Overview【1】
Phosphatidylserine (PS) is the only phospholipid that can regulate the function of key proteins in cell membranes. It is widely present in the membranes of all animals, higher plants and microorganisms. It is one of the important components of cell membranes. In addition It is also the main acidic phospholipid in the brain, accounting for about 10% to 20% of all phospholipids in the mammalian brain. It has an important regulatory effect on many cell metabolic processes. Its main function is to improve the vitality of brain cells. It has a good effect on treating brain atrophy, preventing Alzheimer’s disease, and improving the brain function of the elderly; at the same time, it can repair brain damage and treat It has a very significant effect on children with ADHD; it also has certain effects on promoting the recovery of brain fatigue, balancing emotions, and alleviating depression.
Physical and chemical properties【3】
Pure PS is a white waxy solid, soluble in most non-polar solvents containing a small amount of water, and insoluble in anhydrous acetone. It can be extracted from tissue cells by chloroform-methanol extraction. When PS is dissolved in water, most of the insoluble lipids form micelles except for a few that form a true solution. At pH 7, PS has two negative charges and one positive charge, leaving a net negative charge. Hydrolysis with a weak alkali produces metal salts of fatty acids, and the remaining parts are not hydrolyzed; hydrolysis with a strong alkali produces fatty acids, serine and glycerol phosphate. PS is easily oxidized when exposed to air, and its color gradually becomes darker, from white to yellow, and finally black. Natural PS is almost unaffected by alcohol. Saturated PS and alcohol form a staggered chain gel, while the interaction between dipalmitoyl-phosphatidylserine and 5% alcohol at room temperature can induce the formation of regular gels.
Structure【5】
PS consists of three parts: a hydrophilic glycerol skeleton as the head, and two longer hydrocarbon chain lipophilic groups as the tail. The head consists of three groups. The serine residue combines with the phosphate residue and is connected to the light group of glycerol at the C-3 position. The other two light groups of glycerol form esters with fatty acids to form the tail. Compared with fatty acids at the C-1 position of glycerol, fatty acids at the C-2 position generally have longer carbon chains and more unsaturated bonds. Phospholipid phthaloserine (PS) refers to a group of compounds rather than a single component. This is because the residues of lipid acetylphthalide residues in products extracted from raw materials from different sources vary greatly. PS is amphipathic, that is, it is both hydrophilic and lipophilic. Its structure determines its unique properties. The negatively charged head is hydrophilic (or water-soluble), and the tail composed of fatty acids is lipophilic (or fat-soluble).
Pharmacokinetics【6】
PS (BC-PS) extracted from bovine cerebral cortex is absorbed slowly after oral administration. After administration to rats with food, the plasma concentration showed an upward trend within 4 hours and reached a peak after 24 hours. Mice were orally administered 〔14C〕-BC-PS mixed with human milk, and the maximum absorption peak was 30 minutes after taking the drug.
After intravenous administration of BC-PS, plasma clearance is extremely rapid, showing a biphasic curve. The half-life of the first phase distribution curve is 5 minutes, which mainly reflects the uptake of the drug by the liver; the half-life of the second phase distribution curve is 15 minutes, which may be related to the effect of blood cells. In addition to the liver, the lungs and spleen are also important for the uptake of BC-PS. The amount of drugs entering the brain is small, mainly concentrated in the cortex, thalamus, hippocampus and other parts.
Part of the BC-PS entering the blood is dephosphorylated and converted into phospholipid phthalethanolamine, or dephthalinated to form hemolytic PS, or serine can be removed, and the latter enters the amino acid metabolism pathway. However, in plasma, fat-soluble phosphatidic acid metabolites still occupy a dominant position, mainly the original drug. The metabolic process of BC-PS in the liver and brain is similar to that in the blood. Regardless of the administration method, BC-PS is mainly excreted through the intestines, followed by the kidneys. Fat-soluble metabolites and parent drugs are mainly excreted through the intestines, while water-soluble metabolites are mainly excreted through the kidneys.
Physiological activity function【4】
1. Improving the vitality of brain cells can prevent Alzheimer’s disease, treat brain atrophy, improve and maintain the brain memory of the elderly and other diseases. As humans age, the loss of PS in the brain may cause decline or even loss of related functions, such as memory and cognitive abilities. Studies have shown that PS supplementation can stimulate the release of dopamine substances to a certain extent, increase the production of neurotransmitter acetylcholine, enhance the metabolism of glucose in the brain, reduce the secretion of hydrocortisone, and even affect the load of sterols on brain cell membranes. Metabolic activity changes the fluidity of cell membranes. It has been verified by clinical trials that the intake of PS has a good effect on Alzheimer’s Disease.
