Synthesis and evaluation of glycosylated quercetin to enhance neuroprotective effects on cerebral ischemia-reperfusion
文献类型： 外文期刊
作者： Wang, Siqi 1 ; Chen, Yuting 1 ; Xia, Chen 3 ; Yang, Chunyan 1 ; Chen, Jian 3 ; Hai, Li 1 ; Wu, Yong 1 ; Yang, Zhongzheng 1 ;
作者机构： 1.Sichuan Univ, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst, Educ Minist & Sichuan Prov,Sichuan Engn Lab Plant, Chengdu 610041, Peoples R China
2.Sichuan Univ, West China Sch Pharm, Sichuan Res Ctr Drug Precis Ind Technol, Chengdu 610041, Peoples R China
3.Sichuan Acad Agr Sci, Inst Agro Prod Proc Sci & Technol, Chengdu 610066, Peoples R China
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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