Choline bitartrate (vitamin B4): where it is found, properties, benefits and harms

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Vitamin B4 or choline is a water-soluble vitamin that was isolated from bile. That is why it has such a name - from the Greek “cholis” - bile. Choline improves metabolism in nervous tissue, prevents the formation of gallstones, normalizes fat metabolism and helps reduce weight. The peculiarity of the vitamin-like substance B4 is the ability to be produced in the body. Thanks to this, in most cases, human internal organs and tissues do not “experience” a lack of useful compounds.

If you have such an opportunity, it is best to take vitamins by injection for medicinal purposes, since their bioavailability or absorption by the body is higher when administered by injection.

Content

• 1 Choline (phosphatidylcholine, vitamin B4) 1.1 Biological effects of choline
• 1.2 Doses and regimen

For what diseases is it recommended to take

Indications for the use of choline are:

• nervous system disorders (including Parkinson's and Alzheimer's diseases),
• mental disorders,
• cardiovascular pathologies,
• atherosclerosis,
• anemia,
• arterial hypertension,
• traumatic brain injuries,
• memory impairment,
• fatty liver - steatosis,
• viral hepatitis,
• cholelithiasis,
• bronchial asthma,
• allergic rhinitis,
• overweight,
• alcoholism.

Vitamin B4 and its derivatives are widely used throughout the world as natural nootropics.

Choline (phosphatidylcholine, vitamin B4)[edit | edit code]

Vitamin B4 content in some foods
Choline

(from the Greek kholy - bile) - belongs to the B vitamins (vitamin B4 or Bp), although animals and microorganisms are able to synthesize it. Choline salts bitartrate or phosphatidylcholine are often used in sports nutrition, although they do not provide benefits. Choline, phosphatidylcholine, and lecithin are completely interchangeable. Gliatilin (alpha-glycerylphosphorylcholine) also provides high bioavailability of choline.

Choline in food.

Its content is especially high in egg yolk (in the form of lecithin), brain, liver, kidneys and heart muscle. Found in cabbage, spinach, soybeans. During heat treatment it is partially destroyed.

Biological effects of choline[edit | edit code]

Choline is widely used in bodybuilding and other sports, as its many effects contribute to improved performance.

• In the body, the most important neurotransmitter-transmitter of nerve impulses, acetylcholine, is synthesized from choline.
• It is an important substrate for the nervous system and improves memory.
• Reduces homocysteine ​​levels and protects the heart.
• Part of phospholipids (for example, lecithin).
• Participates in the synthesis of the amino acid methionine, where it is a supplier of methyl groups.
• Affects carbohydrate metabolism by regulating insulin levels in the body.
• Choline is a hepatoprotector and can therefore be used during a steroid cycle. As a donor of methyl groups, it participates in detoxification processes (detoxification of toxins).

Doses and regimen[edit | edit code]

Choline deficiency practically does not occur, since it comes in sufficient quantities from food and is produced by the body independently. However, during bodybuilding there is an increased need for choline, especially when taking steroids and other drugs that have a toxic effect on the liver. It should be noted that one chicken egg contains approximately 150 mg of choline (lecithin), so eating several eggs with yolks each day can completely eliminate the need for additional supplementation.

Under normal conditions, it is recommended to take approximately 0.5 g of choline; in bodybuilding conditions, the optimal doses increase due to the increased needs of the body to 1-3 g daily.

The maximum dose of choline is 3.5 g. In case of overdose (more than 10 g), the body begins to emit a fishy odor, nausea, depression, decreased blood pressure, sweating, increased salivation and indigestion may occur.

Vitamin B4 deficiency

With a lack of vitamin B4, the following occurs:

• noise in ears;
• apathy, worsening mood, irritability;
• sleep disturbance;
• headaches, memory loss;
• obesity and rapid weight gain.

A decrease in vitamin B4 is caused by poor nutrition, an unbalanced diet, frequent overwork, alcohol, drugs, antibiotics, and severe stress.

If you feel a lack of choline, include these three dishes in your diet:

• beef liver stroganoff;
• egg omelet with tomatoes and parsley;
• pike cutlets.

Author: Telegina Natalya Dmitrievna

Therapist with 25 years of experience

>

Side effects[edit | edit code]

It is known that choline and betaine can be metabolized in the intestine by bacteria to form trimethylamine gas, which resembles the smell of missing fish.[1] Trimethylamine is absorbed through the intestinal wall and metabolized by monooxygenase (FMO3) to form trimethylamine N-oxide.[2] Experiments have shown that adding choline to the diet of animals leads to the formation of atherosclerotic plaques, and the rate of the process directly depended on the concentration of trimethylamine N-oxide.[3] This study also confirmed that destroying the gut microflora with antibiotics eliminates this phenomenon.

