Background and overview[1][2]
Glyceryl phosphocholine (GPC) is a water-soluble small molecule substance that exists normally in the human body and is the biosynthetic precursor of the important neurotransmitter acetylcholine. The most important role of GPC is that the choline it produces is a water-soluble B vitamin, which plays an important role in the brain and nervous system. Research shows that GPC plays an important role in the production of certain hormones and neurotransmitters such as acetylcholine and human growth hormone. This supports the function of the brain and nervous system.
In the body, the most important physiological function of GPC is to cross the blood-brain barrier and provide necessary choline for the synthesis of acetylcholine and phospholipid (PC). Acetylcholine is an important neurotransmitter in the central nervous system and helps the brain complete Learning, memory and cognitive activities, and can control light sleep and motor activity. Taking GPC directly can promote the formation of phosphoinositides in the brain and increase the synthesis of phospholipids in the brain, providing more phospholipid compounds for signal transmission in the central nervous system, increasing the synthesis of phosphatidylcholine in the body, and helping Resist cell membrane damage and decline in peripheral nerve function caused by age. GPC was first launched in Italy. In recent years, GPC has attracted more and more attention in our country.
Physical and chemical properties[1]
The molecular formula of GPC is C8H20NO6P, which is miscible with water, soluble in methanol and ethanol, insoluble in chloroform, ether, oil, etc., and has no characteristic absorption under ultraviolet and visible light. GPC content determination methods include high performance liquid chromatography (equipped with evaporative light scattering detector or refractive index detector) and digestion phosphorus determination method. Commonly used other methods include TLC method (the developing solvent is: V(CH2Cl2): V(H2O): V(triethylamine) = 35: 60: 5 or V (CHCl3): V (CH3OH): V (CH3COOH): V(CH3CH2CHO): V(H2O) = (45: 25: 7: 4: 2)), chemical identification method (prepare 5% GPC test solution, add a certain amount of sodium hydroxide solution and potassium permanganate When the solution is heated, an odor similar to trimethylamine is produced. This gas turns moist red litmus paper blue) and infrared absorption spectrum identification method. The structure of GPC was analyzed using nuclear magnetic resonance spectroscopy, and the detection data of GPC’s H spectrum, C spectrum, DEPTpvc composite stabilizer spectrum, HSQC spectrum, COSY spectrum, HMBC spectrum and P spectrum were obtained. The structure and chemical shift assignment of GPC were obtained. picture.
Security[2]
Glycerylphosphocholine is an endogenous substance in the human body. In 2009, the magazine “Mutation Research” published 480 tests for the carcinogenicity and genotoxicity of sold drugs. Glycerylphosphocholine was listed in “Not retrieved Data for the “Pharmaceuticals” category. It is not reproductively toxic, genotoxic or carcinogenic. During preclinical trials on more than 2,000 patients, it was found that more than 40 cases (2.14%) of adverse reactions occurred in total. The main clinical adverse symptoms of this product include: burning sensation in the stomach, excitement, insomnia, headache and nausea; in some cases, adverse reactions occurred. Patients experienced symptoms such as vomiting, diarrhea, confusion, dizziness, and cataplexy; but overall, the safety of glycerophosphocholine is good.
Tolerance[2]
According to clinical trials in multiple centers, glycerophosphocholine has been used to treat patients with Alzheimer’s disease and multiple cerebral infarct dementia. The course of treatment for Alzheimer’s disease with glycerophosphocholine is 180 days, 0.4 g each time, and the medicine is taken three times a day. The results show that glyceryl phosphocholine has a significant effect in treating Alzheimer’s disease, and patients tolerate glyceryl phosphocholine well; research on the use of glyceryl phosphocholine in the treatment of multiple cerebral infarction dementia has been conducted on 120 patients. A trial was conducted on several mildly ill patients with multiple cerebral infarction dementia. The course of treatment was 80 days, and 1 g of glycerophosphocholine was injected intramuscularly each time.
The results show that glycerophosphocholine has a significant effect on multiple cerebral infarct dementia and is well tolerated by patients. Glyceryl phosphocholine is used to treat cerebral ischemic stroke, mild multiple cerebral infarction type dementia, and mild Alzheimer’s disease without any major local or systemic adverse reactions. There were no clinically or statistically significant changes in vital signs (diastolic blood pressure, systolic blood pressure, and heart rate) nor in any laboratory parameters.Finally, it is concentrated and purified on a Sephadex column to obtain high-purity GPC.
4) Phospholipase hydrolysis method
GPC is prepared by enzymatic hydrolysis, which belongs to the field of lipid development and application technology. It uses phospholipase A1 to hydrolyze soybean powder phospholipids in an aqueous system to prepare GPC, and the GPC yield reaches 95%. Lipozyme IM and phospholipase A2 were used to jointly catalyze the hydrolysis of phosphatidylcholine in a microemulsion system for 48 h to prepare GPC, with a maximum yield of 94%. This method uses dual enzyme catalysis, which is costly and requires a long reaction time; Utilize Phospholipase A1 catalyzed the hydrolysis of PC80, and the yield of product GPC was 86% after 24 h. An adsorption method is used to prepare immobilized phospholipase A1 and catalyze phosphatidylcholine to prepare GPC. This method has a GPC yield of up to 85%. This method improves the storage stability of phospholipase A1, simplifies the separation and purification process, and realizes the enzyme’s Reuse multiple times.
Main reference materials
[1] Research progress in the preparation of glycerophosphocholine
[2] Research progress in preparation and purification technology of glycerophosphocholine
