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绿茶多酚(-)-表没食子儿茶素-3-没食子酸酯通过增加与血清白蛋白的亲和力增强石杉碱甲对乙酰胆碱酯酶的抑制作用。

Green tea polyphenol (-)-epigallocatechin-3-gallate enhances the inhibitory effect of huperzine A on acetylcholinesterase by increasing the affinity with serum albumin.

作者信息

Zhang Lei, Cao Hui, Wen Jun, Xu Ming

机构信息

Research Institute for Molecular Pharmacology and Therapeutics, Central South University, Changsha, Hunan, People's Republic of China.

出版信息

Nutr Neurosci. 2009 Aug;12(4):142-8. doi: 10.1179/147683009X423283.

Abstract

The green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) was investigated for its enhancement effect of huperzine A on inhibiting acetylcholinesterase (AChE). The inhibitory effect of huperzine A on acetylcholinesterase is quite weak in the whole phase. EGCG hardly inhibits the AChE activity within the range 10-300 mg/kg. However, upon addition of EGCG to the huperzine A groups, a remarkably enhanced inhibitory effect was observed. The EGCG also can largely prolong the inhibitory time. These results indicate that addition of EGCG to huperzine A can reduce the dose of huperzine A required compared with huperzine A alone. The enhancement and complementary effect of EGCG on huperzine A activity may partly be due to the antioxidant property of EGCG. One of the beneficial effects of green tea is to induce a feeling of relief. It is conceivable that this function may be regulated by EGCG in the central nervous system since EGCG is distributed in the brain after oral administration. EGCG can be used as an enhanced supplement for huperzine A to treat Alzheimer's disease.

摘要

研究了绿茶多酚(-)-表没食子儿茶素-3-没食子酸酯(EGCG)对石杉碱甲抑制乙酰胆碱酯酶(AChE)的增强作用。在整个阶段,石杉碱甲对乙酰胆碱酯酶的抑制作用相当弱。在10 - 300 mg/kg范围内,EGCG几乎不抑制AChE活性。然而,在石杉碱甲组中加入EGCG后,观察到抑制作用显著增强。EGCG还能大大延长抑制时间。这些结果表明,与单独使用石杉碱甲相比,在石杉碱甲中添加EGCG可以降低所需的石杉碱甲剂量。EGCG对石杉碱甲活性的增强和互补作用可能部分归因于EGCG的抗氧化特性。绿茶的有益作用之一是能带来舒缓的感觉。可以想象,由于口服后EGCG分布于大脑中,这种功能可能在中枢神经系统中由EGCG调节。EGCG可作为石杉碱甲的增强补充剂用于治疗阿尔茨海默病。

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