Nasser Salma, El-Abhar Hanan S, El-Maraghy Nabila, Abdallah Dalaal M, Wadie Walaa, Mansour Suzan
Pharmacology, Toxicology and Biochemistry Department, Faculty of Pharmacy, Future University in Egypt (FUE), Cairo, Egypt.
Pharmacology, Toxicology and Biochemistry Department, Faculty of Pharmacy, Future University in Egypt (FUE), Cairo, Egypt.
Biomed Pharmacother. 2025 Feb;183:117816. doi: 10.1016/j.biopha.2025.117816. Epub 2025 Jan 13.
While cognitive impairment has been documented in ulcerative colitic patients, the possible influence of central β3-adrenergic receptor (β3-AR) signaling on this extraintestinal manifestation remains unclear. Previously, we identified an imperative role for mirabegron (MA) as an agonist of β3-AR, in decreasing the BACE-1/beta-amyloid (Aβ) cue in the colons of UC rats. Consequently, we investigated its therapeutic potential for alleviating cognitive impairment associated with UC. To fulfil our aim, rats administered iodoacetamide were treated with the β3-AR agonist (MA) alone, with the antagonist (SR59230A) for 8 days, or kept untreated. The animals' behavior (MWM and NOR tests) and hippocampal structure were assessed. Mechanistically, necroptosis, ER stress (ERS), Aβ-amyloidosis, inflammation/oxidative burden, and gut/BBB dysfunction were analyzed. Post-administration of MA improved weight gain, colon/hippocampal structures, and memory. Additionally, it inhibited serum levels of lipopolysaccharide and Annexin-1, indicating recovered gut and BBB integrity. MA turned off the pathogenic BACE-1/Aβ axis in the hippocampus, necroptosis trajectory (TNFR-1/RIPK1/RIPK3/MLKL), and the IRE-1α/JNK signal. Moreover, MA enhanced the transcription factor PPAR-γ, decreased NF-κΒ/TNF-α inflammatory hub, and modulated the redox imbalance by decreasing malondialdehyde and increasing catalase. Notably, MA's behavioral, structural, and molecular beneficial actions were hindered by the pre-administration of SR59230A. From a novel standpoint, we recognized the β3-AR as a therapeutic target for UC-associated cognitive impairment in the hippocampus. In this context, the aptitude of MA to inhibit UC-induced hippocampal amyloidogenesis, alongside its anti-necroptotic, anti-ERS, anti-inflammatory, and antioxidant effects, contribute to these central enhancements, while also regulating permeability in both gut and BBB barriers.
虽然溃疡性结肠炎患者存在认知障碍,但中枢β3肾上腺素能受体(β3-AR)信号传导对这种肠外表现的可能影响仍不清楚。此前,我们发现米拉贝隆(MA)作为β3-AR激动剂,在降低UC大鼠结肠中β分泌酶1/β淀粉样蛋白(Aβ)信号方面具有重要作用。因此,我们研究了其缓解与UC相关的认知障碍的治疗潜力。为实现我们的目标,给给予碘乙酰胺的大鼠单独用β3-AR激动剂(MA)、拮抗剂(SR59230A)治疗8天,或不进行治疗。评估动物的行为(水迷宫和新物体识别测试)和海马结构。从机制上分析坏死性凋亡、内质网应激(ERS)、Aβ淀粉样变性、炎症/氧化负担以及肠道/血脑屏障功能障碍。给予MA后,体重增加、结肠/海马结构和记忆力得到改善。此外,它抑制血清脂多糖和膜联蛋白-1水平,表明肠道和血脑屏障完整性得以恢复。MA关闭了海马体中致病性β分泌酶1/Aβ轴、坏死性凋亡途径(肿瘤坏死因子受体-1/受体相互作用蛋白激酶1/受体相互作用蛋白激酶3/混合谱系激酶结构域样蛋白)以及肌醇需求酶1α/应激活化蛋白激酶信号。此外,MA增强转录因子过氧化物酶体增殖物激活受体γ,降低核因子κB/肿瘤坏死因子-α炎症枢纽,并通过降低丙二醛和增加过氧化氢酶来调节氧化还原失衡。值得注意的是,预先给予SR59230A会阻碍MA的行为、结构和分子有益作用。从一个新的角度来看,我们认识到β3-AR是UC相关海马体认知障碍的治疗靶点。在这种情况下,MA抑制UC诱导的海马体淀粉样蛋白生成的能力,以及其抗坏死性凋亡、抗内质网应激、抗炎和抗氧化作用,促成了这些中枢改善,同时还调节肠道和血脑屏障的通透性。