摘要
槲皮素广泛分布于植物、食物和饮料中,具有多种生理活性,如:抗氧化、抗癌、预防和治疗心脑血管疾病等。流行病学和营养学家认为:槲皮素是一种最有希望应用于疾病预防和治疗的天然化合物,但是因其生物利用度低、水溶性差、代谢迅速及酶降解等问题,使得槲皮素作为药物应用于临床受到了限制。因此,对槲皮素修饰、改性及修饰物的活性检测成为当前研究的热点,如:对槲皮素醚化、酰化、羰基取代、A和B环改性及形成金属配合物。综述了最近十年对槲皮素结构修饰得到具有抗癌活性的衍生物。
Quercetin is widely distributed in edible plants with many aspects of physiological activity such as anti-oxidation, anti-cancer, pre-vention and treatment of cardiovascular and cerebrovascular diseases. Epidemiologists and nutritionists consider that quercetin as the most promising natural compound for the prevention and treatment of diseases has been limited for clinical application because of low bioavailability, poor water solu-bility, rapid metabolism and enzyme degradation. Therefore, intense research efforts have been focused on modification structural and improvement na-ture of quercetin, as well as derivative activity detection. The modification of the quercetin includes O-alkylation, C-4 carbonyl replacement, O-acyla-tion, functionalization of A and B-rings and metal coordination. The developments in the synthesis and anticancer-related activities of quercetin derivatives reported in the last decades are summarized.
作者
李阳杰
张方瑞
冯亚莉
翟广玉
LI Yang-jie;ZHANG Fang-rui;FENG Ya-li;ZHAI Guang-yu(CoUege of Pharmacy and Chemical Engineering,Zhengzhou university of industrial technology,Xin Zheng 451100;School of Pharmacy,Zunyi Medical College,Zunyi 393003)
出处
《化学与粘合》
CAS
2018年第6期445-451,460,共8页
Chemistry and Adhesion
基金
2018年度郑州工业应用技术学院校级科研项目(编号:2018LX010)
关键词
槲皮素
槲皮素衍生物
抗癌
细胞增殖
多重耐药(MDR)
Quercetin
quercetin derivatives
anticancer
cell proliferation
multidrug resistance （MDR）
