Chemistry:Glycerophosphorylcholine
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| Formula | C8H20NO6P |
| Molar mass | 257.223 g·mol−1 |
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L-α-Glycerophosphorylcholine (alpha-GPC, choline alfoscerate, sn-glycero-3-phosphocholine) is a natural choline compound found in the brain. It is also a parasympathomimetic acetylcholine precursor[1] which has been investigated for its potential for the treatment of Alzheimer's disease[2] and other dementias.[3]
Alpha-GPC rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of acetylcholine.[2] It is a non-prescription drug in most countries. The FDA determined that intake of no more than 196.2 mg/person/day is considered generally recognized as safe (GRAS).[4]
Production
Industrially, alpha-GPC is produced by the chemical or enzymatic deacylation of phosphatidylcholine enriched soya phospholipids followed by chromatographic purification. Alpha-GPC may also be derived in small amounts from highly purified soy lecithin as well as from purified sunflower lecithin.[5][6]
Safety
A retrospective cohort study involving 12 million participants in South Korea found that α-GPC users had a higher risk of stroke ( + 46 % ). The authors suggested that one possible explanation is that dysbiosis may lead to α-GPC being metabolized into trimethylamine (TMA) in the gastrointestinal tract, and then to trimethylamine N-oxide (TMAO) in the liver, which has implications for cardiovascular health. However, they also noted that the study could be influenced by confounding variables, as α-GPC is often prescribed to individuals with preexisting health risks.[7]
A later systematic review and meta-analysis criticized the statistical analysis of the South Korean cohort study, describing it as questionable and imprecise. The review concluded that α-GPC has a favorable safety and tolerability profile and is effective in improving cognitive function and daily living in patients with dementia disorders of neurological origin, adult-onset vascular dementia, and Alzheimer’s disease.[8]
References
- ↑ "Cognitive improvement in mild to moderate Alzheimer's dementia after treatment with the acetylcholine precursor choline alfoscerate: a multicenter, double-blind, randomized, placebo-controlled trial". Clinical Therapeutics 25 (1): 178–93. January 2003. doi:10.1016/S0149-2918(03)90023-3. PMID 12637119.
- ↑ 2.0 2.1 "Cholinergic precursors in the treatment of cognitive impairment of vascular origin: ineffective approaches or need for re-evaluation?". Journal of the Neurological Sciences 257 (1–2): 264–9. June 2007. doi:10.1016/j.jns.2007.01.043. PMID 17331541.
- ↑ "Treatment of dementia with neurotransmission modulation". Expert Opinion on Investigational Drugs 12 (10): 1633–54. October 2003. doi:10.1517/13543784.12.10.1633. PMID 14519085.
- ↑ "Generally Recognized as Safe (GRAS) Determination for the Use of AlphaSize® Alpha-Glycerylphosphoryl Choline". United States Food and Drug Administration. 25 January 2012. https://www.accessdata.fda.gov/scripts/fcn/gras_notices/GRN000419.pdf.
- ↑ "Choline alphoscerate (alpha-glyceryl-phosphoryl-choline) an old choline- containing phospholipid with a still interesting profile as cognition enhancing agent". Current Alzheimer Research 10 (10): 1070–9. December 2013. doi:10.2174/15672050113106660173. PMID 24156263.
- ↑ "Revisiting choline alphoscerate profile: a new, perspective, role in dementia?". The International Journal of Neuroscience 123 (7): 444–9. July 2013. doi:10.3109/00207454.2013.765870. PMID 23387341.
- ↑ "Association of L-α Glycerylphosphorylcholine With Subsequent Stroke Risk After 10 Years". JAMA Network Open 4 (11): e2136008. November 2021. doi:10.1001/jamanetworkopen.2021.36008. ISSN 2574-3805. PMID 34817582.
- ↑ "Activity of Choline Alphoscerate on Adult-Onset Cognitive Dysfunctions: A Systematic Review and Meta-Analysis". Journal of Alzheimer's Disease 92 (1): 59–70. 2023-03-07. doi:10.3233/JAD-221189. PMID 36683513.
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