Safety assessment of AGPC as a food ingredient

Safety assessment of AGPC as a food ingredient
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DOI:
10.1016/j.fct.2011.03.012
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发表时间:
2011-06-01
影响因子:
4.3
通讯作者:
Montesano, Federica
Montesano, Federica
中科院分区:
农林科学2区
文献类型:
--
作者:
Brownawell, Amy M.;Carmines, Edward L.;Montesano, Federica

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α-甘油磷酸胆碱(AGPC)是卵磷脂的半合成衍生物。口服给药后,它被转化为磷脂酰胆碱,这是一种代谢活性形式的胆碱,能够到达胆碱能突触末梢,在那里它增加乙酰胆碱的合成和释放。进行了一系列研究以证明AGPC的安全性。大鼠和小鼠的口服LD 50等于或大于10,000 mg/kg。有些动物在死亡前出现惊厥。给犬给予高达3000 mg/kg AGPC仅导致活动减少。大鼠(高达1000 mg/kg/天)和比格犬(高达300 mg/kg/天)的亚慢性和慢性经口毒性研究产生的症状主要包括活动减少;摄食量和体重增量略有下降;肝脏重量略有下降,同时血浆甘油三酯、胆红素和碱性磷酸酶显着下降。无组织病理学相关性。体内和体外试验清楚地表明AGPC没有致突变活性。根据这些结果,AGPC在体外或体内均无遗传毒性,急性经口毒性较低,经口接触26周后的口服NOAEL为150 mg/kg bw/天。(C)2011爱思唯尔有限公司保留所有权利。
alpha-Glycerylphosphorylcholine (AGPC) is a semi-synthetic derivative of lecithin. Following oral administration, it is converted to phosphatidylcholine, a metabolically active form of choline that is able to reach cholinergic synaptic endings where it increases acetylcholine synthesis and release. A series of studies were conducted to demonstrate the safety of AGPC. The oral LD50 was equal to or greater than 10,000 mg/kg in rats and mice. Deaths were preceded by convulsions in some animals. Dosing of dogs with up to 3000 mg/kg AGPC resulted only in reduced activity. Sub-chronic and chronic oral toxicity studies in rats (up to 1000 mg/kg/day) and beagles (up to 300 mg/kg/day) produced symptomology primarily consisting of reduced activity; slight decreases in food consumption and body weight gain; and slight reduction in liver weight, paralleled by significant decreases in plasma triglycerides, bilirubin, and alkaline phosphatase. There were no histopathological correlates. The in vivo and in vitro assays clearly indicated that AGPC was devoid of mutagenic activity. Based on these results, AGPC is not genotoxic in vitro or in vivo, exhibits low acute oral toxicity and, has an oral NOAEL of 150 mg/kg bw/day following 26 weeks oral exposure. (C) 2011 Elsevier Ltd. All rights reserved.