Abstract

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.

Highlights

  • IntroductionAlpha-glycerylphosphorylcholine (choline alphoscerate, GPC) is a natural endogenously produced choline derivative and acetylcholine precursor in the brain which (in the form of a synthetic compound) is widely used as a food supplement [1]

  • Introduction lAlpha-glycerylphosphorylcholine is a natural endogenously produced choline derivative and acetylcholine precursor in the brain which is widely used as a food supplement [1]

  • The acute (15 min) treatment with different concentrations of GPC had no impact on the cell viability of Neonatal rat cardiac myocytes (NRCMs) in comparison to the vehicle control

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Summary

Introduction

Alpha-glycerylphosphorylcholine (choline alphoscerate, GPC) is a natural endogenously produced choline derivative and acetylcholine precursor in the brain which (in the form of a synthetic compound) is widely used as a food supplement [1]. It is converted metabolically to phosphatidylcholine, the active form of choline that is able to increase acetylcholine levels in the brain [2,3,4]. In terms of its use as a food/health supplement, oral GPC intake/supplementation has gained growing attention in both the media and in scientific areas. Since 1998, the Institute of Medicine of the National Academy of Sciences (USA) has recognized choline as an essential nutrient for humans and has made recommendations for the dietary choline intake (Institute of Medicine and National Academy of Sciences 1998). GPC contributes to the synthesis of membrane phospho- and glycerolipids, and positively influences membrane fluidity [4, 6]

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