University of Calgary, Calgary, Alberta, Canada.
Dalhousie University, Halifax, Nova Scotia, Canada.
Arthritis Rheumatol. 2016 Feb;68(2):542-52. doi: 10.1002/art.39411.
Activation of antiinflammatory cholinergic (vagal) pathways can reduce inflammation, and in vitro studies support a pivotal role of α7 nicotinic acetylcholine receptors (α7-nAChR), macrophages, and T cells in these events. The aim of this study was to assess α7-nAChR agonists as an antiinflammatory treatment for Freund's complete adjuvant (CFA)-induced monoarthritis.
Arthritis was induced by intraarticular injection of CFA unilaterally into the knee joints of mice. Animals were treated with α7-nAChR agonists (AR-R17779 or A844606), with or without antagonists (COG133 or methyllycaconitine), and joint inflammation and pain were assessed. Experiments were repeated in c-Kit(W-sh) mast cell-deficient mice, and the effects of an α7-nAChR agonist on mast cell proliferation, migration, and activation by lipopolysaccharide (LPS) were tested.
Treatment with α7-nAChR agonists significantly exacerbated CFA-induced arthritis and pain, as gauged by all indices of assessment, the specificity of which was confirmed by coadministration of an nAChR antagonist that attenuated the increase in disease severity. Toluidine blue-positive mast cells were increased in the joint capsule of CFA plus AR-R17779-treated mice, and AR-R17779 enhanced LPS-induced TNF proliferation and migration of a human mast cell line. The AR-R17779-driven increase in severity of CFA-induced arthritis was significantly reduced in mast cell-deficient mice.
Using CFA to elicit a local inflammatory response, we found that pharmacologic activation of α7-nAChR exacerbated joint inflammation and pain, in part via mast cells, which illustrates the organ- and disease-specific nature of regulatory neuroimmune mechanisms. Thus, α7-nAChR activation may not be uniformly antiinflammatory in all types of inflammatory joint disease.
激活抗炎性胆碱能(迷走)途径可以减轻炎症,体外研究支持α7 烟碱型乙酰胆碱受体(α7-nAChR)、巨噬细胞和 T 细胞在这些事件中的关键作用。本研究旨在评估α7-nAChR 激动剂作为福氏完全佐剂(CFA)诱导的单关节炎的抗炎治疗。
通过向小鼠膝关节腔内单侧注射 CFA 诱导关节炎。用 α7-nAChR 激动剂(AR-R17779 或 A844606)治疗动物,并用或不用拮抗剂(COG133 或甲基-六氢槟榔碱),并评估关节炎症和疼痛。在 c-Kit(W-sh)肥大细胞缺陷小鼠中重复实验,并测试 α7-nAChR 激动剂对肥大细胞增殖、迁移和脂多糖(LPS)激活的影响。
用 α7-nAChR 激动剂治疗显著加重了 CFA 诱导的关节炎和疼痛,所有评估指标均显示出这种加重作用,并用 nAChR 拮抗剂共同给药证实了这种加重作用的特异性,该拮抗剂减轻了疾病严重程度的增加。甲苯胺蓝阳性肥大细胞在 CFA 加 AR-R17779 治疗的小鼠关节囊中增加,AR-R17779 增强了 LPS 诱导的 TNF 增殖和人肥大细胞系的迁移。在肥大细胞缺陷小鼠中,AR-R17779 驱动的 CFA 诱导关节炎严重程度的增加显著降低。
使用 CFA 引起局部炎症反应,我们发现,α7-nAChR 的药理学激活加重了关节炎症和疼痛,部分通过肥大细胞,这说明了调节神经免疫机制的器官和疾病特异性。因此,α7-nAChR 激活在所有类型的炎性关节疾病中可能不是一致的抗炎作用。