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 language | English |
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Pages (from-to) | 2423-2428 |
Number of pages | 6 |
Journal | FEBS Letters |
Volume | 581 |
Issue number | 13 |
DOIs | |
Publication status | Published - 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