Mhillaj Emanuela, Papi Massimiliano, Paciello Fabiola, Silvestrini Andrea, Rolesi Rolando, Palmieri Valentina, Perini Giordano, Fetoni Anna Rita, Trabace Luigia, Mancuso Cesare
Department of Healthcare Surveillance and Bioethics, Section of Pharmacology, Università Cattolica del Sacro Cuore, Rome, Italy.
Fondazione Policlinico Universitario Agostino Gemelli IRCCS, Rome, Italy.
Front Cell Dev Biol. 2020 Sep 29;8:561179. doi: 10.3389/fcell.2020.561179. eCollection 2020.
The formation and aggregation of amyloid-β-peptide (Aβ) into soluble and insoluble species represent the pathological hallmarks of Alzheimer's disease (AD). Over the last few years, however, soluble Aβ (sAβ) prevailed over fibrillar Aβ (fAβ) as determinant of neurotoxicity. One of the main therapeutic strategies for challenging neurodegeneration is to fight against neuroinflammation and prevent free radical-induced damage: in this light, the heme oxygenase/biliverdin reductase (HO/BVR) system is considered a promising drug target. The aim of this work was to investigate whether or not celecoxib (CXB), a selective inhibitor of the pro-inflammatory cyclooxygenase-2, modulates the HO/BVR system and prevents lipid peroxidation in SH-SY5Y neuroblastoma cells. Both sAβ (6.25-50 nM) and fAβ (1.25-50 nM) dose-dependently over-expressed inducible HO (HO-1) after 24 h of incubation, reaching statistical significance at 25 and 6.25 nM, respectively. Interestingly, CXB (1-10 μM, for 1 h) further enhanced Aβ-induced HO-1 expression through the nuclear translocation of the transcriptional factor Nrf2. Furthermore, 10 μM CXB counteracted the Aβ-induced ROS production with a mechanism fully dependent on HO-1 up-regulation; nevertheless, 10 μM CXB significantly counteracted only 25 nM sAβ-induced lipid peroxidation damage in SH-SY5Y neurons by modulating HO-1. Both carbon monoxide (CORM-2, 50 nM) and bilirubin (50 nM) significantly prevented ROS production in Aβ-treated neurons and favored both the slowdown of the growth rate of Aβ oligomers and the decrease in oligomer/fibril final size. In conclusion, these results suggest a novel mechanism through which CXB is neuroprotective in subjects with early AD or mild cognitive impairment.
淀粉样β肽(Aβ)形成并聚集成可溶性和不溶性物质是阿尔茨海默病(AD)的病理特征。然而,在过去几年中,可溶性Aβ(sAβ)作为神经毒性的决定因素,其作用超过了纤维状Aβ(fAβ)。对抗神经退行性变的主要治疗策略之一是对抗神经炎症并预防自由基诱导的损伤:鉴于此,血红素加氧酶/胆绿素还原酶(HO/BVR)系统被认为是一个有前景的药物靶点。这项工作的目的是研究选择性促炎环氧化酶-2抑制剂塞来昔布(CXB)是否能调节HO/BVR系统并预防SH-SY5Y神经母细胞瘤细胞中的脂质过氧化。在孵育24小时后,sAβ(6.25 - 50 nM)和fAβ(1.25 - 50 nM)均呈剂量依赖性地过度表达诱导型HO(HO-1),分别在25 nM和6.25 nM时达到统计学显著水平。有趣的是,CXB(1 - 10 μM,作用1小时)通过转录因子Nrf2的核转位进一步增强了Aβ诱导的HO-1表达。此外,10 μM CXB通过完全依赖HO-1上调的机制抵消了Aβ诱导的ROS产生;然而,10 μM CXB仅通过调节HO-1显著抵消了25 nM sAβ诱导的SH-SY5Y神经元脂质过氧化损伤。一氧化碳(CORM-2,50 nM)和胆红素(50 nM)均显著预防了Aβ处理神经元中的ROS产生,并有利于减缓Aβ寡聚体的生长速率以及降低寡聚体/纤维的最终大小。总之,这些结果提示了一种新机制,通过该机制CXB对早期AD或轻度认知障碍患者具有神经保护作用。