Choline is a nutrient found in many food sources, including milk, liver, eggs, peanuts, soybeans, beef, cauliflower, kale, and cabbage. It is used in the body for two main purposes, as a precursor to the neurotransmittor acetylcholine and to form lecithin. Although not yet considered an essential nutrient in humans, deficiency may result in liver disease (1), and an adequate intake has been set at 550 mg per day (with an upper limit of 3,500 mg per day). Various conditions, such as stress (including exercise), aging, and certain supplements (such as carnitine and some nootropics) may increase choline need. This article will examine the application of three different types of choline supplements, choline (as bitartate, citrate, chloride, etc.), phosphatidylcholine, and alpha-glycerylphosphorylcholine (alpha-GPC).
Choline
Choline is available in many forms, including choline bitartrate, choline citrate, and choline chloride. Of all of the forms of choline supplements, these are the least effective. Choline supplements have not been researched in many areas (phosphatidylcholine, which is more effective, is generally preferred), but they do not appear to effect cognition or physical performance in healthy individuals after exhaustive activity (2). Large doses of choline administered to rats were rapidly metabolized, implying that the body has a strong adaptive response (3). Additionally, acute dosing of large amounts of choline bitartrate does not change the amount of choline or its metabolites in the human brain (4). Choline supplements are primarily useful where choline levels are low and it becomes the rate limiting factor for phospholipid and acetylcholine synthesis, such as neurodegeneration (5).
Although choline does not appear to be effective for much, it may aid in weight loss, expecially when combined with carnitine. Supplemental choline aids in the conservation of carnitine, increasing its effectiveness (6), and it should also be noted that choline requirements may not be met in periods of caloric restriction. 700 mg of carnitine combined with 1000 mg of choline has been found to reduce bodyfat more than either supplement alone (6). The combination of choline and carnitine along with caffeine causes significant body fat reduction in rats, and exerts a physiological response similar to that of exercise (7).
Lecithin (Phosphatidylcholine)
Lecithin, which contains phosphatidylcholine, has all the beneficial effects of choline, but is both more bioavailable and less expensive. It also has more promising studies supporting supplementation. In humans, choline chloride (2-3 g) raises serum choline by 86% and values return to normal within 4 hours, whereas lecithin increases levels by 265% and choline levels stay above normal for 12 hours (8). After long-term administration, the amount of choline in the blood returns to normal, but phosphatidylcholine remains elevated in certain areas, such as the cortex and striatum (9). Although lecithin supplementation does not effect acetylcholine levels under normal conditions, it facilitates its release in times where there is elevated need for acetylcholine (10). This includes periods of stress – in a study where rats were subjected to C-H-R (cold-hypoxia-restraint), a test that measures adaptation and resistance to stress, lecithin increased both tolerance and recovery (11).
Exercise is another activity that increases both mental and physical stress. Exercise causes a significant depletion of choline levels, and it has been hypothesized that this may impair performance (12). Unfortunately, lecithin has not yet been shown to increase athletic performance, although it does prevent the decline in choline seen with exercise (13).
Long term use of lecithin may aid in the prevention of neurological degeneration. Combined with pyruvate, it slowed nerve degeneration in mice (14). Studies in senile mice also indicate improved memory, increased acetylcholine, and improved learning (combined with B12) (15, 16).
Alpha-GPC
Alpha-glycerylphosphorylcholine is the most bioavailable form of choline, and also has some mild nootropic effects. It improves performance in both active and conditioning tasks in both young and old mice by increasing production of inositol phosphate (17), as well as increasing protein kinase C activity (an effect of other nootropics, such as oxiracetam) (18), acetylcholine release (18), and nerve growth factor (19). It has been effectively used to treat Alzheimer's and increase recovery from stroke, and it also increases GH in both young and old humans (20).
The only problem with alpha-GPC at present is the cost. One gram a day is the recommended dosage, which will be cost-prohibitive for most people. However, any dosage will impart benefits, so a low dose of alpha-GPC combined with lecithin is cost-effective. Pinnacle AlphaDopa employs a sublingual delivery system for alpha-GPC, which may also improve the effectiveness of a given amount.
