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[槲皮素衍生物抗肿瘤活性的研究进展]

[Research progress on antitumor activity of quercetin derivatives].

作者信息

Feng Ya-Li, Lu Ling-Pan, Zhai Guang-Yu

机构信息

School of Pharmaceutical and Chemical Engineering, Zhengzhou Institute of Industrial Technology Xinzheng 451150, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2020 Aug;45(15):3565-3574. doi: 10.19540/j.cnki.cjcmm.20200428.602.

Abstract

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.

摘要

槲皮素是一种典型的黄酮类化合物,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、防治心脑血管疾病等功能。槲皮素是一种具有明确抗肿瘤活性的天然化合物。由于其生物利用度低、水溶性差,槲皮素在临床应用中存在局限性。通过对槲皮素结构进行修饰,已获得了具有良好溶解性、高生物利用度、代谢稳定性和低毒性的槲皮素衍生物。近年来,已合成了大量的槲皮素醚、酯、配合物、C-4羰基氧基取代衍生物、A、B环修饰化合物等衍生物,并对其体外抗癌活性进行了测试。本文综述了近5年合成的具有抗肿瘤活性的槲皮素衍生物。

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