Ginsenoside-Rg1, one of the major active molecules from Panax ginseng, is a functional ligand of glucocorticoid receptor.
We have examined the possibility that a component of Panax ginseng, ginsenoside-Rg1 (G-Rg1), acts by binding to the glucocorticoid receptor (GR). G-Rg1 competed for [3H]dexamethasone (Dex) binding to GR with a specific affinity of 1-10 microM and activated a glucocorticoid responsive element-containing luciferase reporter gene. The dose-dependence patterns of G-Rg1 and Dex for these two effects were nearly identical, although two to three orders of magnitude higher concentration of G-Rg1 than that of Dex was required for the same magnitude of response. At the cellular level, the growth of FT02B cells was suppressed by G-Rg1 as well as by Dex, each of whose effects were abolished by RU486. These results demonstrate that G-Rg1 is a functional ligand of GR.
Lee
Y J
YJ
College of Pharmacy, Seoul National University, South Korea.
Chung
E
E
Lee
K Y
KY
Lee
Y H
YH
Huh
B
B
Lee
S K
SK
D000818:Animals; D001667:Binding, Competitive; D006528:Carcinoma, Hepatocellular; D002455:Cell Division; D003907:Dexamethasone / Q000378:metabolism; D036145:Ginsenosides; D005938:Glucocorticoids / Q000037:antagonists & inhibitors / Q000378:metabolism; D008024:Ligands; D015735:Mifepristone / Q000494:pharmacology; D005894:Panax / Q000737:chemistry*; D010946:Plants, Medicinal; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000378:metabolism*; D011993:Recombinant Fusion Proteins; D012503:Saponins / Q000378:metabolism* / Q000494:pharmacology; D015533:Transcriptional Activation / Q000187:drug effects / Q000502:physiology*; D014407:Tumor Cells, Cultured
D036145:Ginsenosides; D005938:Glucocorticoids; D008024:Ligands; D011965:Receptors, Glucocorticoid; D011993:Recombinant Fusion Proteins; D012503:Saponins; D015735:Mifepristone; D003907:Dexamethasone; C035054:ginsenoside Rg1