天然产物研究与开发 ›› 2021, Vol. 33 ›› Issue (1): 165-177.doi: 10.16333/j.1001-6880.2021.1.019

• 综述 • 上一篇    

Nrf2及天然产物导向的Nrf2激活剂研究进展

程茂军1,郭杰1,刘婧2,谢赛赛1,3*   

  1. 1江西中医药大学 中药固体制剂制造技术国家工程研究中心;2江西中医药大学药学院;3江西本草天工科技有限责任公司,南昌 330004
  • 出版日期:2021-01-28 发布日期:2021-01-28
  • 基金资助:
    国家自然科学基金 (81760622);江西省科技创新杰出青年人才培养计划(20192BCB 23018);江西省自然科学基金(20192ACBL21034);南昌市“双百计划”人才项目(20200729)

Research progress of Nrf2 and natural product-oriented Nrf2 activator

CHENG Mao-jun1,GUO Jie1,LIU Jing2,XIE Sai-sai1,3*   

  1. 1National Pharmaceutical Engineering Research Center for Solid Preparation in Chinese Herbal Medicine,Jiangxi University of Traditional Chinese Medicine;2School of Pharmacy,Jiangxi University of Traditional Chinese Medicine;3Jiangxi Herbfine Hi-tech Pharmaceutical Co.,Ltd.,Nanchang 330004,China

  • Online:2021-01-28 Published:2021-01-28

摘要: 氧化应激能够破坏细胞内氧化还原平衡,造成系统和组织损伤,最终引起一系列疾病的产生。转录因子E2相关因子2(Nrf2),受Kelch样环氧氯丙烷相关蛋白1(Keap1)蛋白的调控,是细胞氧化应激反应中的关键因子,在氧化应激条件下,Nrf2从Keap1中分离,然后进入细胞核与抗氧化反应元件(ARE)结合,增加了Ⅱ相解毒酶的表达,保护细胞免受氧化损伤。天然产物对于药物发现具有重要意义,研究显示,Nrf2激活剂绝大多数也是天然产物或天然产物的衍生物。本文介绍Nrf2-Keap1信号通路的作用机制以及常见的天然产物导向的Nrf2激活剂。


关键词: 氧化应激, 转录因子E2相关因子2, 激活剂, 天然产物, 衍生物

Abstract:

Oxidative stress can cause a series of diseases by destroying the oxidative balance in the cell and damaging the system or tissue.The nuclear factor erythroid 2 related factor 2 (Nrf2) regulated by Kelch-like ECH-associated protein 1 (Keap1) protein is a key factor in cellular oxidative stress response.To protect cells from oxidative damage,Nrf2 is separated from Keap1,which enters the nucleus and combines with the antioxidant response element (ARE),increasing the expression of phase Ⅱ detoxification enzyme.It is found that natural products are of great significance for drug research and development,and most of Nrf2 activators are also natural products or derivatives of natural products.This article describes the mechanism of action of the Nrf2-Keap1 signaling pathway and common natural product-oriented Nrf2 activators.

Key words: oxidative stress, Nrf2, activator, natural product, derivative

中图分类号:  R914 R96