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Phosphatidylcholine

Phosphatidylcholine SLOW PUSH (1 gram in 10ml) with Glutathione SLOW PUSH $175 (1 gram)

Phosphatidylcholine (derived from lecithin), a primary dietary source of choline, is composed of a phosphate group, 2 fatty acids, and choline. The composition of essential fatty acids in phosphatidylcholine determines its value in promoting health. When phosphatidylcholine is ingested, most of it is broken down into choline, glycerol free fatty acids, and the phosphate group, rather than being incorporated intact into cellular membranes.

 

• Although choline can be manufactured in humans from either methionine or serine, it has recently been designated an essential nutrient.

 

Function


• Choline is required for the proper metabolism of fats; it facilitates the movement of fats in and out of cells. Like Vitamin B12, 5-adenosylmethionine, and Folic Acid, choline acts in the human body as a methyl donor. As such, choline is essential for proper liver function due to its key role in the lipotropic effect, i.e., the export of fat from the liver. In the absence of adequate choline, fats become trapped in the liver, where they block metabolism. Stagnation of fat and bile eventually leads to the development of more serious liver disorders such as cirrhosis.
• Choline is needed for cell membrane integrity because of the critical role it plays in the manufacture of primary components of cell membranes, such as phosphatidylcholine and sphingomyelin.
• Choline is essential in the synthesis of acetylcholine. Choline supplementation increases the accumulation of acetylcholine which plays a crucial role in many brain processes, including memory. (Canty, DJ and Zeisel, SH. Nutr Reviews. 52;327-339, 1994)
• Phosphatidylcholine increases the solubility of cholesterol and thereby decreases cholesterol‘s ability to induce atherosclerosis. Phosphatidylcholine aids in lowering cholesterol levels, removing cholesterol from tissue deposits, and inhibiting platelet aggregation. (Brook, JG, Linn, S, and Aviram, M. Biochem Med Metabol Biol. 35;31-39, 1986.) The high content of linoleic acid in phosphatidylcholine may be responsible for much of the benefit derived from supplementation.

Mode of Action


• Choline acts as a methyl donor, especially in liver function.
• Choline enables synthesis of acetylcholine, phosphatidylcholine and sphingomyelin.

Requirements

 

• Choline has recently been designated as an essential nutrient.

Food sources

• As free choline in vegetables (especially cauliflower and lettuce), whole grains, liver, and soy.
• As lecithin (containing 10-20% phosphatidylcholine) in grains, legumes, meat and egg yolks.
Deficiency
• True choline deficiency appears to be rare or non-existent and has only been induced in a research setting.
• Deficiencies typically present as muscle weakness, tingling in the fingers and toes, weight loss or fatigue.
• Liver and kidney disorders develop when animals are fed a choline-deficient diet.
• Fatty infiltration of the liver and other signs of liver dysfunction develops in humans fed a choline-deficient diet.
• Choline is an essential nutrient for human cells in cell cultures, and humans receiving intravenous feeding with solutions low in choline develop signs of choline deficiency.
(Canty, DJ and Zeisel, SH. Nutr Reviews. 52;327-339, 1994; Zeisel, SH, et al. FASEB J 5;2093-2098, 1991)

 

