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• W2193758384 abstract "The <i>α</i>7 pentamer nicotinic acetylcholine receptors (nAChRs) are a target in transduction of anti-inflammatory signals from the central nervous system to the gastrointestinal (GI) tract. The aim of this study was to investigate the anti-inflammatory action of the novel <i>α</i>7 nAChR partial agonist encenicline and to determine the mechanism underlying its activity. Anti-inflammatory activity of encenicline was evaluated using trinitrobenzenesulfonic acid (TNBS)- and dextran sulfate sodium (DSS)-induced models of colitis. Macroscopic score, ulcer score, colon length and thickness, as well as myeloperoxidase (MPO) activity were recorded. Immunohistochemistry (IHC) was used to measure the infiltration of immune cells in the colon. Furthermore, we employed flow cytometry to determine the effect of encenicline on frequencies of FoxP3⁺ and interleukin (IL)-17A⁺ T cells in the mouse colon. Encenicline attenuated TNBS- and DSS-induced colitis in mice via <i>α</i>7 nAChRs, as indicated by significantly reduced macroscopic parameters and MPO activity. Treatment with encenicline significantly reduced the infiltration of macrophages, neutrophils, and B cells in the colon of TNBS-treated animals, as indicated by IHC. In the TNBS model encenicline reduced the frequency of FoxP3⁺ IL-17A⁺ T cells in the colon. In the DSS-model treatment encenicline increased the frequency of FoxP3⁺ T cells and reduced IL-17A⁺ T cells. Stimulation of <i>α</i>7 nAChR with partial agonist encenicline alleviates colitis via alteration of the number and/or activation status of the immune cells in the gut, emphasizing a potential role of <i>α</i>7 nAChRs as a target for anticolitic drugs." @default.
• W2193758384 created "2016-06-24" @default.
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• W2193758384 date "2015-10-13" @default.
• W2193758384 modified "2023-10-17" @default.
• W2193758384 title "Encenicline, an 7 Nicotinic Acetylcholine Receptor Partial Agonist, Reduces Immune Cell Infiltration in the Colon and Improves Experimental Colitis in Mice" @default.
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• W2193758384 doi "https://doi.org/10.1124/jpet.115.228205" @default.
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