Synthesis of novel EGCG-glucose conjugates and studies of their antioxidative properties for neuroprotections

文献类型： 外文期刊

第一作者： Lu, Jiaqi

作者： Lu, Jiaqi;Chen, Jinxia;Yang, Chunyan;Wu, Yong;Deng, Junling;Xiang, Zuoya;Chen, Jian;Wu, Yong

作者机构：

关键词： EGCG; Glucose conjugate; Brain target; Antioxidant; Neuroprotection

期刊名称：FOOD BIOSCIENCE （ 影响因子：5.318； 五年影响因子：5.846 ）

ISSN： 2212-4292

年卷期： 2022 年 49 卷

页码：

收录情况： SCI

摘要： Epigallocatechin-3-gallate (EGCG) is a polyphenol naturally sourced in green tea with extensive bioactivities, including antioxidant, anti-carcinogenic, anti-microbial, anti-obesity, and neuroprotection. However, EGCG is unstable in neutral or alkaline conditions and has poor lipid solubility, leading to inadequate systemic absorption, reduced pharmacokinetics, limited biodistribution, and first-pass metabolism. The aim of this study is to solve these problems, thus two novel EGCG-glucose conjugates, Glu-EGCG and 2Glu-EGCG possessing one and two glucose, respectively, were designed, synthesized, and characterized. The EGCG-glucose conjugates' chemical stability, cytotoxicity and alleviation H2O2-induced antioxidative damage to neuronal cell and anti -oxidative neuroprotection activities were examined. Compared with their precursor EGCG, Glu-EGCG and 2Glu-EGCG are more stable, less toxic to PC12 and bEnd.3 cell, stronger ability to attenuate H2O2-induced injury to PC12 cells resulting higher cell viability and lower reactive oxygen species (ROS) in the cell. Animal study results further proved that Glu-EGCG and 2Glu-EGCG possess higher antioxidative activities than EGCG, through decreasing the ischemia area, inhibiting morphological changes and neuronal loss in brain tissues, and modulating the oxidative factor and antioxidant factor. In conclusion, 2Glu-EGCG shows stronger antioxidant activities than Glu-EGCG does. Both EGCG-glucose conjugates are promising brain target antioxidative neuroprotection agents.

分类号：

  • 相关文献
作者其他论文 更多>>

微信小程序