Department of Experimental Pharmacology, Mossakowski Medical Research Centre, Polish Academy of Sciences, 5 Pawinskiego Street, 02-106 Warsaw, Poland.
Nutrients. 2019 Jul 12;11(7):1569. doi: 10.3390/nu11071569.
Medicines containing citicoline (cytidine-diphosphocholine) as an active principle have been marketed since the 1970s as nootropic and psychostimulant drugs available on prescription. Recently, the inner salt variant of this substance was pronounced a food ingredient in the major world markets. However, in the EU no nutrition or health claim has been authorized for use in commercial communications concerning its properties. Citicoline is considered a dietetic source of choline and cytidine. Cytidine does not have any health claim authorized either, but there are claims authorized for choline, concerning its contribution to normal lipid metabolism, maintenance of normal liver function, and normal homocysteine metabolism. The applicability of these claims to citicoline is discussed, leading to the conclusion that the issue is not a trivial one. Intriguing data, showing that on a molar mass basis citicoline is significantly less toxic than choline, are also analyzed. It is hypothesized that, compared to choline moiety in other dietary sources such as phosphatidylcholine, choline in citicoline is less prone to conversion to trimethylamine (TMA) and its putative atherogenic N-oxide (TMAO). Epidemiological studies have suggested that choline supplementation may improve cognitive performance, and for this application citicoline may be safer and more efficacious.
自 20 世纪 70 年代以来，含有胞磷胆碱（胞嘧啶二磷酸胆碱）作为活性成分的药物已作为处方中的益智药和精神兴奋剂药物上市。最近，这种物质的内盐变体在世界主要市场被宣布为食品成分。然而，在欧盟，其特性的商业宣传中没有被授权使用任何营养或健康声明。胞磷胆碱被认为是胆碱和胞嘧啶的膳食来源。胞嘧啶也没有任何被授权的健康声明，但有一些关于胆碱的声明被授权，涉及到它对正常脂质代谢、维持正常肝功能和正常同型半胱氨酸代谢的贡献。本文讨论了这些声明对胞磷胆碱的适用性，得出的结论是，这个问题不是微不足道的。还分析了令人关注的数据，这些数据表明，按摩尔质量计算，胞磷胆碱的毒性明显低于胆碱。据推测，与其他膳食来源（如磷脂酰胆碱）中的胆碱部分相比，胞磷胆碱中的胆碱更不容易转化为三甲胺（TMA）及其潜在的动脉粥样硬化 N-氧化物（TMAO）。流行病学研究表明，胆碱补充剂可能改善认知表现，而对于这种应用，胞磷胆碱可能更安全、更有效。
