Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
PLoS One. 2018 Sep 27;13(9):e0203837. doi: 10.1371/journal.pone.0203837. eCollection 2018.
Countless neurodegenerative diseases are associated with perverse multiple targets of cyclic nucleotide signalling, hastening neuronal death. Cilostazol, a phosphodiesterase-III inhibitor, exerts neuroprotective effects against sundry models of neurotoxicity, however, its role against Huntington's disease (HD) has not yet been tackled. Hence, its modulatory effect on several signalling pathways using the 3-nitropropionic acid (3-NP) model was conducted. Animals were injected with 3-NP (10 mg/kg/day, i.p) for two successive weeks with or without the administration of cilostazol (100 mg/kg/day, p.o.). Contrary to the 3-NP effects, cilostazol largely preserved striatal dopaminergic neurons, improved motor coordination, and enhanced the immunohistochemical reaction of tyrosine hydroxylase enzyme. The anti-inflammatory effect of cilostazol was documented by the pronounced reduction of the toll like receptor-4 (TLR-4) protein expression and the inflammatory cytokine IL-6, but with a marked elevation in IL-10 striatal contents. As a consequence, cilostazol reduced IL-6 downstream signal, where it promoted the level of suppressor of cytokine signalling 3 (SOCS3), while abated the phosphorylation of Janus Kinase 2 (JAK-2) and Signal transducers and activators of transcription 3 (STAT-3). Phosphorylation of the protein kinase B/glycogen synthase kinase-3β/cAMP response element binding protein (Akt/GSK-3β/CREB) cue is another signalling pathway that was modulated by cilostazol to further signify its anti-inflammatory and antiapoptotic capacities. The latter was associated with a reduction in the caspase-3 expression assessed by immunohistochemical assay. In conclusion the present study provided a new insight into the possible mechanisms by which cilostazol possesses neuroprotective properties. These intersecting mechanisms involve the interference between TLR-4, IL-6-IL-10/JAK-2/STAT-3/SOCS-3, and Akt/GSK-3β/CREB signalling pathways.
无数神经退行性疾病都与环核苷酸信号的反常多靶点有关,加速神经元死亡。西洛他唑是一种磷酸二酯酶-3 抑制剂,对多种神经毒性模型具有神经保护作用,但尚未研究其对亨廷顿病 (HD) 的作用。因此,使用 3-硝基丙酸 (3-NP) 模型研究了其对几种信号通路的调节作用。动物连续两周腹腔注射 3-NP(10 mg/kg/天),同时或不给予西洛他唑(100 mg/kg/天,口服)。与 3-NP 的作用相反,西洛他唑大量保留纹状体多巴胺能神经元,改善运动协调,并增强酪氨酸羟化酶酶的免疫组织化学反应。西洛他唑的抗炎作用通过 Toll 样受体-4 (TLR-4) 蛋白表达和炎症细胞因子 IL-6 的显著减少以及纹状体中 IL-10 含量的显著增加得到证明。结果,西洛他唑减少了 IL-6 的下游信号,促进了细胞因子信号转导抑制因子 3 (SOCS3) 的水平,同时减弱了 Janus 激酶 2 (JAK-2) 和信号转导和转录激活因子 3 (STAT-3) 的磷酸化。蛋白激酶 B/糖原合成酶激酶-3β/cAMP 反应元件结合蛋白 (Akt/GSK-3β/CREB) 线索的磷酸化是另一种被西洛他唑调节的信号通路,进一步表明其抗炎和抗细胞凋亡能力。通过免疫组织化学测定评估, caspase-3 表达的减少与该通路有关。总之,本研究为西洛他唑具有神经保护特性的可能机制提供了新的见解。这些交叉机制涉及 TLR-4、IL-6-IL-10/JAK-2/STAT-3/SOCS-3 和 Akt/GSK-3β/CREB 信号通路之间的干扰。