2. Academic Validation
  3. Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs

Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs

  • Bioorg Med Chem Lett. 2023 Sep 7:95:129468. doi: 10.1016/j.bmcl.2023.129468.
Juan Zhang 1,  Yong-Si Cai 1,  Hua-Long Ji 1,  Mengqi Ma 1,  Jin-He Zhang 1,  Zhi-Qiang Cheng 1,  Kai-Ming Wang 1,  Cheng-Shi Jiang 2,  Chunlin Zhuang 3,  Yang Hu 4,  Ning Meng 5
Affiliations

Affiliations

  • 1 School of Biological Science and Technology, University of Jinan, Jinan 250022, China.
  • 2 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: bio_jiangcs@ujn.edu.cn.
  • 3 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: zclnathan@163.com.
  • 4 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: mls_huy@ujn.edu.cn.
  • 5 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: mls_mengn@ujn.edu.cn.
PMID: 37689216 DOI: 10.1016/j.bmcl.2023.129468
Abstract

One effective strategy for treating atherosclerosis is to inhibit the injury of vascular endothelial cells (VECs) induced by oxidized low-density lipoprotein (oxLDL) and high glucose (HG). This study synthesized and evaluated a series of novel Nrf2 activators derived from the marine natural product phidianidine for their ability to protect human umbilical VECs against oxLDL- and HG-induced injury. The results of in vitro bioassays demonstrated that compound D-36 was the most promising Nrf2 activator, effectively inhibiting the Apoptosis of HUVECs induced by oxLDL and HG. Furthermore, Nrf2 knockdown experiments confirmed that compound D-36 protected against oxLDL- and HG-induced Apoptosis in HUVECs by activating the Nrf2 pathway. These findings provide important insights into a new chemotype of marine-derived Nrf2 activators that could potentially be optimized to develop effective anti-atherosclerosis agents.

Keywords

High glucose; Nrf2 activator; Phidianidine B; Vascular endothelial cell; oxLDL.

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