Key result
Ginsenoside Rg5 promotes angiogenesis and vasorelaxation by acting as an IGF-1 receptor agonist.
Ginsenoside Rg5 promotes therapeutic angiogenesis and vasorelaxation through specific activation of the IGF-1R pathway, suggesting potential benefits for vascular function.
No immediate clinical implications; leaves open translation of IGF-1R agonism to human vascular therapies.
Ginsenoside Rg5 is a compound newly synthesized during the steaming process of ginseng; however, its biological activity has not been elucidated with regard to endothelial function. We found that Rg5 stimulated in vitro angiogenesis of human endothelial cells, consistent with increased neovascularization and blood perfusion in a mouse hind limb ischemia model. Rg5 also evoked vasorelaxation in aortic rings isolated from wild type and high cholesterol-fed ApoE −/− mice but not from endothelial nitric-oxide synthase (eNOS) knock-out mice. Angiogenic activity of Rg5 was highly associated with a specific increase in insulin-like growth factor-1 receptor (IGF-1R) phosphorylation and subsequent activation of multiple angiogenic signals, including ERK, FAK, Akt/eNOS/NO, and G i -mediated phospholipase C/Ca 2+ /eNOS dimerization pathways. The vasodilative activity of Rg5 was mediated by the eNOS/NO/cGMP axis. IGF-1R knockdown suppressed Rg5-induced angiogenesis and vasorelaxation by inhibiting key angiogenic signaling and NO/cGMP pathways. In silico docking analysis showed that Rg5 bound with high affinity to IGF-1R at the same binding site of IGF. Rg5 blocked binding of IGF-1 to its receptor with an IC 50 of ∼90 nmol/liter. However, Rg5 did not induce vascular inflammation and permeability. These data suggest that Rg5 plays a novel role as an IGF-1R agonist, promoting therapeutic angiogenesis and improving hypertension without adverse effects in the vasculature.The mechanism by which ginsenoside Rg5 regulates vascular function remains unclear. Results Rg5 increases angiogenesis and vasorelxation by activating multiple signal transduction pathways downstream of insulin-like growth fastor-1 receptor (IGF-1R). Conclusion Rg5 promotes endothelial cell function through activation of IGF-1R. Significance These findings reveal a mechanism for the positive regulation of vascular function by Rg5-mediated IGF-1R activation.
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Cho et al. (2014) studied this question. Ginsenoside Rg5 was evaluated on Angiogenesis and vasorelaxation. Ginsenoside Rg5 promotes angiogenesis and vasorelaxation by acting as an insulin-like growth factor-1 receptor agonist, blocking IGF-1 binding with an IC50 of ~90 nmol/liter.
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