Fucoxanthin, a Marine Carotenoid, Reverses Scopolamine-Induced Cognitive Impairments in Mice and Inhibits Acetylcholinesterase in Vitro.
Fucoxanthin, a Marine Carotenoid, Reverses Scopolamine-Induced Cognitive Impairments in Mice and Inhibits Acetylcholinesterase in Vitro.
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岩藻黄质是一种海洋类胡萝卜素，可逆转东莨菪碱引起的小鼠认知障碍并在体外抑制乙酰胆碱酯酶
DOI：
10.3390/md14040067
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发表时间：
2016-03-25
期刊：
影响因子：
5.4
通讯作者：
Wang Q
中科院分区：
文献类型：
--
作者：
Lin J;Huang L;Yu J;Xiang S;Wang J;Zhang J;Yan X;Cui W;He S;Wang Q
褐藻黄质是一种天然胡萝卜素，富含在可食用的棕色海藻中，已被证明具有抗癌、抗氧化、抗肥胖和抗糖尿病的作用。在这项研究中，我们第一次报道了岩藻黄质有效地保护小鼠免受东莨菪碱诱导的认知障碍。此外，岩藻黄质还能显著逆转东莨菪碱诱导的乙酰胆碱酯酶(AChE)活性升高，降低胆碱乙酰转移酶活性和脑源性神经营养因子(BDNF)的表达。通过体外AChE活性测定，我们发现岩藻黄质直接抑制AChE，IC50值为81.2μM。分子对接分析表明，岩藻黄质可能与AChE内的外周阴离子位置相互作用，这与岩藻黄质以非竞争性方式抑制AChE的酶活性结果一致。根据我们目前的发现，我们预计岩藻黄质通过作用于多个靶点，包括抑制AChE和增加BDNF的表达，可能对阿尔茨海默病具有很好的治疗效果。
Fucoxanthin, a natural carotenoid abundant in edible brown seaweeds, has been shown to possess anti-cancer, anti-oxidant, anti-obesity and anti-diabetic effects. In this study, we report for the first time that fucoxanthin effectively protects against scopolamine-induced cognitive impairments in mice. In addition, fucoxanthin significantly reversed the scopolamine-induced increase of acetylcholinesterase (AChE) activity and decreased both choline acetyltransferase activity and brain-derived neurotrophic factor (BDNF) expression. Using an in vitro AChE activity assay, we discovered that fucoxanthin directly inhibits AChE with an IC50 value of 81.2 μM. Molecular docking analysis suggests that fucoxanthin likely interacts with the peripheral anionic site within AChE, which is in accordance with enzymatic activity results showing that fucoxanthin inhibits AChE in a non-competitive manner. Based on our current findings, we anticipate that fucoxanthin might exhibit great therapeutic efficacy for the treatment of Alzheimer’s disease by acting on multiple targets, including inhibiting AChE and increasing BDNF expression.