Drug Design, Development and Therapy (Feb 2020)

Focus on Notoginsenoside R1 in Metabolism and Prevention Against Human Diseases

  • Liu H,
  • Yang J,
  • Yang W,
  • Hu S,
  • Wu Y,
  • Zhao B,
  • Hu H,
  • Du S

Journal volume & issue
Vol. Volume 14
pp. 551 – 565

Abstract

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Hai Liu,1,2 Jianqiong Yang,3 Wanqing Yang,1 Shaonan Hu,1 Yali Wu,1 Bo Zhao,1 Haiyan Hu,1 Shouying Du1 1School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, People’s Republic of China; 2College of Pharmacy, Gannan Medical University, Ganzhou, Jiangxi, People’s Republic of China; 3Department of Clinical Research Center, The First Affiliated Hospital of Gannan Medical University, Ganzhou, Jiangxi, People’s Republic of ChinaCorrespondence: Shouying DuSchool of Chinese Materia Medica, Beijing University of Chinese Medicine, 11 North 3rd Ring East Road, Chaoyang District, Beijing, People’s Republic of ChinaTel +86 17812165051Fax +86 10 64286231Email [email protected]: Notoginsenoside (NG)-R1 is one of the main bioactive compounds from Panax notoginseng (PN) root, which is well known in the prescription for mediating the micro-circulatory hemostasis in human. In this article, we mainly discuss NG-R1 in metabolism and the biological activities, including cardiovascular protection, neuro-protection, anti-diabetes, liver protection, gastrointestinal protection, lung protection, bone metabolism regulation, renal protection, and anti-cancer. The metabolites produced by deglycosylation of NG-R1 exhibit higher permeability and bioavailability. It has been extensively verified that NG-R1 may ameliorate ischemia-reperfusion (IR)-induced injury in cardiovascular and neuronal systems mainly by upregulating the activity of estrogen receptor α-dependent phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) and nuclear factor erythroid-2-related factor 2 (NRF2) pathways and downregulating nuclear factor-κB (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. However, no specific targets for NG-R1 have been identified. Expectedly, NG-R1 has been used as a main bioactive compound in many Traditional Chinese Medicines clinically, such as Xuesaitong, Naodesheng, XueShuanTong, ShenMai, and QSYQ. These suggest that NG-R1 exhibits a significant potency in drug development.Keywords: notoginsenoside (NG)-R1, Panax notoginseng, micro-circulatory hemostasis, permeability, bioavailability

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