摘要
槲皮素是一个典型的类黄酮,主要存在于日常食用的各种蔬菜、水果和中草药中,具有抗氧化、抗肿瘤、预防和治疗心脑血管疾病等作用。槲皮素是具有确定抗肿瘤活性的天然化合物,由于生物利用度低、水溶性差,限制了在临床上的应用。槲皮素的结构通过修饰,获得了溶解性好、生物利用度高、代谢稳定和毒副作用小的槲皮素衍生物。最近几年来,已经合成了大量槲皮素醚类、酯类、配合物、C-4羰基氧取代衍生物、A、B环修饰化合物及其他衍生物,并进行了体外抗癌活性检测。该文综述了最近5年合成的具有抗肿瘤活性的槲皮素衍生物。
Quercetin is a kind of typical flavonoid, mainly found in various vegetables, fruits and Chinese herbs that are consumed daily, with the functions of anti-oxidation, anti-tumor, prevention and treatment of cardiovascular and cerebrovascular diseases. Quercetin is a natural compound with defined anti-tumor activity. Due to its low bioavailability and poor water solubility, quercetin has limitations in clinical application. The quercetin derivatives with good solubility, high bioavailability, metabolic stability, and low toxicity have been obtained through modification of quercetin structure. In recent years, a large number of quercetin ethers, esters, complexes, C-4 carbonyloxy substituted derivatives, A,B-ring modified compounds and other derivatives have been synthesized and tested for in vitro anticancer activity. The quercetin derivatives with anti-tumor activity synthesized in the last 5 years were reviewed in this paper.
作者
冯亚莉
卢令攀
翟广玉
FENG Ya-li;LU Ling-pan;ZHAI Guang-yu(School of Pharmaceutical and Chemical Engineering,Zhengzhou Institute of Industrial Technology,Xinzheng 451150,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2020年第15期3565-3574,共10页
China Journal of Chinese Materia Medica
基金
郑州市高等学校名师技术技能工作室项目(郑教高[2015]70号)。
关键词
槲皮素
修饰
衍生物
醚
酯
配合物
抗肿瘤
quercetin
modification
derivative
ether
ester
complex
anti-tumor
