首页|槲皮素衍生物及其生物活性研究进展

槲皮素衍生物及其生物活性研究进展

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槲皮素是一种天然多酚,是多种植物性食品中发现最丰富的类黄酮类化合物之一.槲皮素是天然的抗氧化剂,可以保护细胞免受自由基造成的损害.槲皮素是一种亲脂性化合物,能够穿过细胞膜,调节众多与疾病进展、化学预防有关的细胞内和细胞外信号通路.槲皮素具有广泛的药理活性,抗炎、抗菌、抗癌和预防心脑血管疾病,但是它的低溶解度和生物利用度限制了其在临床上的应用.为了改善这些缺点,研究者对槲皮素进行了结构修饰,修饰羟基生成酯或者醚,修饰羰基生成腙或者羰基氧被取代的产物,8-位被取代的产物,与金属离子生成配合物等.对槲皮素的结构进行优化修饰获得了溶解性能好、生物利用度高、活性明显改善、抗癌活性增强的槲皮素衍生物.本研究综述了近年来槲皮素衍生物的研究进展,为槲皮素衍生物的进一步开发提供参考.
Research Progress on Quercetin Derivatives and Their Biological Activities
Quercetin,a natural polyphenol,is one of the most abundant flavonoids found in many plant foods.Quercetin is a natural antioxidant,which can protect cells from damage caused by free radicals.Quercetin is a lipophilic compound that can pass through the cell membrane and regulate many intracellular and extracellular signal pathways related to disease progression and chemoprevention.Quercetin has a wide range of pharmacological activities,anti-inflammatory,antibacterial,anti-cancer and prevention of cardiovascular and cerebrovascular diseases,but its low solubility and bioavailability limit its clinical application.In order to improve these drawbacks,people have carried out structural modifications on quercetin,such as modifying hydroxyl groups to generate esters or ethers,modifying carbonyl groups to generate hydrazone or carbonyl oxygen substituted products,8-substituted products,and forming complexes with metal ions.Quercetin derivatives with good solubility,high bioavailability,improved activity and enhanced anti-cancer activity were obtained by optimizing the structure of quercetin.The research progress of quercetin derivatives in recent years is reviewed to provide reference for the further development of quercetin derivatives.

quercetinderivativesanti-oxidationanti-inflammationanti-cancer

李珂、刘金海、翟广玉

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郑州工业应用技术学院药学与化学工程学院,郑州 451100

槲皮素 衍生物 抗氧化 抗炎 抗癌

2024

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子:0.957
ISSN:1001-2494
年,卷(期):2024.59(15)