Institute of Biological Chemistry and Nutrition, University of Hohenheim, Stuttgart, Germany.
Ageing Res Rev. 2012 Jan;11(1):163-80. doi: 10.1016/j.arr.2011.06.006. Epub 2011 Jul 7.
Tocotrienols (T(3)) belong to the family of vitamin E compounds (α-, β-, γ-, δ-tocopherols and -tocotrienols) and have unique biological properties that make them potential neuroprotective dietary factors. In addition to their antioxidant activity, T(3) at micromolar concentrations exert cholesterol-lowering activities in cells, animal models and some, but not all, human studies by means of inhibition of the activity of the rate-limiting enzyme in cholesterol biosynthesis, 3-hydroxy-3-methylglutaryl coenzyme A reductase. At lower concentrations (∼10 nmol/L), T(3) modulate signalling pathways involved in neuronal cell death in cell culture experiments. Targets of T(3) include prenyl transferases, non-receptor tyrosine kinase, phospholipase A(2), 12-lipoxygenase, cyclooxygenase-2, and nuclear factor κB. The low bioavailability and rapid excretion of T(3) represents a major hurdle in their preventive use. Fasting plasma concentrations, even after supplementation with high doses, are below 1 μmol/L. T(3) bioavailability may be enhanced by ingestion with a high-fat meal, self-emulsifying drug delivery systems, or phytochemicals that inhibit T(3) metabolism and excretion. T(3) have no known adverse effects when consumed as part of a normal diet and the studies reviewed here support the notion that they may have potential as neuroprotective agents. However, experiments in relevant animal models and randomised human intervention trials addressing the neuroprotection mediated by T(3) are scarce and, thus, highly warranted.
生育三烯酚(T(3))属于维生素 E 化合物(α-、β-、γ-、δ-生育酚和生育三烯酚)家族,具有独特的生物学特性,使其成为有潜力的神经保护膳食因子。除了抗氧化活性外,T(3)在微摩尔浓度下通过抑制胆固醇生物合成限速酶 3-羟-3-甲基戊二酰辅酶 A 还原酶的活性,在细胞、动物模型和一些(但不是全部)人体研究中发挥降低胆固醇的作用。在较低浓度(∼10 nmol/L)下,T(3)在细胞培养实验中调节涉及神经元细胞死亡的信号通路。T(3)的靶标包括prenyl 转移酶、非受体酪氨酸激酶、磷脂酶 A(2)、12-脂氧合酶、环氧化酶-2 和核因子 κB。T(3)的低生物利用度和快速排泄是其预防性使用的主要障碍。即使补充高剂量,空腹血浆浓度仍低于 1 μmol/L。T(3)的生物利用度可以通过与高脂肪餐一起摄入、自乳化药物递送系统或抑制 T(3)代谢和排泄的植物化学物质来增强。当作为正常饮食的一部分摄入时,T(3)没有已知的不良反应,这里回顾的研究支持这样一种观点,即它们可能具有作为神经保护剂的潜力。然而,与 T(3)介导的神经保护相关的相关动物模型和随机人类干预试验的实验很少,因此非常有必要进行这些实验。