Non-genomic effects of ginsenoside-Re in endothelial cells via glucocorticoid receptor

Kar Wah Leung*, Fung Ping LEUNG, Yu Huang, Nai Ki MAK, Ricky N S WONG

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

46 Citations (Scopus)

Abstract

We demonstrated that ginsenoside-Re (Re), a pharmacological active component of ginseng, is a functional ligand of glucocorticoid receptor (GR) using competitive ligand-binding assay (IC50 = 156.6 nM; Kd = 49.7 nM) and reporter gene assay. Treatment with Re (1 μM) raises intracellular Ca2+ ([Ca2+]i) and nitric oxide (NO) levels in human umbilical vein endothelial cells as measured using fura-2 and 4-amino-5-methylamino-2′,7′-difluorofluorescein diacetate, respectively. Western blot analysis shows that Re increased phosphorylation of endothelial nitric oxide synthase. These effects were abolished by GR antagonist RU486, siRNA targeting GR, non-selective cation channel blocker 2-aminoethyldiphenylborate, or in the absence of extracellular Ca2+, indicating Re is indeed an agonistic ligand for the GR and the activated GR induces rapid Ca2+ influx and NO production in endothelial cells.

Original languageEnglish
Pages (from-to)2423-2428
Number of pages6
JournalFEBS Letters
Volume581
Issue number13
DOIs
Publication statusPublished - 29 May 2007

Scopus Subject Areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

User-Defined Keywords

  • Angiogenesis
  • Endothelial cell
  • Ginsenoside
  • Glucocorticoid receptor
  • Intracellular calcium concentration
  • Nitric oxide

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