Alpha-GPC

BACKGROUND: Choline, as a neurotransmitter acetylcholine precursor, is reportedly associated with cognitive function. Although there are several cohort and animal studies on choline-containing foods and cognitive function, only a few interventional studies were reported. Egg yolk is a rich source of different choline-containing chemical forms, such as phosphatidylcholine (PC), lysophosphatidylcholine (LPC), and α-glycerophosphocholine (α-GPC). This study aimed to investigate the effect of consuming 300 mg of egg yolk choline per day on cognitive function of Japanese adults. METHODS: A 12-week, randomized, double-blind, placebo-controlled, parallel-group study was conducted in 41 middle-aged and elderly males and females (43.9% female) aged ≥ 60 years and ≤ 80 years without dementia. Participants were randomly assigned to placebo and choline groups. The choline group received a supplement containing egg yolk choline (300 mg/day), and the placebo group received an egg yolk supplement free from choline for 12 weeks. Assessments of Cognitrax, Trail Making Tests (TMT) part A and B, the MOS 36-Item Short-Form Health Survey (SF-36), the Simplified Japanese Version of the WHO-Five Well-Being Index (WHO-5), and plasma choline levels were performed before and 6 and 12 weeks after supplement intake. In the present study, 19 subjects (9 in the placebo group and 10 in the choline group) were excluded due to the violation of the discontinuation criteria or participant compliance, and 41 subjects were analyzed. RESULTS: The change amount of verbal memory scores and verbal memory test-correct hit (delay) was significantly higher in the choline group than in the placebo group at baseline-6 and baseline-12 weeks. The plasma free choline level was significantly higher in the choline group compared with the placebo group at 6 weeks. Conversely, the choline group showed significantly lower Cognitrax processing speed scores, symbol digit coding testing correct responses, and SF-36 physical quality of life summary scores compared to the placebo group at 6 weeks. CONCLUSIONS: The results suggested that continued 300 mg/day intake of egg yolk choline improved verbal memory, which is a p

The effects of alpha-glycerylphosphorylcholine (alpha-GPC) on endogenous cortical GABA release were studied both in vivo and in vitro. In freely moving rats, equipped with epidural cups, alpha-GPC (30-300 mg/kg i.p.) increased GABA release. This effect was potentiated by atropine, both systematically administered (5 mg/kg i.p.) and locally applied (1.4 microM), but not by mecamylamine (4 mg/kg i.p.). The alpha-GPC-induced increase in GABA release was abolished in rats pretreated with the alpha 1 receptor antagonist prazosin (14 micrograms/kg i.p.). In cortical slices alpha-GPC (0.4 mM) increased the spontaneous GABA efflux. This effect was abolished by tetrodotoxin (0.5 microM) and prazosin (1 microM), but not by atropine (0.15 microM) or mecamylamine (2.5 microM). These results indicate that the facilitatory response by alpha-GPC on GABA release does not depend on a direct activation of either muscarinic or nicotinic receptors, but suggest the involvement of the noradrenergic system.

The in vivo and in vitro effect of oxiracetam, aniracetam and alpha-glycerylphosphorylcholine (alpha GPC) on protein kinase C (PKC) activity was studied in rat brain cortex and hippocampus. Administration of oxiracetam and alpha GPC in vivo elicited an early increase of particulate histone-directed PKC activity accompanied by a decrease of soluble activity and followed a few hours later by a down regulation of the enzyme. The effect was also observed in vitro when either oxiracetam or alpha GPC were administered at nanomolar concentrations to rat brain cortex slices. Aniracetam had no effect in the cortex but promoted PKC translocation both in vivo and in vitro in the hippocampus. In cortex slices the effect of oxiracetam was antagonized by the addition of AP-5, an NMDA receptor blocker, but not by CNQX and L-AP3, antagonists of AMPA and metabotropic glutamate receptors, respectively. Scopolamine also prevented the increase of particulate PKC elicited by oxiracetam in vitro. In the hippocampus the increase of particulate PKC activity was antagonized by AP-5, CNQX and L-AP3, indicating participation by both ionotropic and metabotropic glutamate receptors in the action of aniracetam. The data support the hypothesis that PKC activation may be a common mechanism amongst cognition stimulating drugs from different chemical classes.

