Citicoline is a single nucleotide composed of nucleic acid
Citicoline is a single nucleotide composed of nucleic acid, cytosine, pyrophosphate and choline, which is mainly used in clinical treatment of a variety of neurodegenerative diseases, such as Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis and so on. Studies have also shown that citicoline can increase the brain's uptake of dopamine and glutamate, thereby improving cognitive performance. Ciphocholine can also reduce the release of free fatty acids and restore the activity of mitochondrial ATPase and cell membrane Na+/K+ ATPase, thus alleviating brain injury. However, the pathophysiological mechanisms of neurodegenerative diseases are complex and involve cholinergic deficiency, glutamate excitotoxicity, neuroinflammation, immune dysregulation, decreased glucose metabolism, and breakdown of the blood-brain barrier.
Citicoline can stabilize the cell membrane by stimulating S-adenosine-L-methionine, increase the dendrite complexity and spinous process density of motor neuron structure, improve the plasticity of nerves in non-damaged areas, and promote functional recovery.
Citicoline can reduce the level of water-soluble lecithin phosphate by upregating choline phosphate cytidylytransferase (CCT) and inhibit the activity of secretory phospholipase A2(PLA2) or inhibit the activation of PLA2 by inhibiting TNF-a/IL-1b to reduce the loss of phospholipids, thereby increasing the synthesis of phospholipid and repairing nerve membranes.
Citicoline can also increase the expression of anti-apoptotic factors such as Bcl-2 and inhibit glutamate release to reduce cytotoxicity.
Ciphocholine promotes rapid repair of damaged cell surfaces and mitochondrial membranes, maintains cell tightness and biological function, and reduces free fatty acid release, thereby reducing toxic oxygenated metabolites and free radical production.
Citicoline can increase vasopressin and plasma adrenotropin levels, and stimulate the release of growth hormone, thyrotropin and luteinizing hormone.
There are many preparation methods of citicoline sodium, mainly three ways.
One is microbial fermentation. This method has some problems such as low product concentration and unstable yield.
One is organic chemical synthesis. There are some problems in this method, such as the product is difficult to separate from shrinkage mixture, not suitable for medicinal use, low reaction conversion rate, many by-products, high cost and serious environmental pollution.
There is also an enzymatic synthesis method, such as the use of beer yeast mud and other microorganisms for biosynthesis. The free brewer's yeast mud cells were used for enzymatic synthesis. The process was simple, the conversion rate was high and the cost was low. The production process of citicoline sodium synthesized by enzymatic synthesis can be divided into two parts: enzymatic synthesis process and extraction and purification process.
Taken orally, it is rapidly absorbed, hydrolyzed in the intestine and liver to choline and cytosine, which enter the bloodstream, cross the blood-brain barrier, and recombine into citicoline in the central nervous system, where 80% of phospholipid synthesis is affected by citicoline concentration in the body.
In addition, citicoline is converted to acetylcholine in the central nervous system and oxidized to betaine in the kidneys and liver. The water solubility of citicoline is good, the bioavailability is as high as 90%, and only less than 1% is excreted in the stool after oral administration. There are 2 peaks of absorption in plasma, 1 hour and 24 hours after ingestion.
In rat models, levels of radiolabelled citicoline increased steadily in the brain 10 hours after ingestion and were widely distributed in the white and gray matter of the brain. High concentrations remain at 48 hours, and its elimination is very slow, with only a small amount excreted daily through urine, feces, and respiration. Exogenous ingestion of citicoline can promote rapid repair of damaged cell membranes and mitochondria, maintain cell integrity and biological performance, and inhibit apoptosis and death.