2. Reduce the secretion of stress hormones and related factors, promote brain fatigue recovery, balance unstable emotions, and also have certain effects on relieving depression. PS can regulate the hormone levels of emotional neurotransmitters in the brain, and can also suppress the levels of adrenocorticotropic hormone and cortisone in the serum. There are clinical case studies showing that PS can significantly improve symptoms such as mood disorders, abnormal behavior, anxiety and irritability in patients with depression, and no side effects occurred during the clinical period.
3. Improve the memory effect of young students, enhance their concentration when studying, and effectively improve their academic performance. Moreover, it also has a very significant effect in treating children with ADHD and other diseases. PS is an important nutrient in the nervous system. It can not only activate the activity of various enzymes in the nerve transmission process and slow down the decrease of neurotransmitters, but can also repair a variety of brain damage and remove most harmful substances. ADHD in children caused by brain malnutrition, brain damage, or genetically reduced neurotransmitter quantities are all available.�. Repair brain damage, remove harmful substances, improve attention, concentration, and improve hyperactivity by flipping to the outside of cells. Research shows that insufficient amounts of brain neurotransmitters can reduce inhibitory activity in the central nervous system, causing children to increase their movements. Phosphatidylserine is an important neurological component that can nourish brain components and activate various brain-related enzymes, thereby slowing down the occurrence of ADHD caused by insufficient amounts of brain neurotransmitters.
4. Competitive sports nutrition
PS can help maintain the functional balance of the brain (reduce its excitability when the function is hyperactive, and excite it when the function is suppressed), eliminating the harm of neurological fatigue; PS can inhibit ACTH and cortisol produced by exercise, and increase testosterone/ Cortisol ratio reduces the loss of amino acids in muscle tissue; PS can prevent physiological decline caused by exercise stress and overload training; PS can protect muscle membranes and avoid phospholipase damage due to muscle damage; PS can increase the transfer of glucose to muscle cells. Transmission efficiency protects nutrients from being lost from muscle cells; PS can speed up physical recovery and prevent muscle pain; PS can improve athletes’ psychological conditions during training and competition, relieve mental stress, and regulate competition emotions.
5. Treatment of depression
Monoamine neurotransmitters such as norepinephrine and 5-hydroxytryptamine can transmit excitement, so the decrease or lack of monoamines will inhibit the transmission of excitement and cause depression. Before and after taking PS, the concentration of norepinephrine and 5-hydroxytryptamine in the plasma of patients increased, and the patients’ depression level was reduced by an average of 70%, and symptoms such as mood disorders, abnormal behavior, anxiety, and irritability were significantly improved.
6. Cofactors for activating enzymes
Many key proteins in signal transduction require PS as a cofactor for enzymes to achieve optimal activity. The activation of protein kinase C (PKC) is a classic example. Before activation, the PKC proenzyme is located in the cytoplasm and is in a passivated state. It is transferred from the cytoplasm to the cell membrane under the action of diacylglycerol (DAG) and becomes a “to-be-activated state”. After enzyme catalysis, PKC forms an activated PKC?PS?DAG?Ca2+ complex with Ca2+, PS, and DAG. Activated protease kinase C can phosphorylate serine and threonine residues, thereby affecting biological information transmission.
Main reference materials
[1] Yang Weidong, Ma Yaning. Preparation and research progress of phosphatidylserine[J]. Inner Mongolia Agricultural Science and Technology, 2009(04):83-84+90.
[2] Rao Xue’e, Lin Weiling. Research progress on the application of phosphatidylserine[J]. Strait Pharmacy, 2015, 27(11):9-11.
[3] Zhou Fang, Li Hongjun, Yang Fuxi, Zou Zhongyi, Meng Lingjun, Mei Linlin. Research progress of phosphatidylserine [J]. Food Industry Science and Technology, 2008(05):297-300.
[4]Hu Fei. Research on the preparation of phospholipase D and its catalytic synthesis of phosphatidylserine [D]. Hefei University of Technology, 2013.
[5] Yang Zhibiao. Research on the preparation and catalytic synthesis of phosphatidylserine by phospholipase D [D]. Northwest University, 2008.