Therapeutic Uses

Liver Disorders

Phosphatidylcholine is used in the treatment of a variety of liver disorders, including:
• Acute & Chronic Viral Hepatitis: Chronic viral manifestations severely challenge the liver yet numerous controlled trials have established PC as a safe and potent intervention for infection (Mueting 1972, Hirayama 1980, Yamo1978, Kosina 1981, Jenkins 1982, Visco 1985, Hantak 1990, Ilic and Begic-Janev 1991). Optimal results were achieved in these studies when subjects were maintained on a combination of oral and infused PC utilizing higher doses. Once clinical indicators began returning to normal subjects were maintained on oral doses of PC. In addition to decreases in liver enzymes, serum lipids, immune markers and bilirubin, subjects experienced reversal of fatty degeneration, inflammation, jaundice, liver swelling and fibrosis, per liver biopsy.
• Cirrhosis of the liver
• Decreased bile solubility
• Diabetic fatty liver
• Drug-induced liver damage: The use of anticonvulsant drugs often leads to liver toxicity. Subjects who had received anticonvulsants for an average of five years were assessed by GGT elevation (Hisanaga 1980) and given PC for six months. Positive outcome was consistently achieved in subjects in addition to a decrease in GGT levels.
• Toxic liver damage: (Kuntz 1965) reported remarkable effects with PC in subjects with chemical poisoning and Esslinger (1966) with plant toxin.
• Fatty liver: 650 subjects with varying degrees of liver damage were followed for 5 years. Subjects received intravenous PC at 950 mg along with oral PC (450- 700 mg). When blood parameters returned to normal subjects were shifted to oral PC only. Subjects were categorized as to severity of liver damage: fatty degeneration, acute inflammation, chronic aggressive inflammation, and advanced fibrotic damage. All groups in the study had marked benefit. There was reversal of fatty degeneration in many subjects and in those with acute inflammation PC accelerated recovery by an average of ten days. (Wallnoefer and Hanusch 1973).
• Alcohol-induced liver disease: Studies with baboons have found that phosphatidylcholine supplementation protects against alcohol-induced liver abnormalities and cirrhosis; presumably some of these same effects will be present in humans. Nevertheless, choline salts do not seem to be of any value in the treatment of alcohol-induced liver disease in humans but may be useful in general liver support. (Lieber,CS and Rubin, E. N Engl J Med 280;705-708, 1969)

Detoxification

The health of the membrane is synonymous with the health of the entire organism. Toxins have an affinity for fatty acids; they literally take up residence in the lipid environment and in so doing, weaken and disrupt. The probable result is early apoptosis, premature death of the cell. Generally, normal mitosis provides for new cellular growth to maintain the health of the body, i.e. the previous discussion on photo receptors. However, toxicity's affinity for lipids can easily redistribute toxins and diseased toxic lipids into the new growth. In a healthy state with adequate glutathione and ascorbate to bind the toxins before they take up new residence, the body can keep the bad guys under control. However, if defenses are weak, toxins can continually be redistributed and eventually hide in the CNS and bone where the regeneration process is at a slower pace.

 

The goal of detoxification is to 1) encourage regrowth with a renewed effort at the correct balancing of the essential nutrients, with the exchange of high energy lipids (PUPA and HUP A) to fuel regeneration and the eventual detoxification process; and 2) at the correct time, the inclusion of the toxin removal specialists, ascorbate, chlorella, and if possible IV glutathione.

Detoxification of neurotoxins requires that the cell membrane is nourished with balanced essential fatty acids (4:1, plus HUFAs) and supportive phospholipids. Phosphatidylcholine (PC) is the most abundant phospholipid of the cell membrane and protects the liver, with its 33,000 square meters of membrane, against toxicity and infection. The liver plays a pivotal role in detoxification but due to its fatty acid content and the lipid soluble characteristics of neurotoxins, lipid based interventions are required to impact toxic burdens. Once the liver has been damaged it can no longer metabolize fats normally. Pools of lipids are then deposited within hepatocytes throughout the liver. Beta oxidation of fatty acids is suppressed impairing detoxification and prostaglandin production. Extensive research with PC has revealed that it protects the liver against damage from alcohol, pharmaceuticals, environmental pollutants, xenobiotics and infection due to viral, bacterial and fungal manifestations (Lieber 1994a, 1994b, 1995, 2001a, 2001b).

Hypercholesterolemia and Atherosclerosis

Phosphatidylcholine increases the solubility of cholesterol and thereby decreases its ability to induce atherosclerosis. Phosphatidylcholine also aids in lowering cholesterol levels, removing cholesterol from tissue deposits, and inhibiting platelet aggregation. (Brook, JG, Linn, S, and Aviram, M. Biochem Med Metabol Biol. 35;31-39, 1986.) Here some of the beneficial effects may be attributable to the high content of linoleic acid in phosphatidylcholine.

