Azelastine is more potent than olopatadine in inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells
| Autor: | Sheila Jeudy, Achilles Athanasiou, Richard Letourneau, Kristiana Kandere, Duraisamy Kempuraj, Theoharis C. Theoharides, William Boucher, Kathleen Spear, Kim Fitzgerald, Man Huang |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Pulmonary and Respiratory Medicine
medicine.medical_specialty Azelastine Hydrochloride Immunology Tryptase Lymphocyte Activation Histamine Release chemistry.chemical_compound Internal medicine Anti-Allergic Agents medicine Humans Immunology and Allergy Mast Cells Olopatadine Hydrochloride Cells Cultured Dose-Response Relationship Drug biology Interleukin-6 business.industry Serine Endopeptidases Olopatadine Fetal Blood Mast cell Azelastine medicine.anatomical_structure Endocrinology chemistry Antiallergic agent biology.protein Phthalazines Tryptases business Dibenzoxepins Histamine medicine.drug |
| Zdroj: | Annals of Allergy, Asthma & Immunology. 88:501-506 |
| ISSN: | 1081-1206 |
| DOI: | 10.1016/s1081-1206(10)62389-7 |
| Popis: | Background Mast cells are involved in early- and late-phase reactions by releasing vasoactive molecules, proteases, and cytokines. Certain histamine-1 receptor antagonists and other antiallergic drugs seem to inhibit the release of mediators from rat and human mast cells. Objective Azelastine and olopatadine are antiallergic agents present in the ophthalmic solutions azelastine hydrochloride (Optivar, Asta Medica/Muro Pharmaceuticals, Tewksbury, MA), and olopatadine hydrochloride (Patanol, Alcon Laboratories, Fort Worth, TX), respectively. We investigated the effect of these drugs on interleukin-6 (IL-6), tryptase, and histamine release from cultured human mast cells (CHMCs). Methods CHMCs were grown from human umbilical cord blood-derived CD34+ cells in the presence of stem cell factor and IL-6 for 14 to 16 weeks. Sensitized CHMCs were pretreated with various concentrations of azelastine or olopatadine for 5 minutes. CHMCs were then challenged with anti-immunoglobulin E, and the released mediators were quantitated. Results The greatest inhibition of mediator release was seen with 24 μM azelastine; this level of inhibition was matched with the use of 133 μM olopatadine. At this concentration, these drugs inhibited IL-6 release by 83% and 74%, tryptase release by 55% and 79%, and histamine release by 41% and 45%, respectively. Activated CHMCs were characterized by numerous filopodia that were inhibited by both drugs as shown by electron microscopy. Conclusions These results indicate that azelastine and olopatadine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine. |
| Databáze: | OpenAIRE |
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