• Journal of the Korea Academia-Industrial cooperation Society
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• v.15 no.11
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• pp.6774-6781
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• 2014

This study examined the efficacy and the mechanism of action of biological response modifiers, ginsenosides Rb1 and Rg1 isolated from Panax ginseng C.A. Meyer on human keratinocytes HaCaT cell lines. A non-significant cytotoxic response was obtained in the HaCaT cell lines on treatment with various concentrations of ginsenosides Rb1 and Rg1 for different time durations. Furthermore, the global changes in the mRNA profile of HaCaT cells were investigated using DNA microarrays after stimulation with the ginsenosides Rb1 and Rg1. Ginsenosides Rb1 and Rg1 strongly increased FGF2 in HaCaT cells, and were found to be a candidate gene for antioxidant activity and elasticity. Other key candidate genes for antioxidant activity, such as FANCD2, LEPR, and FAS, also show enhanced regulation in HaCaT cells treated with ginsenoside Rb1. This study will be useful for understanding the regulatory genes involved in skin elasticity and signal transduction pathway stimulated by the ginsenoside Rb1. This paper currently focuses on the key factors regulating the interaction of anti-aging principles and skin elasticity.

• Journal of Ginseng Research
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• v.35 no.1
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• pp.60-68
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• 2011

The chemical and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity changes of ginsenoside $Rb_1$-glycine and ginsenoside $Rg_1$-glycine mixtures by Maillard reaction were investigated to identify the role of Maillard reaction in the increased antioxidant activity of ginseng by heat-processing. The DPPH radical scavenging activity of $Rg_1$-glycine mixture was more strongly increased by heat-processing than that of $Rb_1$-glycine mixture. From the analyses of ginsenosides, $Rb_1$ was gradually changed into 20(S)-$Rg_3$, 20(R)-$Rg_3$, $Rk_1$ and $Rg_5$ by heat-processing. $Rg_1$ was gradually changed into 20(S)-$Rh_1$, 20(R)-$Rh_1$, $Rk_3$ and $Rh_4$ by heat-processing. However, the generation of these less-polar ginsenosides was not related to the increased DPPH radical scavenging activity of $Rb_1$-glycine and $Rg_1$-glycine mixtures because their DPPH radical scavenging activities were already significantly increased when dried at $50^{\circ}C$, which temperature induce no structural changes of ginsenosides. In the comparison of browning compound levels of $Rg_1$-glycine and $Rb_1$-glycine mixtures, the extents of Maillard reaction were positively correlated with their increased free radical scavenging activities. Based on the chemical and DPPH radical scavenging activity changes of $Rg_1$-glycine and $Rb_1$-glycine mixtures by heat-processing, we clearly identified that the increased free radical scavenging activity of ginsenoside is mediated by the Maillard reaction between sugar moiety of ginsenoside and amino acid.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.10 no.2
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• pp.418-424
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• 2009

The analytical conditions of ginsenosides were optimized using high performance liquid chromatography (HPLC). The optimal analysis conditions were set up from the experiments using different gradient conditions, and the ginsenosides contents of red ginseng products and their raw materials were analysed. Red ginseng contained 0.29% Rg1, 0.82% Rb1, 0.38% Rc, 0.32% Rb2, 0.11% Rd, showing the highest ginsenoside contents. Among the red ginseng products, red ginseng extract showed the highest content. The ginsenoside contents were varied according to the raw material type and product type. Re and Rb1 contents were the highest in most raw materials and products.

• Journal of Ginseng Research
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• v.18 no.1
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• pp.17-24
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• 1994

Effect of ginsenoside mixture, ginsenoside $Rb_1$,$Rb_2$,$Rg_1$ and the fat soluble fraction of the roots of Panax ginseng C.A. Meyer on the activity of glucokinase (GK) in vitro has been observed and found that GK activity was increased about 15c1c at the concentration of ginsenoside mixture and/or the fat soluble fraction being $10^{-7}$,$10^{-5}$%. It was also observed that glucose uptake by rat liver was increased in the presence of either ginsenoside mixture or the fat soluble fraction by perfusion technique. Ginsenoside mixture stimulated various enzymes related to glucose metabolism, however, both ginsenoside mixture and the fat soluble fraction did not stimulate GK activity as expected. Primary culture of liver cells showed that the ginsenoside mixture and the fat soluble fraction increased GK activity significantly and they stimulated the GK activity synergistically in the co-presence of insulin.

