Synthesis and evaluation of glycosylated quercetin to enhance neuroprotective effects on cerebral ischemia-reperfusion

文献类型： 外文期刊

第一作者： Wang, Siqi

作者： Wang, Siqi;Chen, Yuting;Yang, Chunyan;Hai, Li;Wu, Yong;Yang, Zhongzheng;Wang, Siqi;Chen, Yuting;Yang, Chunyan;Hai, Li;Wu, Yong;Yang, Zhongzheng;Xia, Chen;Chen, Jian

作者机构：

关键词： Quercetin; Glycosylation; Neuroprotection; Cerebral ischemia-reperfusion

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY （ 影响因子：3.461； 五年影响因子：3.364 ）

ISSN： 0968-0896

年卷期： 2022 年 73 卷

页码：

收录情况： SCI

摘要： Quercetin (Que), a polyphenolic flavonoid compound with antioxidant properties has been explicated to have neuroprotective effects on neuronal injury/neurodegenerative diseases. However, low water-solubility, instability and inability to cross the blood-brain barrier (BBB) imped its application. To enhance the neuroprotective effects and improve the potential application of quercetins as a nutraceutical or medicine, we designed and synthesized two types of glycosylated quercetins--Glu-Que and 2Glu-Que through click reaction. Glu-Que and 2Glu-Que improved the water solubility and stability of quercetin, as well as alleviating H2O2-induced neurotoxicity by increasing the cell viability of PC12 cells and reducing the ROS generation. What's more, glycosylated quercetins enhanced neuroprotective effects on cerebral ischemia-reperfusion (I/R). Among the two types of glycosylated quercetin, 2Glu-Que displayed higher neuroprotective potential than Glu-Que. In conclusion, the glycosylated quercetin 2Glu-Que, with better water solubility, bioavailability and brain-targeting ability, significantly enhanced the neuroprotective effects of quercetin, making it a promising nutraceutical or candidate drug in neuroprotection.

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