Choline Alphoscerate (Alpha-Glyceryl-Phosphoryl-Choline) An Old Choline- containing Phospholipid with a Still Interesting Profile As Cognition Enhancing Agent

Abstract

Cholinergic precursors have represented the first approach to counter cognitive impairment occurring in adultonset dementia disorders. These compounds were early leaved because their clinical efficacy was not clearly demonstrated. This is probably not true for some choline-containing phospholipids including choline alphoscerate. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. An ongoing trial indicates that association between the acetylcholinesterase inhibitor donepezil and choline alphoscerate is accompanied by an improvement in several cognitive tests superior to that induced by donepezil alone. It is suggested that this association may represent a therapeutic option to prolong beneficial effects of cholinergic therapies in Alzheimer's disease patients with concomitant ischemic cerebrovascular disorders. In summary, choline alphoscerate has significant effects on cognitive function with a good safety profile and tolerability. Although limited both in terms of size of the samples investigated and of the length of treatment, preclinical and clinical results presented suggest that cognitive enhancing capabilities of choline alphoscerate merit of being further investigated in appropriate trials.

Targeting Mitochondrial Dysfunction with L-Alpha Glycerylphosphorylcholine

“…Earlier studies from our laboratory have demonstrated that GPC administration can reduce several signs of oxidative and inflammatory tissue damage in experimental IR models [12, 13]. The anti-inflammatory action of a potentially parasympathomimetic compound is an interesting finding, because that targets the inflammatory cascade without the confounding effects of mediators deriving from the metabolism of the lipid side-chains [14]. …”

Нейропротекція При Гострому Ішемічному Інсульті: Від Нейрофармакології До Фармакотерапії

“…Серед численних функцій ацетилхоліну в центральній нервовій системі (ЦНС) особливо слід відзначити регуляцію когнітивних функцій, рухових реакцій (ініціація рухів, рухові стереотипи тощо), церебрального судинного тонусу (за рахунок впливу на біосинтез NO). Також необхідно відзначити виключно важливу роль ацетилхоліну як ключового компонента підтримки нейромедіаторного балансу і, відповідно, регуляції психоемоційної сфери, поведінки тощо [6,27]. Крім того, велика роль ацетилхоліну і в активації процесів нейропластичності в ЦНС [24].…”

Neuroprotective Effects of Choline and Other Methyl Donors

“…Choline-containing compounds have also shown promising results in animal models. For example, GPC has been shown to induce Ach release in the rat hippocampus and cause positive structural changes in this area of the brain that is associated with attention, learning and memory [97]. Long-term supplementation of CDP-choline in the rat diet has been shown to prevent the development of spatial memory deficit in aged rats [98].…”