甘油磷酰胆碱的分析、制备及纯化研究进展

Advances in analysis,preparation and purification of glycerophosphocholine

甘油磷酰胆碱(GPC)作为重要神经递质乙酰胆碱的生物合成前体,能够促进乙酰胆碱在脑部的合成,增强人体的记忆力和认知能力,预防老年痴呆类疾病,已引起医药界的高度关注。为进一步促进GPC相关产品的研究与应用,本文重点介绍了近几年GPC的分析、制备及纯化技术的研究进展,并比较了不同方法的优缺点。指出高效液相色谱法(HPLC)是分析GPC的主流方法,但没有一种检测器能检测到所有关键的杂质,需要多种检测器联用才可判断GPC的质量是否达到要求。全化学合成和水解卵磷脂(PC)是制备GPC的主要方法。文中指出全化学合成法具有收率高、产品纯度高和制备工艺完善的优点,但起始原料昂贵,全化学合成的GPC中会残留基因毒性杂质,严重影响产品品质。水解PC法能够制备出食品级GPC,所得产品无毒无害,但水解法收率低,产品纯度低,纯化难度大,难以规模化生产。结晶法和柱色谱法是纯化GPC粗品的主要方法。结晶法得到的产品纯度高,但收率低,生产成本高。柱色谱法能除去大量杂质,除杂效果好,但生产过程中会产生大量“三废”,纯化周期长。文中分析表明,HPLC和多种检测器联用是定量分析GPC及其相关杂质的最有效方法,水解PC以制备食品级GPC是如今的研究热点,开发出高效的纯化技术是工业化生产GPC的关键和难点。

Glycerophosphocholine(GPC),as the biosynthetic precursor of the important neurotransmitter acetylcholine,can promote the synthesis of acetylcholine in the brain,enhance the human memory and cognitive ability,and prevent Alzheimer’s disease.In order to further promote the research and application of GPC-related products,this article focuses on the research progress of its analysis,preparation and purification technology in recent years.The advantages and disadvantages of different methods were compared.High performance liquid chromatography(HPLC)is the mainstream method for analyzing GPC,but no detector can detect all key impurities alone.It requires a combination of multiple detectors to determine whether the quality of GPC meets the requirements.Full chemical synthesis and hydrolysis of lecithin(PC)are the main methods for preparing GPC.Full chemical synthesis has the advantages of high yield,high product purity and perfect preparation technology,but the starting materials are expensive,and even worse,some impurities in the fully chemically synthesized GPC are genotoxic and seriously affect quality.Hydrolysis of PC can prepare food-grade GPC,and the product is non-toxic and harmless,but the hydrolysis method has a low yield,low product purity,high purification difficulty,and difficulty in large-scale production.Crystallization and column chromatography are the main methods for purifying crude GPC products.The product obtained by crystallization has high purity,but low recovery and high production costs.Column chromatography can remove a large amount of impurities and has a good impurity removal effect,but a large amount of wastes will be produced during the process,and the purification cycle will be long.Analysis shows that the combination of HPLC and multiple detectors is the most effective method for the quantitative analysis of GPC and its related impurities.Hydrolysis of PC to prepare food-grade GPC is now a research hotspot.The development of efficient purification technology is the key point in industrial production of GPC.