槲皮素衍生物的合成研究进展
收稿日期: 2022-03-06
修回日期: 2022-04-16
网络出版日期: 2022-07-05
基金资助
郑州市高等学校名师技术技能工作室([2015]70)
Research Progress on the Synthesis of Quercetin Derivatives
Received date: 2022-03-06
Revised date: 2022-04-16
Online published: 2022-07-05
Supported by
Technical Skills Studio of Famous Teachers in Zhengzhou Colleges and Universities([2015]70)
槲皮素是天然的抗氧化剂, 主要存在于蔬菜、水果等植物中, 可调节众多与疾病进展有关的细胞内外信号通路, 能抗炎、抗病毒、抗癌、预防和治疗心脑血管疾病等, 具有广泛的药理活性. 由于槲皮素的结构特征, 其生物利用度低, 限制了其在临床上的应用. 然而, 槲皮素的低分子质量和易修饰的化学基团, 使其具有药物开发的潜力. 因此, 研究人员通过各种方法设计合成新的槲皮素衍生物, 以改善其不利因素, 已经合成了许多性能优良、溶解性能好、生物利用度高、代谢稳定、毒副作用小且生物活性显著的槲皮素衍生物. 综述了近年来槲皮素衍生物的合成及其生物活性研究进展, 为槲皮素衍生物的进一步开发提供参考.
毛雅君 , 邵香敏 , 李阳杰 , 曹瑞梅 , 冯亚莉 , 翟广玉 . 槲皮素衍生物的合成研究进展[J]. 有机化学, 2022 , 42(11) : 3588 -3605 . DOI: 10.6023/cjoc202203016
Quercetin, as a natural antioxidant, is mainly found in vegetables, fruits and other plants. It can regulate many intracellular and extracellular signaling pathways related to disease progression. It can be anti-inflammatory, antiviral, anticancer, prevention and treatment of cardiovascular and cerebrovascular diseases, thus has a wide range of pharmacological activities. Due to the structural characteristics of quercetin, its low bioavailability limits its clinical application. However, the low molecular mass and easily modifiable chemical groups of quercetin make it attractive for drug development. Therefore, researchers have designed and synthesized new quercetin derivatives through various methods to improve its unfavorable factors. Many quercetin derivatives with excellent properties, good solubility, high bioavailability, stable metabolism, low toxicity and significant biological activity have been synthesized. The recent progress in the synthesis of quercetin derivatives and their biological activities is reviewed, providing a reference for the further development of quercetin derivatives.
Key words： quercetin; derivative; synthesis; antioxidant; anticancer; biological activity
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