Choline was discovered by Adolph Strecker in 1864 and was synthesized two years thereafter. It is an essential nutrient necessary for physical and cognitive health. It was recognized by the US Institute of Medicine as a vital nutrient in 1998. The human body can secrete small amounts of choline through consuming choline enriched foods like beef, eggs, soy, milk and liver.
The amount of this nutrient in these foods however are lacking, hence most individuals have deficient choline levels. Since choline is very important for normal growth and development, search for choline supplements including use of alpha GPC started. Today, alpha GPC is a prescribed medication for Alzheimer’s disease in Europe. It is also currently available as a dietary supplement for brain health in the US.
Alpha GPC, also known as L-Alpha glycerylphosphorylcholine/choline alphoscerate is a phospholipid building block and a water soluble compound that easily crosses the blood brain barrier to aide in memory and overall cognitive functions. Its chemical structure is primarily a choline particle attached to a glycerol configuration through a phosphate group. Without the two fatty acids linked on its structure, it is a lecithin molecule or a phosphatidylcholine.
[msgbox]Chemical name/ IUPAC: (2S)-2,3-Dihydroxypropyl 2-(trimethylammonio) ethyl phosphate
Chemical formula: C8H20NO6P
Uses: Memory and cognition enhancer, choline supplement[/msgbox]
Mechanism of action
Alpha-GPC treatment can be done through oral and parenteral (intravenous) routes which increase the levels of glycerophosphocoline in the brain suggesting easy passage across the blood brain barrier. Repeated consumption of this choline supplement will significantly increase neuronal uptake of inositol phosphate. This is caused by phospholipid synthesis increase potentiating potassium activated hippocampal calcium release and receptor facilitated inositol phosphate production. These events enhance phospholipid synthesis and metabolism which facilitates cognitive processes.
Additionally, alpha-GPC plays a role on the transmission of different neurotransmitters. It increases dopamine release on the cerebellum and frontal cortex whilst improve potassium activated neuronal dopamine release and increase in DOPAC (a dopamine metabolite) production. It also increase serotonin levels on the same brain regions – cerebellum and frontal cortex.
Alpha GPC increases acetylcholine concentration in the brain particularly on the frontal cortex. However, it appears that it is more reliable in maintaining acetylcholine levels during stress whilst enhance acetylcholine transporter release. Also, it exerts neuroprotective mechanisms through increasing cholinergic brain activities via nicotonic acetylcholine receptor activation . Alpha GPC also increases the release of GABA by acting on the alpha-1 adrenergic receptors.
Memory and attention improvement
One of the benefits associated with alpha GPC intake includes improvement on different cognitive functions including memory and attention. In one particular study, the effects of L-alpha GPC on memory disorder initiated by scopolamine were evaluated. 32 healthy individuals were recruited as participants. This sample population was subsequently divides into four groups.
All participants randomly received pre-treatment for 10 days with either a placebo or alpha GPC after which they received scopolamine or placebo on the 11th day. The effects of this drug supplement were evaluated through different mnemonic and attention tests. Data analysis revealed that alpha GPC has the potential to antagonize memory and attention impairment triggered by scopolamine .
Alzheimer’s disease treatment
Early literature data demonstrate that alpha GPC, one of the more potent precursors of acetylcholine, can help in alleviating impaired memory, ability to learn and motor function on individuals suffering with Alzheimer’s disease. A study was therefore launched to assess the tolerability and efficacy of choline alfoscerate/alpha GPC as a treatment for cognitive problems including Alzheimer’s. In this multicenter, placebo-controlled, double-blind trial, individuals diagnosed with mild to moderate dementia were randomly treated with alpha GPC or placebo for 180 days.
Effects of the treatment were assessed using different scales such as Mini Mental State Examination (MMSE), Alzheimer’s Disease Assessment Scale (ADAS), Clinical Global Impression (CGI) scale and Global Improvement Scale (GIS). Results analysis revealed that significant statistical difference were observed on those who were treated with choline alfoscerate on all scales compared to those who were in placebo. As such, this trial suggests that alpha GPC is clinically safe and useful in treating mild to moderate dementia symptoms of the Alzheimer’s type .
Enhancement of fat oxidation
Other than potentially treating cognitive related problems, alpha GPC also appears to help in growth hormone secretion and substitute choline in the body which may help protect the liver. The mechanism of alpha GPC in exerting this hepatic protective ability seems to arise from its ability to increase fat metabolism. To clarify whether there is a basis for these claims; a group of researchers investigated the physiologic responses of the body upon intake of a single dose of alpha GPC. 8 healthy male individuals were recruited. They were randomly given placebo and alpha GPC.
Analysis of laboratory blood samples collected before and after alpha GPC and placebo treatment revealed that choline levels were significantly increased after a single dose of alpha GPC. This study suggests that alpha GPC can help in increasing fat oxidation as well as improve growth hormone release. Indeed, this particular dietary supplement may help in protecting the liver from steatosis and other hepatic related problems .
Cerebral ischemic attack recovery
Alpha GPC is a drug supplement that is able to increase the levels of choline in that brain. It was also purported to protect the neuronal cell walls. As such, it is claimed that alpha GPC can also assist in cerebral ischemic attack recovery. A multicenter trial on 2044 individuals who recently suffered transient ischemic attack or stroke was carried out to reveal the effects of this acetylcholine precursor on promoting stroke recovery. Participants were given daily doses of alpha GPC for 5 months and 28 days. Efficacy of the drug was assessed using different cognitive scales. This study confirms that alpha GPC is tolerable and can help in increasing rate of stroke recovery .
In a randomized trial, the effects of supplements intended to enhance, alertness, focus, reaction time and decrease fatigue was measured. One of these supplements include alpha GPC. 19 physically healthy and active college students were recruited to join in the study. The participants were given cognitive enhancing supplements. Effects of these drugs were assessed using different cognitive questionnaires/scales. Results indicated that ingestion of alpha GPC can help in improving reaction performance and brain functions even in times of increased stress .
Alpha GPC is generally safe (with minimal subjective side effects such as insomnia, heartburn, nausea and headache ) and efficient in producing a wide array of therapeutic effects on humans. It is approved for use as a drug supplementation in the US. However, individuals who intend to consume this particular cognitive enhancer should take precautions before use.