• Natural Product Sciences
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• v.20 no.2
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• pp.119-125
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• 2014

According to the results of my study on the chromatographic analysis of fresh ginseng (Panax ginseng C. A. Meyer) roots, most of the contents of protopanxadiol ginsenosides $Rb_1$, Rc, $Rb_2$, and Rd are derived from the corresponding malonyl ginsenosides in fresh ginseng by a heat process. Also, I confirmed that acetyl ginsenosides are naturally occurring constituents in fresh ginseng, not decarboxylates from malonyl ginsenosides. Seven neutral ginsenosides $Rg_1$, Re, Rf, Rc, $Rb_1$, $Rb_2$, and Rd were transformed to specific conversions in red ginseng preparation conditions. The conversion paths progress by three rules concluded from my study. These conversion rules are I: the ether bond is stable at positions 3 and 6 in the dammarane skeleton, II: the ether bond between sugars is stable in glycosides, and III: the ether bond to glycosides is unstable at position 20 in the dammarane skeleton.

• Biomolecules & Therapeutics
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• v.25 no.2
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• pp.202-212
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• 2017

Doxorubicin (DOX) is a highly effective chemotherapeutic agent; however, the dose-dependent cardiotoxicity associated with DOX significantly limits its clinical application. In the present study, we investigated whether Rb1 could prevent DOX-induced apoptosis in H9C2 cells via aryl hydrocarbon receptor (AhR). H9C2 cells were treated with various concentrations ($-{\mu}M$) of Rb1. AhR, CYP1A protein and mRNA expression were quantified with Western blot and real-time PCR analyses. We also evaluated the expression levels of caspase-3 to assess the anti-apoptotic effects of Rb1. Our results showed that Rb1 attenuated DOX-induced cardiomyocytes injury and apoptosis and reduced caspase-3 and caspase-8, but not caspase-9 activity in DOX-treated H9C2 cells. Meanwhile, pre-treatment with Rb1 decreased the expression of caspase-3 and PARP in the protein levels, with no effects on cytochrome c, Bax, and Bcl-2 in DOX-stimulated cells. Rb1 markedly decreased the CYP1A1 and CYP1A2 expression induced by DOX. Furthermore, transfection with AhR siRNA or pre-treatment with AhR antagonist CH-223191 significantly inhibited the ability of Rb1 to decrease the induction of CYP1A, as well as caspase-3 protein levels following stimulation with DOX. In conclusion, these findings indicate that AhR plays an important role in the protection of Ginsenoside Rb1 against DOX-triggered apoptosis of H9C2 cells.

• Journal of Applied Biological Chemistry
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• v.62 no.4
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• pp.375-384
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• 2019

The root of Panax ginseng C.A. Meyer were extracted with 70% aqueous EtOH and the concentrates were partitioned into MeOH and H₂O fractions using Diaion HP-20. The repeated SiO₂ or octadecyl SiO₂ column, and MPLC for the MeOH fraction led to isolation of four malonyl ginsenosides. The chemical structures of these compounds were determined as malonyl ginsenoside Rd (1) malonyl ginsenoside Rc (2) malonyl ginsenoside Rb2 (3) malonyl ginsenoside Rb1 (4) based on spectroscopic analyses including Nuclear magnetic resonance and HR-TOF/MS. The contents of malonyl ginsenoside Rb1 was highist as 5.44 mg/g of five years of ginseng. And malonyl ginsenoside Rd was lowest as 0.11 mg/g of six years of ginseng. Additionally, the malonyl ginsenoside Rd exhibited hepatoprotective effect against ethanol-induced hepatotoxicity in HepG2 cell line.

