Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine of University of Electronic Science and Technology of China, No. 32 West Second Section First Ring Road, Chengdu, 610072, P. R. China.
Department of Hematology, Miller School of Medicine, University of Miami, Miami, 33136, USA.
Chem Biodivers. 2019 Nov;16(11):e1900400. doi: 10.1002/cbdv.201900400. Epub 2019 Oct 10.
The Keap1-Nrf2/ARE signaling pathway is an important defense system against exogenous and endogenous oxidative stress injury. The dysregulation of the signaling pathway is associated with many diseases, such as cancer, diabetes, and respiratory diseases. Over the years, a wide range of natural products has provided sufficient resources for the discovery of potential therapeutic drugs. Among them, polyphenols possess Nrf2 activation, not only inhibit the production of ROS, inhibit Keap1-Nrf2 protein-protein interaction, but also degrade Keap1 and regulate the Nrf2 related pathway. In fact, with the continuous improvement of natural polyphenols separation and purification technology and further studies on the Keap1-Nrf2 molecular mechanism, more and more natural polyphenols monomer components of Nrf2 activators have been gradually discovered. In this view, we summarize the research status of natural polyphenols that have been found with apparent Nrf2 activation and their action modes. On the whole, this review may guide the design of novel Keap1-Nrf2 activator.
Keap1-Nrf2/ARE 信号通路是对抗外源和内源氧化应激损伤的重要防御系统。该信号通路的失调与许多疾病有关，如癌症、糖尿病和呼吸道疾病。多年来，广泛的天然产物为发现潜在的治疗药物提供了充足的资源。其中，多酚类物质具有 Nrf2 激活作用，不仅抑制 ROS 的产生，抑制 Keap1-Nrf2 蛋白-蛋白相互作用，还能降解 Keap1 并调节 Nrf2 相关通路。事实上，随着天然多酚分离纯化技术的不断提高和对 Keap1-Nrf2 分子机制的进一步研究，越来越多的天然多酚单体成分作为 Nrf2 激活剂逐渐被发现。有鉴于此，我们总结了目前已发现的具有明显 Nrf2 激活作用及其作用模式的天然多酚类物质的研究现状。总的来说，这篇综述可能有助于设计新型的 Keap1-Nrf2 激活剂。
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