Thus, choline itself has an antiatherogenic effect, but at the same time its metabolite can lead to the opposite result. These are only theoretical data that are not confirmed in humans.

Research[edit | edit code]

Posted by Dietitian Joel Fuhrman

Eggs are rich in choline, which, like cholesterol, is present in high concentrations in prostate cancer cells. A 2011 study that followed 27,607 men from 1994 to 2008 found that those who ate two and a half or more eggs per week had an 81% increased risk of prostate cancer compared to men who ate less than half an egg. in Week. A prospective study of health care workers observing egg consumption in 47,896 men confirmed these findings. Men whose choline levels were highest had a 70% increased risk of prostate cancer.

Other studies have found that choline is involved in the growth and development of cancer. For example, in the highly respected US Nurses' Health Study, increased choline was associated with an increased risk of developing colorectal adenoma. A 2012 study identified a link between egg yolk consumption and carotid artery platelet counts in more than twelve hundred people. Platelet development in the blood vessels increased in proportion to the amount of egg yolks consumed. People with the highest egg consumption performed as well as if the study participants were smokers. People who ate the most egg yolks (an average of about four per week) showed two-thirds of the plaque formation in their carotid arteries, which is comparable to smokers who smoked a pack of cigarettes a day for forty years!

One after another, studies continue to show that egg yolks are not as harmless as everyone used to think. In fact, they pose a particular risk for people who are overweight, prediabetic, or diabetic.

What functions does it perform?

Vitamin B4 (choline alfoscerate and choline bitartrate) is involved in most vital processes occurring in the body. The main ones:

• Cell formation. Choline is necessary for the synthesis of fats, which maintain the structural integrity of membranes.
• Signal transmission. Vitamin B4 is involved in the production of a component that ensures intercellular communication.
• DNA formation. Choline plays an important role in this process, along with folate (folic acid compounds) and vitamin B12.
• Lipid metabolism. Vitamin B4 is necessary for the production of a substance that prevents the accumulation of fats and promotes the elimination of cholesterol.
• Respiratory function. Choline is involved in the formation of surfactant, a component necessary for normal lung function.
• Activity of the nervous system. Vitamin B4 serves as a material for the synthesis of an important neurotransmitter - acetylcholine. This substance ensures the performance of such functions as thinking, cardiac activity, speech apparatus, muscle movement, etc.

For the normal functioning of all organs and systems, it is recommended to include foods rich in choline in the menu, as well as use dietary supplements based on it (see below).

Historical background[edit | edit code]

Source:
Clinical Pharmacology by Goodman and Gilman, Volume 4
.
Editor
: Professor A.G.
Gilman Ed.
: Practice, 2006.

In 1932, Best et al. found fatty liver degeneration in insulin-treated dogs with their pancreas removed, which could be prevented by adding lecithin (from raw egg yolk) or bovine pancreas to the food. The substance responsible for this effect turned out to be choline. These data gave impetus to widespread study of the role of lipotropic substances, especially choline, in animal nutrition. The functions of choline in the body are associated not only with lipid metabolism, but also with other important processes.

Why do we need choline?

Choline ensures normal metabolism, optimal functioning of the intestines and other internal organs. Without vitamin B4, complete transmission of nerve impulses is impossible.

In addition, choline takes part in a number of important physiological processes:

• Renewal of the cellular structure of tissues after toxic injuries from both toxic substances and pharmaceuticals and drugs.
• Control of metabolism, fat excretion, reduction of cholesterol parameters.
• Prevents the destruction of nerve fiber cells.
• Activates the regeneration of the liver structure.
• Suppresses the formation of intraorgan stones.
• Reduces fatty acid levels.
• Participates in the production of methionine.
• Has a beneficial effect on myocardial function.
• Strengthens pancreatic cells responsible for producing insulin.
• Stimulates reproductive function.
• It has a beneficial effect on the condition of patients with diabetes.

[Video] Medical consultant of NPTsRIZ, geneticist, Ph.D. Irina Yuryevna Saburova talks about the mechanisms of action of choline:

Pharmacological action[edit | edit code]

While having the same effects as acetylcholine, choline is much less active. Even 10 g of choline when taken orally does not have a clear effect. Physiological functions. Choline performs several functions in the body. It is an important component of phospholipids, promotes the mobilization of fatty acids in the liver (lipotropic effect), serves as a donor of methyl groups and is necessary for the formation of the mediator acetylcholine (Chapter 6) and platelet activating factor (Chapter 26).

