Laboratory of Neurophysiology, GIGA Neurosciences, University of Liège, 4000 Liège, Belgium.
Int J Mol Sci. 2023 Jul 10;24(14):11296. doi: 10.3390/ijms241411296.
Thiamine (vitamin B1) is essential for the brain. This is attributed to the coenzyme role of thiamine diphosphate (ThDP) in glucose and energy metabolism. The synthetic thiamine prodrug, the thioester benfotiamine (BFT), has been extensively studied and has beneficial effects both in rodent models of neurodegeneration and in human clinical studies. BFT has no known adverse effects and improves cognitive outcomes in patients with mild Alzheimer's disease. In cell culture and animal models, BFT has antioxidant and anti-inflammatory properties that seem to be mediated by a mechanism independent of the coenzyme function of ThDP. Recent in vitro studies show that another thiamine thioester, O,S-dibenzoylthiamine (DBT), is even more efficient than BFT, especially with respect to its anti-inflammatory potency, and is effective at lower concentrations. Thiamine thioesters have pleiotropic properties linked to an increase in circulating thiamine concentrations and possibly in hitherto unidentified open thiazole ring derivatives. The identification of the active neuroprotective metabolites and the clarification of their mechanism of action open extremely promising perspectives in the field of neurodegenerative, neurodevelopmental, and psychiatric conditions. The present review aims to summarize existing data on the neuroprotective effects of thiamine thioesters and give a comprehensive account.
硫胺素（维生素 B1）对大脑至关重要。这归因于硫胺素二磷酸（ThDP）在葡萄糖和能量代谢中的辅酶作用。合成的硫胺素前药，硫代酯苯磷汀（BFT）已被广泛研究，并在神经退行性变的啮齿动物模型和人类临床研究中均具有有益作用。BFT 没有已知的不良反应，并改善轻度阿尔茨海默病患者的认知结果。在细胞培养和动物模型中，BFT 具有抗氧化和抗炎特性，这些特性似乎通过与 ThDP 辅酶功能无关的机制介导。最近的体外研究表明，另一种硫胺素硫代酯，O，S-二苯甲酰硫胺素（DBT）比 BFT 更有效，尤其是在抗炎效力方面，并且在较低浓度下有效。硫胺素硫代酯具有与循环硫胺素浓度增加相关的多效性特性，并且可能与以前未知的开噻唑环衍生物有关。活性神经保护代谢物的鉴定及其作用机制的阐明为神经退行性、神经发育和精神疾病领域开辟了极其有前景的前景。本综述旨在总结硫胺素硫代酯的神经保护作用的现有数据并进行全面说明。
