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A New Palmitoylethanolamide Form Combined with Antioxidant Molecules to Improve Its Effectivess on Neuronal Aging.
Brain Sciences ( IF 2.7 ) Pub Date : 2020-07-17 , DOI: 10.3390/brainsci10070457
Vera Morsanuto 1 , Rebecca Galla 1 , Claudio Molinari 1 , Francesca Uberti 1
Affiliation  

Palmitoylethanolamide is a nutraceutical compound naturally produced in many plants and animal source foods, but the natural form is poorly water-soluble. It has demonstrated an anti-inflammatory role as a neuroprotective mediator, acting on several molecular targets of the central nervous system involved on brain aging process. In healthy adults, palmitoylethanolamide is an endogenous PPAR-α (peroxisome proliferator-activated receptor α) agonist through which it performs anti-inflammatory activity and provides its effects by activating the cannabinoid receptor. The different formulations of palmitoylethanolamide (micronized palmitoylethanolamide, FM-LipoMatrix® palmitoylethanolamide and FM-LipoMatrix® palmitoylethanolamide plus lipoic acid and vitamin D3) were analyzed starting from intestinal barrier, to verify their bioavailability, to in primary astrocytes in which cell viability, reactive oxygen species (ROS) and nitric oxide (NO) production, NFKB activity, MAPK, p53 and PPARα activities were investigated. Additionally, cannabinoid and estrogen receptors were analyzed using the western blot technique. The combination of palmitoylethanolamide in FM-LipoMatrix®, lipoic acid and vitamin D3 shows better absorption predicting an improvement on plasma concentration; this formulation also shows a reduction in ROS and NO production and the data show the interaction of palmitoylethanolamide with cannabinoids and estrogen receptors inhibiting neuroinflammatory markers. All these data support the hypothesis of a new potential strategy to restore brain function and slow down brain aging in humans.

中文翻译:

一种新的棕榈酰乙醇酰胺形式与抗氧化剂分子结合以改善其对神经元衰老的功效。

棕榈酰乙醇酰胺是许多植物和动物源食品中天然产生的营养化合物,但天然形式的水溶性差。它已显示出作为神经保护介质的抗炎作用,作用于与大脑衰老过程有关的中枢神经系统的多个分子靶标。在健康成年人中,棕榈酰乙醇酰胺是一种内源性PPAR-α(过氧化物酶体增殖物激活的受体α)激动剂,通过它执行抗炎活性并通过激活大麻素受体发挥作用。十六酰胺乙醇的不同制剂(微粉化的十六酰胺乙醇,FM-LipoMatrix ®十六酰胺乙醇和FM LipoMatrix ®从肠屏障开始分析棕榈酰乙醇酰胺加硫辛酸和维生素D3),以验证其生物利用度,直至原代星形胶质细胞的细胞存活率,活性氧(ROS)和一氧化氮(NO)产生,NFKB活性,MAPK,p53研究了PPARα的活性。此外,使用蛋白质印迹技术分析了大麻素和雌激素受体。棕榈酰的FM-LipoMatrix组合®,硫辛酸和维生素D3表现出更好的吸收,预示着血浆浓度的改善;该配方还显示出ROS和NO的产生减少,数据显示棕榈酰乙醇酰胺与大麻素和抑制神经炎性标志物的雌激素受体的相互作用。所有这些数据都支持一种新的潜在策略来恢复人类大脑功能并减缓人类大脑衰老的假说。
更新日期:2020-07-17
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