Phospholipid component[edit | edit code]

Choline is part of the main phospholipid - lecithin, plasmalogens (present in large quantities in mitochondria) and sphingomyelins (which the brain is especially rich in). Thus, choline serves as an essential structural component of many biological membranes and plasma lipoproteins.

Lipotropic action[edit | edit code]

As already mentioned, the important role of choline as a dietary component was first noticed in connection with its ability to reduce fat content in the liver of dogs with experimental diabetes mellitus. Substances that stimulate the removal of excess fat from the liver are called lipotropic. These include choline, inositol, methionine, vitamin B 12 and folic acid. Some of them apparently serve as donors of methyl groups in the synthesis of choline. As a result, the formation of lipid components of plasma lipoproteins occurs and the transport of fat from the liver is accelerated. A methyl group donor, choline can serve as a donor of (methyl)methyl groups necessary for the synthesis of other compounds. First, betaine is formed from choline, which is a direct donor of the methyl group. The methyl group can then be transferred to homocysteine, resulting in the formation of methionine. The role of vitamin B12 (cyanocobalamin) and folic acid in the metabolism of single-carbon compounds is discussed in Chap. 54.

Formation of acetylcholine[edit | edit code]

Acetylcholine is synthesized from choline and acetyl-CoA by choline acetyltransferase and broken down by AChE (Chapter 6). In the endothelium of the brain capillaries there is a system of facilitated diffusion of choline in both directions, and the amount of choline entering the central nervous system depends on its concentration in the plasma. When choline chloride is administered to rats, not only the concentration of choline in the plasma increases, but also the concentrations of choline and acetylcholine in the brain. These data may help in the treatment of diseases in which acetylcholine synthesis is reduced (see below). Synthesis of platelet activating factor. This factor is formed from choline-containing membrane phospholipids, in which at position 1 of the glycerol residue there is an alkyl ester instead of a fatty acid ester. Hormone-sensitive phospholipase A2 acts on the phospholipid, forming 1-O-alkyllisophosphatidylcholine. Under the action of a specific acetyl transferase, which catalyzes the transfer of the acetyl group from acetyl-CoA to position 2 of this intermediate product, platelet activating factor is formed. It plays an important role in inflammatory reactions and other processes (Chapter 26). Deficiency symptoms. Choline deficiency in animals is accompanied by fatty degeneration and cirrhosis of the liver, an increased risk of hepatic cell cancer, hemorrhagic kidney damage and impaired coordination of movements. Fortunately, none of these manifestations of choline deficiency have been observed in humans.

What products contain

Choline is found in plant and animal foods. The tables show the main sources of vitamin B4.

Food of animal origin:

Plant food:

Choline and its derivatives - salts and esters - are used as very useful food additives.

Need[edit | edit code]

Tissues obtain choline from both exogenous (dietary) and endogenous (metabolic) sources. In the body, choline is synthesized by transferring the methyl group of methionine to ethanolamine or through a series of reactions requiring the presence of vitamin B12 and folic acid as cofactors (Chapter 54). Thus, to prevent fatty liver disease, it is necessary to consume sufficient amounts of methyl group donors in food. Large amounts of choline also have a therapeutic effect in some diseases of the nervous system, which is probably due to the stimulation of acetylcholine synthesis. However, none of the functions of choline gives grounds to classify it as a vitamin. It is not a cofactor of any known enzymatic reactions and produces therapeutic effects in gram doses far greater than the effective doses of any vitamin.

The daily requirement for choline is 550 mg for men and 425 mg for women (Table XIII.2). Americans on average consume 400-900 mg of choline per day as part of lecithin. Thus, it is difficult to imagine a diet lacking in choline. However, when methionine and folic acid intakes are low, choline deficiency can lead to biochemical signs of liver dysfunction, and therefore choline can be considered an essential dietary component in this situation (Jacob et al., 1999). The Committee on Nutrition of the American Academy of Pediatrics (1993) recommends adding choline to infant formula in an amount of at least 7 mg/100 kcal, which approximately corresponds to its concentration in human milk (9 ± 2 mg%).

Food sources[edit | edit code]

Choline is found in egg yolk, liver and peanuts (mainly in lecithin).

Interaction with other elements

Vitamin B4 is better accepted by the body in combination with such active ingredients as:

• lecithin,
• folic acid,
• B vitamins.

In turn, choline promotes better absorption of vitamins A, D, E, K.

