天然产物研究与开发 ›› 2024, Vol. 36 ›› Issue (3): 540-553.doi: 10.16333/j.1001-6880.2024.3.017

• 综述 • 上一篇    

二氢杨梅素结构修饰及生物活性研究进展

吴   聪1，王文茂3，彭彩云1,2*，盛文兵1,2*   

  1. 1湖南中医药大学 药学院；2湖南中医药大学 中医药民族医药创新发展国际实验室，长沙 410208；3湖南乾坤生物科技有限公司 张家界莓茶工程技术研究中心，张家界427000
  • 出版日期:2024-03-20 发布日期:2024-03-20
  • 基金资助:
    湖南省自然科学基金面上项目（2021JJ30502）；湖南教育厅科研项目重点项目（21A0239）；湖南中医药大学科研基金一般项目（2020XJJJ014）；湖南省天然药物资源与功能实验室开放基金一般项目（2022ZYYGN01）

Research advances of the structural modification and biological activity of dihydromyricetin

WU Cong1,WANG Wen-mao3,PENG Cai-yun1,2*,SHENG Wen-bing1,2*   

  1. 1School of Pharmacy,Hunan University of Chinese Medicine;2TCM and Ethnomedicine Innovation and Development International Laboratory,Hunan University of Chinese Medicine,Changsha 410208,China;3Zhangjiajie Meicha Technology Research Center,Hunan Qiankun Biotechnology Co.,Ltd.,Zhangjiajie 427000,China
  • Online:2024-03-20 Published:2024-03-20

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摘要：

二氢杨梅素是一种二氢黄酮醇，具有抗菌、抗炎、抗肿瘤以及保肝护肝等多种生物活性。由于其结构中的6个羟基导致其脂溶性差及生物利用度低，因此对其进行结构修饰以期提高生物利用度和生物活性。本文综述了二氢杨梅素的化学法结构修饰及其生物活性等研究工作，化学修饰方法涉及醚化反应、酯化反应和金属配合物等方法，合成的衍生物具有抗病毒、抗菌、抗氧化、神经保护以及抑制肿瘤细胞增殖等活性，并且提出二氢杨梅素结构修饰过程中存在的挑战及发展方向，为更好地开发二氢杨梅素衍生物提供技术服务。

关键词: 黄酮, 二氢杨梅素, 结构修饰, 生物活性

Abstract:

Dihydromyricetin is a kind of flavanonol,which possesses a variety of biological activities such as antibacterial,anti-inflammatory,anti-tumor and liver protection.The six hydroxyl groups in structure lead to its poor lipid solubility and low bioavailability,and it is expected to improve its bioavailability and biological activity by structural modification.In this paper,we reviewed studies on the structural modification of dihydromyricetin and the biological activities of corresponding derivatives.The chemical modification methods involve etherification reactions,esterification reactions and metal complexe formation,and the derivatives of dihydromyricetin have antiviral,antibacterial,antioxidant,neuroprotection and antitumor activities.Then the challenges arising from the structural modification of dihydromyricetin and the development directions are presented.Further efforts on more thoughtful structural modification are necessary to improve both biological activity and druggability.

Key words: flavone, dihydromyricetin, structural modification, biological activity

中图分类号:  R914

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