Alpha GPC

L-Alpha glycerylphosphorylcholine (alpha-GPC, choline alfoscerate) is a natural choline compound found in the brain. It is also a parasympathomimetic acetylcholine precursor which has been investigated for its potential for the treatment of Alzheimer’s disease[2] and other dementias.

Alpha-GPC rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of acetylcholine. 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.

RESEARCH

An Italian multicentre clinical trial on 2,044 patients suffering from recent stroke were supplied alpha-GPC in doses of 1,000 mg/day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales (Mathew Scale (MS), Mini Mental State Test (MMST), Crichton Rating Scale (CRS) and the Global Deterioration Scale (GDS)) three of which reached statistical significance.[non-primary source needed] In trials utilizing alpha-GPC in vascular dementia, alpha-GPC administration was reported to improve performance on psychometric tests and to be well tolerated.

Small scale studies focusing on the effects of alpha-GPC on physical performance have also reported that alpha-GPC supplementation can increase maximum power and velocity in specified tests (counter-movement jump test) and increase lower body force (isometric mid-thigh pull test). In iron deficient women, alpha-GPC supplementation has also been reported to enhance non-heme iron uptake from dietary sources.

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 from purified sunflower lecithin.

L-Alpha-glycerylphosphorylcholine (GPC) is a widely used food supplement. GPC has been shown to exert beneficial effects in several organs; however, the cardiac effects of GPC have yet to be investigated. The aim of the present study was therefore to map out the effects of GPC on cardiac myocytes, with or without ischemia–reperfusion insult. Neonatal rat cardiac myocytes were treated with GPC at 1, 10, 80, and 100 µM concentrations for 15 min, 3 h, or 24 h, respectively. Cell viability by calcein assay and the degree of oxidative stress by DHE (superoxide level) and H₂DCF (total ROS accumulation) staining were measured. In separate experiments, cardiomyocytes were pre-treated with the optimal concentration of GPC for 3 h and then cells were exposed to 4 h of simulated ischemia followed by 2 h of reperfusion (SI/R). Cell viability was measured at the end of the SI/R protocol. In normoxic conditions, the 15-min and the 3-h GPC treatment did not affect cell viability, total ROS, and superoxide levels. Under SI/R conditions, the 3-h GPC treatment protected the cardiac myocytes from SI/R-induced cell death and did not alter the level of oxidative stress. The 24-h GPC treatment in normoxic conditions resulted in significant cell death and increased oxidative stress at each concentration. Here we provide the first evidence for the cytoprotective effect of short-term GPC treatment. However, long-term administration of GPC may exert cytotoxicity in a wide concentration range in cardiac myocytes. These results may draw attention to a comprehensive cardiac safety protocol for the testing of GPC.

INTRODUCTION

There are some limitations in the present study as this is the first study to investigate the effects of a broad concentration range of GPC on cardiac cells. Nevertheless, in vivo experiments would certainly supply further information regarding the functional cardiac effects of GPC. The mechanisms of action of GPC on cardiac cells are poorly characterized, and therefore it should be studied with multiple omics technologies in any depth.

In conclusion, in the present study, we have shown for the first time that choline donor L-Alpha-GPC (which is widely used as a food supplement and generally considered as safe for human use) had ambiguous effects on cardiac cells. It may be beneficial in short-term administration to maintain the physiological balance of ROS production under normoxic, healthy conditions and could be also protective in I/R conditions, but could, in fact, be cytotoxic if it surrounded the cells for long enough. Besides the duration of the treatment, the correct dosage can also be a crucial factor, as a fine-tuning effect seemed to occur in a small, but dietary-relevant concentration range. Thus (despite many limitations of this in vitro study), our results indicate the need for a comprehensive cardiac safety testing of GPC.

Dosage Notes

Alpha GPC is about 40% choline by weight. So 1,000 mg of Alpha GPC provides approximately 400 mg of choline.

• Alpha GPC suggested dosage for cognitive benefits is 400 – 1,200 mg per day.
• Athletic training suggested dosage of Alpha GPC is 400 mg first thing in the morning, and another 400 mg dose 15 – 30 minutes before working out.
• Clinical treatment of Alzheimer’s Disease, dementia and other cognitive disorders dosage of up to 1,200 mg per day.

For higher dosages, split the daily Alpha GPC total into 2 or 3 doses per day. For example, 1,200 mg would be taken 400 mg at a time.

References