The amount of the substance in the body may decrease:

• with excessive alcohol consumption,

• as a result of taking antibacterial drugs,
• when using steroid hormones.

Absorption, exchange and excretion[edit | edit code]

Choline is absorbed in the intestine either as such or as part of lecithin. In the intestinal mucosa, lecithin is hydrolyzed to form glycerophosphocholine, which enters the liver (where it releases choline) or, through the lymphatic vessels, into the systemic circulation. Free choline, especially when taken in large doses, is not completely absorbed, and intestinal bacteria convert it into trimethylamine. Since this substance gives stool a strong rotten fish smell, it is better to use lecithin as a source of choline.

Physicochemical characteristics

Chemical formula of the substance: C5H14NOX, or [ (CH3)3N+CH2CH2OH ] X−.

The structural formula of choline is presented below:

Although choline chloride is used for medical purposes, its structural formula is:

Another name for vitamin B4 is trimethylethanolamine. It is a colorless substance with a strong odor. It is highly soluble in water, therefore it is classified as a water-soluble compound. Vitamin B4 destruction occurs at temperatures above 180C. Reacts with many acids to form salts.

This video explains the properties of choline better:

No. 191. Organic chemistry. Topic 28. Vitamins. Part 9. Vitamin B4

Application[edit | edit code]

The effectiveness of choline in fatty degeneration and cirrhosis of the liver (usually alcohol-related) has not been proven. Because choline can be precursed by other methyl group donors, a well-balanced diet may alleviate symptoms of liver damage as much as choline itself. Fatty liver degeneration often develops in patients on total parenteral nutrition. Since parenteral nutrition solutions usually do not contain choline, choline deficiency may be the cause of liver pathology in such cases.

For diseases of the nervous system, which may be a consequence of decreased acetylcholine synthesis, it has been proposed to use large doses of choline or a related compound, citicoline (choline ester CDP). However, in none of these diseases (late neuroleptic hyperkinesis, Huntingon's disease, Gilles de la Tourette's syndrome, ataxia due to hereditary vitamin E deficiency, Alzheimer's disease) has the therapeutic effect of choline been reliably proven (Chapters 20 and 22). Recent controlled clinical trials suggest benefits for citicoline in stroke (Clark et al., 1997) and age-related verbal memory loss (Spiers et al., 1996), but these data require confirmation.

Daily requirement

The data presented will be approximate only. To date, there is no reliable data on the amount of the required substance. A special analysis for the content of microelements helps determine the level of vitamin B 4 (choline) in the body.

TOP 3 vitamins for children with choline and omega-3

The product rating was compiled based on the cost of 1 serving and composition.

№3 SmartyPants, Kids Complete, Multivitamin, Cherry Berry

SmartyPants, Children's Multivitamin, Cherry, 120 Gummies

★★★★★

RUB 1,458

More details

Price for 1 serving – 9 rubles. 78 kop.

Brief information:

• country of origin – USA;
• package volume – 120 chewable tablets;
• daily dosage – 4 pcs.

The product contains vitamins, minerals and fish oil. The tablets have white grape, mixed berry and cherry flavors. Does not contain GMOs.

Pros:

• stimulates brain function.

Minuses:

• may trigger the development of allergies.

No. 2 Chewable lozenges Univit Kids Omega 3 with choline

Univit Kids Omega 3 with choline, chewable lozenges n30

from 465 ₽

More details

The cost of 1 serving is 14 rubles. 77 kop.

General description:

• Country: Germany;
• packaging volume – 30 lozenges;
• daily norm - for children under 7 years old - 1 pc., 7-14 years old - 2-3 pcs.

This choline and omega acid supplement is used to strengthen the immune system and improve intelligence. Lozenges are produced in the shape of dolphins. The manufacturer recommends giving them to the child during or after meals.

Pros:

• the drug strengthens the immune system;
• helps the child concentrate.

Minuses:

• emits an unpleasant odor.

№1 SmartyPants, Kids Complete

SmartyPants, Kids Formula, Strawberry Banana Orange Lemon Flavors, 120 Chewable Tablets

★★★★★

RUB 1,458

More details

Price for 1 serving – 9 rubles. 78 kop.

General information:

• country of origin – USA;
• package volume – 120 gummies;
• daily norm – 4 pcs.

Kids Complete chewable vitamins with choline can be given to children from the age of three. They contain microelements that are necessary for a growing body, and purified fish oil.

Pros:

• have the taste of orange, lemon, strawberry, banana;
• do not cause allergic reactions.

Minuses:

• No.