Faculty of Medicine and Pharmacy, University of Oradea, Oradea, Romania.
Department of Pharmacology, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa, Egypt.
FASEB J. 2024 Sep 15;38(17):e70030. doi: 10.1096/fj.202400823R.
Citicoline, a compound produced naturally in small amounts in the human body, assumes a pivotal role in phosphatidylcholine synthesis, a dynamic constituent of membranes of neurons. Across diverse models of brain injury and neurodegeneration, citicoline has demonstrated its potential through neuroprotective and anti-inflammatory effects. This review aims to elucidate citicoline's anti-inflammatory mechanism and its clinical implications in conditions such as ischemic stroke, head trauma, glaucoma, and age-associated memory impairment. Citicoline's anti-inflammatory prowess is rooted in its ability to stabilize cellular membranes, thereby curbing the excessive release of glutamate-a pro-inflammatory neurotransmitter. Moreover, it actively diminishes free radicals and inflammatory cytokines productions, which could otherwise harm neurons and incite neuroinflammation. It also exhibits the potential to modulate microglia activity, the brain's resident immune cells, and hinder the activation of NF-κB, a transcription factor governing inflammatory genes. Clinical trials have subjected citicoline to rigorous scrutiny in patients grappling with acute ischemic stroke, head trauma, glaucoma, and age-related memory impairment. While findings from these trials are mixed, numerous studies suggest that citicoline could confer improvements in neurological function, disability reduction, expedited recovery, and cognitive decline prevention within these cohorts. Additionally, citicoline boasts a favorable safety profile and high tolerability. In summary, citicoline stands as a promising agent, wielding both neuroprotective and anti-inflammatory potential across a spectrum of neurological conditions. However, further research is imperative to delineate the optimal dosage, treatment duration, and underlying mechanisms. Moreover, identifying specific patient subgroups most likely to reap the benefits of citicoline as a new therapy remains a critical avenue for exploration.
胞磷胆碱是一种在人体内少量自然产生的化合物，在磷脂酰胆碱的合成中起着关键作用，磷脂酰胆碱是神经元膜的动态组成部分。在各种脑损伤和神经退行性变模型中，胞磷胆碱通过神经保护和抗炎作用显示出其潜力。本综述旨在阐明胞磷胆碱的抗炎机制及其在缺血性中风、头部创伤、青光眼和与年龄相关的记忆障碍等疾病中的临床意义。胞磷胆碱的抗炎作用源于其稳定细胞膜的能力，从而抑制谷氨酸（一种促炎神经递质）的过度释放。此外，它还积极减少自由基和炎症细胞因子的产生，否则这些物质会损害神经元并引发神经炎症。它还具有调节小胶质细胞活性的潜力，小胶质细胞是大脑中的常驻免疫细胞，并阻止 NF-κB 的激活，NF-κB 是调节炎症基因的转录因子。临床试验对胞磷胆碱在急性缺血性中风、头部创伤、青光眼和与年龄相关的记忆障碍患者中的应用进行了严格的检查。虽然这些试验的结果喜忧参半，但许多研究表明，胞磷胆碱可能会改善这些患者的神经功能、减少残疾、加快康复和预防认知能力下降。此外，胞磷胆碱具有良好的安全性和耐受性。总之，胞磷胆碱作为一种有前途的药物，在一系列神经疾病中具有神经保护和抗炎作用。然而，为了阐明最佳剂量、治疗持续时间和潜在机制，还需要进一步的研究。此外，确定最有可能从胞磷胆碱作为一种新疗法中获益的特定患者亚组仍然是一个关键的探索领域。