• Journal of Ginseng Research
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• v.40 no.3
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• pp.278-284
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• 2016

Background: The ginsenoside Rb1 (Rb1) is the most abundant compound in the root of Panax ginseng. Recent studies have shown that Rb1 has a neuroprotective effect. However, the mechanisms underlying this effect are still unknown. Methods: We used stable isotope labeling with amino acids in cell culture, combined with quantitative mass spectrometry, to explore a potential protective mechanism of Rb1 in ${\beta}$-amyloid-treated neuronal cells. Results: A total of 1,231 proteins were commonly identified from three replicate experiments. Among these, 40 proteins were significantly changed in response to Rb1 pretreatment in ${\beta}$-amyloid-treated neuronal cells. Analysis of the functional enrichments and protein interactions of altered proteins revealed that actin cytoskeleton proteins might be linked to the regulatory mechanisms of Rb1. The CAP1, CAPZB, TOMM40, and DSTN proteins showed potential as molecular target proteins for the functional contribution of Rb1 in Alzheimer's disease (AD). Conclusion: Our proteomic data may provide new insights into the protective mechanisms of Rb1 in AD.

• Journal of Ginseng Research
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• v.43 no.4
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• pp.499-507
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• 2019

Background: Ginsenoside Rb1 (Rb1), a dominant component from the extract of Panax ginseng root, exhibits neuroprotective functions in many neurological diseases. This study was intended to investigate whether Rb1 can attenuate cisplatin-induced memory impairments and explore the potential mechanisms. Methods: Cisplatin was injected intraperitoneally with a dose of 5 mg/kg/wk, and Rb1 was administered in drinking water at the dose of 2 mg/kg/d to rats for 5 consecutive wk. The novel objects recognition task and Morris water maze were used to detect the memory of rats. Nissl staining was used to examine the neuron numbers in the hippocampus. The activities of superoxide dismutase, glutathione peroxidase, cholineacetyltransferase, acetylcholinesterase, and the levels of malondialdehyde, reactive oxygen species, acetylcholine, tumor necrosis factor-${\alpha}$, interleukin-$1{\beta}$, and interleukin-10 were measured by ELISA to assay the oxidative stress, cholinergic function, and neuroinflammation in the hippocampus. Results: Rb1 administration effectively ameliorates the memory impairments caused by cisplatin in both novel objects recognition task and Morris water maze task. Rb1 also attenuates the neuronal loss induced by cisplatin in the different regions (CA1, CA3, and dentate gyrus) of the hippocampus. Meanwhile, Rb1 is able to rescue the cholinergic neuron function, inhibit the oxidative stress and neuroinflammation in cisplatin-induced rat brain. Conclusion: Rb1 rescues the cisplatin-induced memory impairment via restoring the neuronal loss by reducing oxidative stress and neuroinflammation and recovering the cholinergic neuron functions.

• Journal of Ginseng Research
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• v.46 no.3
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• pp.376-386
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• 2022

Background: Brain-derived neurotrophic factor (BDNF)-tropomyosin-related kinase B (TrkB) plays a critical role in the pathogenesis of depression by modulating synaptic structural remodeling and functional transmission. Previously, we have demonstrated that the ginsenoside Rb1 (Rb1) presents a novel antidepressant-like effect via BDNF-TrkB signaling in the hippocampus of chronic unpredictable mild stress (CUMS)-exposed mice. However, the underlying mechanism through which Rb1 counteracts stress-induced aberrant hippocampal synaptic plasticity via BDNF-TrkB signaling remains elusive. Methods: We focused on hippocampal microRNAs (miRNAs) that could directly bind to BDNF and are regulated by Rb1 to explore the possible synaptic plasticity-dependent mechanism of Rb1, which affords protection against CUMS-induced depression-like effects. Results: Herein, we observed that brain-specific miRNA-134 (miR-134) could directly bind to BDNF 30 UTR and was markedly downregulated by Rb1 in the hippocampus of CUMS-exposed mice. Furthermore, the hippocampus-targeted miR-134 overexpression substantially blocked the antidepressant-like effects of Rb1 during behavioral tests, attenuating the effects on neuronal nuclei-immunoreactive neurons, the density of dendritic spines, synaptic ultrastructure, long-term potentiation, and expression of synapse-associated proteins and BDNF-TrkB signaling proteins in the hippocampus of CUMS-exposed mice. Conclusion: These data provide strong evidence that Rb1 rescued CUMS-induced depression-like effects by modulating hippocampal synaptic plasticity via the miR-134-mediated BDNF signaling pathway.