BACKGROUND: Choline alphoscerate (alpha glyceryl phosphorylcholine, α-GPC) is a choline-containing phospholipid used as a medicine or nutraceutical to improve cognitive function impairment occurring in neurological conditions including adult-onset dementia disorders. Despite its 1985 marketing authorization, there are still discrepancies between countries regarding its approval as a prescription medicine and discussions about its effectiveness. OBJECTIVE: This study aimed to evaluate the efficacy of the α-GPC compound for treating cognitive impairment in patients with adult-onset neurological disorders. METHODS: Relevant studies were identified by searching PubMed, Web of Science, and Embase. Studies that evaluated the effects of α-GPC alone or in combination with other compounds on adult-onset cognitive impairment reporting cognition, function, and behavior were considered. We assessed the risk of bias of selected studies using the Cochrane risk of bias tool. RESULTS: A total of 1,326 studies and 300 full-text articles were screened. We included seven randomized controlled trials (RCTs) and one prospective cohort study that met our eligibility criteria. We found significant effects of α-GPC in combination with donepezil on cognition [4 RCTs, mean difference (MD):1.72, 95% confidence interval (CI): 0.20 to 3.25], functional outcomes [3 RCTs, MD:0.79, 95% CI: 0.34 to 1.23], and behavioral outcomes [4 RCTs; MD: -7.61, 95% CI: -10.31 to -4.91]. We also observed that patients who received α-GPC had significantly better cognition than those who received either placebo or other medications [MD: 3.50, 95% CI: 0.36 to 6.63]. CONCLUSION: α-GPC alone or in combination with donepezil improved cognition, behavior, and functional outcomes among patients with neurological conditions associated with cerebrovascular injury. The Cholinesterase Inhibitory Properties of Stephaniae Tetrandrae Radix. Kong XP(1)(2), Ren HQ(2)(3), Liu EYL(3)(4), Leung KW(2)(3), Guo SC(2)(3), Duan R(2)(3), Dong TTX(2)(3), Tsim KWK(2)(3). Author information: (1)Institute of Pharmaceutical & Food Engineering, Chinese Medicine Master Studio of Wang Shimin, Shanxi University of Chinese Medicine, 121 Dax

BACKGROUND: Globally, stroke is the second leading cause of death and disability. In different studies conducted previously, the choline-containing phospholipids citicoline and choline alphoscerate have been proposed as adjuvants in the treatment of acute strokes. A systematic review was conducted to provide updated information on the effects of citicoline and choline alphoscerate in patients with acute and hemorrhagic strokes. METHODS: PubMed/Medline, Scopus, and Web of Science were searched to identify relevant materials. Data were pooled, and odds ratios (OR) were reported for binary outcomes. Using mean differences (MD), we evaluated continuous outcomes. RESULTS: A total of 1460 studies were reviewed; 15 studies with 8357 subjects met the eligibility criteria and were included in the analysis. In our study, citicoline treatment did not result in improved neurological function (NIHSS < 1, OR = 1.05; 95% confidence interval (CI): 0.87-1.27) or functional recovery (mRS < 1, OR = 1.36; 95% CI: 0.99-1.87) in patients with acute stroke. Choline alphoscerate improved neurological function and functional recovery in stroke patients based on the Mathew's scale and the Mini-Mental State Examination (MMSE). CONCLUSION: Citicoline did not improve the neurological or functional outcomes in acute stroke patients. In contrast, choline alphoscerate improved neurological function and functional recovery and reduced dependency in stroke patients.

A multicentre, randomised, controlled study compared the efficacy of l-alpha-glyceryl-phosphorylcholine (alpha GPC) and ST200 (acetyl-l-carnitine) among 126 patients with probable senile dementia of Alzheimer's type (SDAT) of mild to moderate degree. Efficacy was evaluated by means of behavioural scales and psychometric tests. The results showed significant improvements in most neuropsychological parameters in the alpha GPC recipients. Improvements also occurred in the ST200 recipients but to a lesser extent. Tolerability was good in both groups. These positive findings require replication in larger, double-blind, longitudinal studies coupling clinical and biological determinations.

L-alpha-glycerylphosphorylcholine (alpha-GPC) is a recently developed cognitive enhancer whose mode of action is considered to involve the release of free choline, which is then utilized for acetylcholine and phosphatidylcholine biosynthesis in the brain. The purpose of this study was to evaluate the profile of free plasma choline levels following a single i.m. dose of alpha-GPC in 12 normal volunteers. Citicoline (CTC), which also acts as a choline precursor, was included for comparison purposes. Each subject was studied on three randomized occasions, (i) in a control day in the absence of drug administration (to evaluate the plasma level profile of endogenous choline), (ii) after i.m. alpha-GPC (1,000 mg) and (iii) after i.m. CTC (1,000 mg) respectively, with a wash-out period of at least 1-week between sessions. Blood samples for plasma choline HPLC determinations were collected at regular intervals over a 6 h period. In the control session, plasma choline levels remained stable during the sampling period. The administration of alpha-GPC was associated with a rapid rise in plasma choline, peak levels being usually observed at the first (0.25 h) or second (0.5 h) sampling time after the injection. Thereafter, the concentration of choline declined gradually and returned to near baseline values at the end of the observation period. After the administration of CTC, plasma choline levels showed a similar time course but were considerably lower than those observed after the administration of alpha-GPC.(ABSTRACT TRUNCATED AT 250 WORDS)

An open clinical trial was carried out to compare the efficacy and the tolerability of 1 g/day alpha-glycerylphosphorylcholine (alpha-GPC) with 1 g/day cytosine diphosphocholine (CDP) both given intramuscularly for 90 days in 120 patients with mild to moderate vascular dementia. The clinical evaluation, carried out at the start as well as halfway through (45 days) and at the end of treatment (90 days), was expressed by psychometric tests (modified Parkside behaviour rating scale, Sandoz clinical assessment geriatric scale, word fluency test, Hamilton's rating scale of depression, narration subtest of Wechsler memory scale). Both treatments produced a definite symptomatic improvement and showed a very good tolerability. The results suggest that in most tests alpha-GPC possessed a statistical higher efficacy and an overall more satisfactory activity assessed by both patients and investigators compared with CDP.