Ginsenoside-Rg1, one of the major active molecules from Panax ginseng, is a functional ligand of glucocorticoid receptor

Lee, Young‐Joo; Chung, Eunah; Lee, Kwang Youl; Lee, Yong Hee; Huh, Bin; Lee, Seung Ki

doi:10.1016/s0303-7207(97)00160-3

Cited by 175 publications

(110 citation statements)

References 19 publications

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“…GR nuclear translocation is required for the physiological and pharmacological functions of GCs. Although no direct evidence for Rg1 binding to GR was reported in this study, our results clearly demonstrate that Rg1 induces nuclear translocation of GR in RAW264.7 and A549 cells, in accordance with previous studies that report Rg1 to be a functional ligand of GR in which a reporter gene and competitive binding methods were used (34)(35)(36).…”

Section: Discussionsupporting

confidence: 92%

“…Even though Rg1 was reported as a functional ligand of GR (34)(35)(36) and demonstrated to drive GR into nucleus, it seems that Rg1 exhibits an altered gene regulation profile, able to affect only a subset of the genes normally regulated by GCs. Our results in this study demonstrate that Rg1 does not impair proliferation or differentiation of osteoblasts, as is the case with DEX.…”

Section: Discussionmentioning

confidence: 99%

“…Previous studies have demonstrated that ginsenoside Rg1 is a functional GR ligand (34). The fact that the transcriptional activity of NF-kB can also be modulated by different kinases, and that Rg1 treatment resulted in an efficient downregulation of MAPK phosphorylation, led us to ask whether Rg1 possesses inhibitory effects on NF-kB in a GR-dependent manner or other kinases.…”

Section: Anti-inflammatory Effect Of Ginsenoside Rg1 Is Gr-dependentmentioning

confidence: 99%

“…Among the ginsenosides, Rg1 is the most abundant and is the active ingredient of P. ginseng (32,33). Previous studies have shown Rg1 to be a functional ligand of GR (34)(35)(36). Furthermore, Rg1 inhibits LPS-stimulated cytokine production in vitro, indicating that Rg1 may exerts anti-inflammatory effects via GR (37,38).…”

mentioning

confidence: 99%

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Ginsenoside Rg1, a Novel Glucocorticoid Receptor Agonist of Plant Origin, Maintains Glucocorticoid Efficacy with Reduced Side Effects

Cheng

Zhu

et al. 2011

The Journal of Immunology

102

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Glucocorticoids (GCs) are widely used to treat inflammatory diseases. However, they cause debilitating side effects, which limit the use of these compounds. In the past decade, many researchers have attempted to find so-called dissociated GCs that have separate distinct transactivation and transrepression activities. Anti-inflammation of GCs is a result of glucocorticoid receptor (GR)-mediated transactivation and transrepression in some tissues, similar to their side effects; therefore, the goal to discover a compound that has anti-inflammatory properties, but lacks the negative side effects seen with GCs, has yet to be achieved. In the present study, we introduce a plant-derived compound, ginsenoside Rg1, which possesses GC and estrogen-like activities. In this study, we show that Rg1 downmodulates LPS-induced proinflammatory cytokine release and inhibits NF-κB nuclear translocation and DNA binding activity. The negative effects on NF-κB activation are due to a decrease in IκB phosphorylation and protein stabilization. Furthermore, the inhibitory effect of Rg1 on NF-κB is GR-dependent, as small interfering RNA knockdown of GR abrogated this function. Rg1 also displayed profound inhibitory effects on LPS-induced MAPK activation. Importantly, Rg1 did not impair proliferation or differentiation of mouse osteoblasts. Finally, we show that Rg1 can effectively inhibit acute and chronic inflammation in vivo, but it does not cause hyperglycemia or osteoporosis as seen with dexamethasone. These results suggest that ginsenoside Rg1 may serve as a novel anti-inflammatory agent and may exhibit a potential profile for therapeutic intervention in inflammatory diseases.

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Section: Discussionsupporting

confidence: 92%

Section: Discussionmentioning

confidence: 99%

Section: Anti-inflammatory Effect Of Ginsenoside Rg1 Is Gr-dependentmentioning

confidence: 99%

mentioning

confidence: 99%

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Ginsenoside Rg1, a Novel Glucocorticoid Receptor Agonist of Plant Origin, Maintains Glucocorticoid Efficacy with Reduced Side Effects

Cheng

Zhu

et al. 2011

The Journal of Immunology

102

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“…Ginsenosides isolated from P. ginseng reportedly serve as functional ligands of glucocorticoid receptors (1), regulate the induction of tyrosine amino transferase gene transcription (2), and potentiate NO-mediated neurogenic vasodilatation (3). In addition, oligopeptides of Panax bind metals (4) and have a somnogenic effect (5).…”

Section: Introductionmentioning

confidence: 99%