Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Int Immunopharmacol. 2011 Aug;11(8):1052-6. doi: 10.1016/j.intimp.2011.02.026. Epub 2011 Mar 5.
Mast cells stimulation activates degranulation process resulting in releasing of mediators, such as histamine. In this study, the effect of aqueous extract of sitagliptin, a selective dipeptidylpeptidase-4 inhibitor, on the mast cell-mediated allergic response was studied with the possible mechanisms of action, focusing on the histamine release and pro-inflammatory cytokine secretion in mast cells. Sitagliptin produced dose dependent inhibition in compound 48/80-induced systemic reactions. In addition, sitagliptin attenuated IgE-mediated skin allergic reaction. Sitagliptin dose-dependently reduced compound 48/80- and IgE-induced histamine release from mast cells. Sitagliptin decreased the secretion of pro-inflammatory cytokines, tumor necrosis factor-α, in mast cells. So, the finding of this study provides evidence that sitagliptin inhibits mast cell derived allergic reactions, and involvement of pro-inflammatory cytokine secretion in such effects.
肥大细胞的刺激会激活脱颗粒过程,导致介质如组胺的释放。在这项研究中,研究了选择性二肽基肽酶-4 抑制剂西他列汀的水提取物对肥大细胞介导的过敏反应的影响,其作用机制可能集中在肥大细胞中的组胺释放和促炎细胞因子分泌上。西他列汀对化合物 48/80 诱导的全身反应呈剂量依赖性抑制。此外,西他列汀减弱了 IgE 介导的皮肤过敏反应。西他列汀剂量依赖性地减少了化合物 48/80 和 IgE 诱导的肥大细胞中组胺的释放。西他列汀减少了促炎细胞因子肿瘤坏死因子-α在肥大细胞中的分泌。因此,这项研究的结果提供了证据表明,西他列汀抑制肥大细胞来源的过敏反应,并且促炎细胞因子分泌参与了这种作用。