References
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2. Deuster PA, Singh A, Coll R, Hyde DE, Becker WJ. Choline ingestion does not modify physical or cognitive performance. Mil Med. 2002 Dec;167(12):1020-5
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7. Hongu N, Sachan DS. Caffeine, carnitine and choline supplementation of rats decreases body fat and serum leptin concentration as does exercise. J Nutr 2000 Feb;130(2):152-7
8. Wurtman RJ, Hirsch MJ, Growdon JH. Lecithin consumption raises serum-free-choline levels. Lancet. 1977 Jul 9;2(8028):68-9
9. Muma NA, Rowell PP. Brain and serum levels of choline and lecithin resulting from long-term administration. Neurochem Res. 1986 Apr;11(4):481-8
10. Jope RS. Effects of phosphatidylcholine administration to rats on choline in blood and choline and acetylcholine in brain. J Pharmacol Exp Ther. 1982 Feb;220(2):322-8
11. Kumar R, Divekar HM, Gupta V, Srivastava KK. Antistress and adaptogenic activity of lecithin supplementation. J Altern Complement Med. 2002 Aug;8(4):487-92
12. Buchman AL, Jenden D, Roch M. Plasma free, phospholipid-bound and urinary free choline all decrease during a marathon run and may be associated with impaired performance. J Am Coll Nutr. 1999 Dec;18(6):598-601
13. Buchman AL, Awal M, Jenden D, Roch M, Kang SH. The effect of lecithin supplementation on plasma choline concentrations during a marathon. J Am Coll Nutr. 2000 Nov-Dec;19(6):768-70
14. Shea TB, Ekinci FJ, Ortiz D, Dawn-Linsley M, Wilson TO, Nicolosi RJ. Efficacy of vitamin E, phosphatidyl choline, and pyruvate on buffering neuronal degeneration and oxidative stress in cultured cortical neurons and in central nervous tissue of apolipoprotein E-deficient mice. Free Radic Biol Med. 2002 Jul 15;33(2):276-82
15. Chung SY, Moriyama T, Uezu E, Uezu K, Hirata R, Yohena N, Masuda Y, Kokubu T, Yamamoto S. Administration of phosphatidylcholine increases brain acetylcholine concentration and improves memory in mice with dementia. J Nutr. 1995 Jun;125(6):1484-9
16. Hung MC, Shibasaki K, Yoshida R, Sato M, Imaizumi K. Learning behaviour and cerebral protein kinase C, antioxidant status, lipid composition in senescence-accelerated mouse: influence of a phosphatidylcholine-vitamin B12 diet. Br J Nutr. 2001 Aug;86(2):163-71
17. Schettini G, Ventra C, Florio T, Grimaldi M, Meucci O, Scorziello A, Postiglione A, Marino A. Molecular mechanisms mediating the effects of L-alpha-glycerylphosphorylcholine, a new cognition-enhancing drug, on behavioral and biochemical parameters in young and aged rats. Pharmacol Biochem Behav. 1992 Sep;43(1):139-51
18. Govoni S, Battaini F, Lucchi L, Pascale A, Trabucchi M. PKC translocation in rat brain cortex is promoted in vivo and in vitro by alpha-glycerylphosphorylcholine, a cognition-enhancing drug. Ann N Y Acad Sci. 1993 Sep 24;695:307-10
19. Vega JA, Cavallotti C, del Valle ME, Mancini M, Amenta F. Nerve growth factor receptor immunoreactivity in the cerebellar cortex of aged rats: effect of choline alfoscerate treatment. Mech Ageing Dev. 1993 Jun;69(1-2):119-27
20. Ceda GP, Ceresini G, Denti L, Marzani G, Piovani E, Banchini A, Tarditi E, Valenti G. alpha-Glycerylphosphorylcholine administration increases the GH responses to GHRH of young and elderly subjects. Horm Metab Res. 1992 Mar;24(3):119-21
