine (CAS 83881-51-0), and stimulated with anti-human immunoglobulin E (IgE). Thromboxane B2 (TBX2) and leukotriene C4 (LTC4) were measured by radioimmunoassay (RIA), TNF alpha by enzyme-linked immunosorbent assay (ELISA). Data represent mean values of % inhibition estimated from the untreated positive control or mean IC50 (n = 5). Azelastine and terfenadine inhibited TNF alpha release with IC50 values of 6.2 mumol/l and 4.3 mumol/l, respectively. Terfenadine reduced TXB2 release by 37 +/- 15%, and LTC4 release was decreased by azelastine and terfenadine very potently by 86% and 100%, respectively. Azelastine shows anti-inflammatory properties in therapeutically relevant concentrations as assessed by its ability to reduce TNF alpha release as well as its ability to inhibit LTC4 production in allergically stimulated human nasal polyp cells. FAU - Kusters, Sabine AU - Kusters S AD - Pulmonary Pharmacology, Corporate Research ASTA Medica AG/Arzneimittelwerk Dresden GmbH, Radebeul, Germany. FAU - Schuligoi, Rufina AU - Schuligoi R FAU - Huttenbrink, Karl-Bernd AU - Huttenbrink KB FAU - Rudert, Jutta AU - Rudert J FAU - Wachs, Angela AU - Wachs A FAU - Szelenyi, Istvan AU - Szelenyi I FAU - Peskar, Bernhard A AU - Peskar BA LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Germany TA - Arzneimittelforschung JT - Arzneimittel-Forschung JID - 0372660 RN - 0 (Cytokines) RN - 0 (Eicosanoids) RN - 0 (Histamine Antagonists) RN - 0 (Leukotrienes) RN - 0 (Tumor Necrosis Factor-alpha) RN - 2CU6TT9V48 (Leukotriene C4) RN - 37341-29-0 (Immunoglobulin E) RN - 54397-85-2 (Thromboxane B2) SB - IM MH - Cytokines/*metabolism MH - Eicosanoids/metabolism MH - Epithelial Cells/drug effects/metabolism MH - Histamine Antagonists/*pharmacology MH - Humans MH - Immunoglobulin E MH - Leukotriene C4/metabolism MH - Leukotrienes/*metabolism MH - Nasal Polyps/*metabolism/pathology MH - Thromboxane B2/metabolism MH - Tumor Necrosis Factor-alpha/metabolism EDAT- 2002/03/07 10:00 MHDA- 2002/03/28 10:01 CRDT- 2002/03/07 10:00 PHST- 2002/03/07 10:00 [pubmed] PHST- 2002/03/28 10:01 [medline] PHST- 2002/03/07 10:00 [entrez] AID - 10.1055/s-0031-1299863 [doi] PST - ppublish SO - Arzneimittelforschung. 2002;52(2):97-102. doi: 10.1055/s-0031-1299863.