• The phospholipid preparation Lipostabil has been researched for use in the treatment of high cholesterol levels and atherosclerosis. In several trials evaluating this 70% phosphatidylcholine content lecithin product from Germany, total serum cholesterol and triglyceride levels dropped significantly and HDL cholesterol levels improved using dosage ranging from 1.5 g once daily to 3.5 g three timed per day. (Lipostabil. Natterman International GMBH,1990; Wojcicki, J, et al. Phytotherapy Res. 9;597-599, 1995)
• A high-concentration phosphatidylcholine preparation, marketed in Germany under the trade name "Essentiale", has produced clinical results consistent enough to gain authorization from the BGA, the German equivalent of the FDA. This form contains 90% phosphatidylcholine, with 50% of the molecule having linoleic acid, the essential fatty acid, bound at the proper position; i.e., the first and second carbon of the glycerol molecule. Using this preparation the standard dosage recommendation is 350 mg three times per day with meals. (Essentiale, Natterman International GMBH, 1989.)

Bipolar Depression

• There is evidence that mania is associated with a reduced brain cholinergic activity. Phosphatidylcholine supplementation at levels of 15-30 g/day has been found to exert beneficial effects in the treatment of bipolar depression. (Wutman, R, et al. Nutrition and the Brain. Vol. 5. Raven Press: New York, 1979; Cohen, B, et al. Am J Psychiat 137:242-243, 1980; Cohen, B, et al. Am J Psychiat 139;1162-1164, 1982.)
• The use of phosphatidylcholine may result in significant improvement or amelioration of symptoms in some patients suffering from bipolar depression by increasing brain choline levels. Some researchers believe that one effect of Lithium carbonate, the standard pharmaceutical treatment for bipolar depression, is the promotion of increased acetylcholine activity in the brain. (Jope, R, et al. Am J Psychiat 142;356-358,1985)

Alzheimer’s Disease

• Choline supplementation increases the accumulation of acetylcholine within the brain in normal patients so many researchers hypothesized that phosphatidylcholine supplementation would benefit Alzheimer patients. Some research has indicated that increasing acetylcholine content in the brain through supplemental choline might result in improved memory. However, clinical trials using phosphatidylcholine have not produced significant benefits. Studies revealed inconsistent improvements in memory from choline supplementation in both normal and Alzheimer’s patients. Nevertheless, criticisms of these studies and their interpretations have been raised on the grounds that sample size was too small, the dosage of phosphatidylcholine used was too low, and the studies themselves were poorly designed. (Rosenberg, G and Davis, KL. Am J Clin Nutr. 36; 709-720, 1982; Levy, R, et al. Lancet 1;474-476,1982; Sitaram, N, et al. Life Sci 22;1555-1560, 1978.)
• Alzheimer’s disease is characterized by a decrease in cholinergic transmission, but the basic defect in cholinergic transmission in Alzheimer’s disease relates to impaired activity of the enzyme acetylcholine transferase, not to a deficiency of choline. Acetylcholine transferase combines choline with an acetyl molecule to form acetylcholine. However, since increased levels of choline do not necessarily increase the activity of this critical enzyme, phosphatidylcholine supplementation will probably not prove efficacious in the majority of patients with Alzheimer’s disease.
• In a patient with mild to moderate dementia, the use of a high-quality phosphatidylcholine preparation at a dosage level of 15 to 25 g/day may be beneficial. (Murray, M. p. 140, 1996.)

Forms

 

• Choline is available as a soluble salt, most commonly as either choline bitartrate, citrate, or chloride, or as phosphatidylcholine in lecithin.
• Most commercial forms of lecithin contains only 10-20% phosphatidylcholine.
• Most supplements labeled as "phosphatidylcholine" contain only 35 percent.
• Some newer and more potent preparations contains up to 98 percent phosphatidylcholine. These more pure forms of phosphatidylcholine are preferred since they are associated with fewer gastrointestinal side effects. This is particularly true in the treatment of those conditions that require large doses of phosphatidylcholine (i.e., 15 to 30 grams) because low-concentration forms such as lecithin would be required in such large amounts that side effects would be nearly inevitable.

Intravenous form is also available. The liver is the largest organ of the body and receives the first flush of PC from an infusion. However an exchange of lipids is systemic with every organ, every neuron, every cell sharing the increased PC and the higher performing lipids (HUFAs). It should be expected that improved metabolic performance would also be systemic.

Side Effects

• Choline and phosphatidylcholine are generally well tolerated.