·1636·中草药2023年3月第54卷第5期ChineseTraditionalandHerbalDrugs2023MarchVol.54No.5槲皮素的结构修饰及生物活性研究进展李阳杰，曹瑞梅，毛雅君，邵香敏，冯亚莉，翟广玉*郑州工业应用技术学院药学与化学工程学院，河南郑州450041摘要：槲皮素是蔬菜、水果、中药中常见的黄酮类化合物，是天然的抗氧化剂，具有抗癌、抗糖尿病、抗菌、抗炎、抗病毒等生物活性。由于槲皮素生物利用度低，限制了其在临床上的应用。通过各种方法设计和合成新的槲皮素衍生物，以改善其缺点，进而发挥预防和治疗疾病的作用。通过对槲皮素衍生物的合成及其抗癌、抗糖尿病、抗炎、抗菌和抗病毒活性进行综述，并对其构效关系进行分析，为天然化合物的开发和利用奠定基础。关键词：槲皮素；羟基修饰；羰基修饰；衍生物；抗癌；抗糖尿病；构效关系中图分类号：R282.710.85文献标志码：A文章编号：0253-2670(2023)05-1636-18DOI:10.7501/j.issn.0253-2670.2023.05.030ResearchprogressonstructuralmodificationandbiologicalactivityofquercetinLIYang-jie,CAORui-mei,MAOYa-jun,SHAOXiang-min,FENGYa-li,ZHAIGuang-yuSchoolofPharmacyandChemicalEngineering,ZhengzhouInstituteofTechnology,Zhengzhou450041,ChinaAbstract:Quercetinisacommonflavonoidfoundinvegetables,fruitsandtraditionalChinesemedicine.Itisanaturalantioxidantwithanti-cancer,anti-diabetes,antibacterial,anti-inflammatory,anti-virusandotherbiologicalactivities.Thelowbioavailabilityofquercetinlimitsitsclinicalapplication.Newquercetinderivativesweredesignedandsynthesizedbyvariousmethodstoimprovetheirshortcomingsandthusplayaroleinthepreventionandtreatmentofdiseases.Byreviewingthesynthesisandanti-cancer,anti-diabetes,anti-inflammatory,antibacterialandantiviralactivitiesofquercetinderivatives,andanalyzingtheirstructure-activityrelationship,welayafoundationforthedevelopmentandutilizationofnaturalcompounds.Keywords:quercetin;hydroxylmodification;carbonylmodification;derivatives;anticancer;antidiabetic;structure-activityrelationship槲皮素为广泛存在于蔬菜（番茄、甘蓝、芦笋等）、水果（苹果、杏、草莓等）、中药（槐米、绞股蓝、银杏叶等）中的黄酮类化合物[1-2]，具有抗氧化、抗炎、降糖、抗癌、预防和治疗心脑血管疾病等药理作用[3-10...
