• Journal of Ginseng Research
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• v.21 no.2
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• pp.132-140
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• 1997

The effects of ginsenosides purified from red ginseng on platelet aggregation were investigated. Preincubation of washed platelets from rats with either ginsenoside Rg3, ginsenosides non-polar fraction (G-NPF), ginsenoside Rg1(Rg1) or ginsenosides polar fraction(G-PF) reduced the plytelet aggrelation induced by collagen in a dose-dependent manner, whereas ginsenoside Rg2 failed to inhibit the aggregation. Their IC50 values of Rg3, G-NPF, Rgl, and G-PF were 8.7$\pm$1.0, 150.3$\pm$0.1, 369.9$\pm$ 1.0, 606.211.3 $\mu\textrm{g}$/ml, respectively. Aggrelation induced by thrombin was also inhibited by Rg3 and G-NPF with IC50 being 5.2$\pm$ 1.1 and 66.5$\pm$0.8 $\mu\textrm{g}$/ml, respectively. The alterations of Intracellular Ca2+ concentration in platelets were monitored using fura-2 as a fluorescent Ca2+ indicator. Both Ca2+ release from internal stores and Ca2+ influx into cytosol were suppressed by Rg3. Rg3 also inhibited granular release of ATP and TXA2 formation induced by thrombin in a dose-dependent manner in the washed platelets. Rg3 also inhibited Aggregation and ATP release from human platelets induced by collagen to a similar extent as were observed in rat platelets. In conclusion, Rg3 is a Potent anti-aggregating component in ginsenosides and may exert its anti-aggrega1ing activity by decreasing TXAa formation and granular secretion in platelets, most likely by inhibiting Ca2+ influx and Ca2+ mobilization from intracellular stores. Thus ginseng may contribute to the prevention and treatment of thrombosis.

• Journal of Ginseng Research
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• v.43 no.4
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• pp.550-561
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• 2019

Background: Gastric ulcer (GU) is a common gastrointestinal disease that can be induced by many factors. Finding an effective treatment method that contains fewer side effects is important. 20 (S)-ginsenoside Rg3 is a kind of protopanaxadiol and has shown superior antiinflammatory and antioxidant effects in many studies, especially cancer studies. In this study, we examined the treatment efficacy of 20 (S)-ginsenoside Rg3 on GU. Methods: Three kinds of GU models, including an alcohol GU model, a pylorus-ligated GU model, and an acetic acid GU model, were used. Mouse endothelin-1 (ET-1) and nitric oxide (NO) levels in blood and epidermal growth factor (EGF), superoxide dismutase, and NO levels in gastric mucosa were evaluated. Hematoxylin and eosin staining of gastric mucosa and immunohistochemical staining of ET-1, inducible nitric oxide synthase (NOS2), and epidermal growth factor receptors were studied. Ulcer index (UI) scores and UI ratios were also analyzed to demonstrate the GU conditions in different groups. Furthermore, Glide XP from $Schr{\ddot{o}}dinger$ was used for molecular docking to clarify the interactions between 20 (S)-ginsenoside Rg3 and EGF and NOS2. Results: 20 (S)-ginsenoside Rg3 significantly decreased the UI scores and UI ratios in all the three GU models, and it demonstrated antiulcer effects by decreasing the ET-1 and NOS2 levels and increasing the NO, superoxide dismutase, EGF, and epidermal growth factor receptor levels. In addition, high-dose 20 (S)-ginsenoside Rg3 showed satisfactory gastric mucosa protection effects. Conclusion: 20 (S)-ginsenoside Rg3 can inhibit the formation of GU and may be a potential therapeutic agent for GU.

• Journal of Ginseng Research
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• v.47 no.2
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• pp.291-301
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• 2023

Introduction: Non-small cell lung cancer (NSCLC) patients are particularly vulnerable to the Coronavirus Disease-2019 (COVID-19). Currently, no anti-NSCLC/COVID-19 treatment options are available. As ginsenoside Rg3 is beneficial to NSCLC patients and has been identified as an entry inhibitor of the virus, this study aims to explore underlying pharmacological mechanisms of ginsenoside Rg3 for the treatment of NSCLC patients with COVID-19. Methods: Based on a large-scale data mining and systemic biological analysis, this study investigated target genes, biological processes, pharmacological mechanisms, and underlying immune implications of ginsenoside Rg3 for NSCLC patients with COVID-19. Results: An important gene set containing 26 target genes was built. Target genes with significant prognostic value were identified, including baculoviral IAP repeat containing 5 (BIRC5), carbonic anhydrase 9 (CA9), endothelin receptor type B (EDNRB), glucagon receptor (GCGR), interleukin 2 (IL2), peptidyl arginine deiminase 4 (PADI4), and solute carrier organic anion transporter family member 1B1 (SLCO1B1). The expression of target genes was significantly correlated with the infiltration level of macrophages, eosinophils, natural killer cells, and T lymphocytes. Ginsenoside Rg3 may benefit NSCLC patients with COVID-19 by regulating signaling pathways primarily involved in anti-inflammation, immunomodulation, cell cycle, cell fate, carcinogenesis, and hemodynamics. Conclusions: This study provided a comprehensive strategy for drug discovery in NSCLC and COVID-19 based on systemic biology approaches. Ginsenoside Rg3 may be a prospective drug for NSCLC patients with COVID-19. Future studies are needed to determine the value of ginsenoside Rg3 for NSCLC patients with COVID-19.

• Food Engineering Progress
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• v.14 no.2
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• pp.159-165
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• 2010

Red ginseng tail roots (9.8 g water/100 g sample) were puffed at 7, 8, 9, and 10 $kg_{f}/cm^{2}$ using a rotational puffing gun. Puffed red ginseng was extracted with 70% ethanol, and the concentrated extract was successively partitioned with diethyl ether, n-butanol and $H_{2}O$. Two unknown ginsenosides from puffed red ginseng were found at 63 and 65 min of retention time in HPLC chromatogram suggesting that chemical structure of some ginsenosides might be altered during the puffing process. Identification of two unknown compounds was carried out using TLC, HPLC and NMR. Two major compounds were isolated from TLC. According to TLC result, compound I was expected to be the mixture of ginsenosides Rk1 and Rg5, and compound II was expected to be a 20(S)-ginsenoside $Rg_{3}$. Three compounds were isolated from n-butanol fraction through repeated silica gel and octadecyl silica gel column chromatographies. From the result of $^{1}H$- and $^{13}C$-NMR data, the chemical structures of unknown compounds were determined as ginsenoside $Rg_{5}$ and 20(S)-ginsenoside $Rg_{3}$. Unfortunately, ginsenoside $Rk_{1}$ could not be separated from ginsenoside-$Rg_{5}$ in the compound I. It was carefully reexamined using HPLC and confirmed that the last unknown compound was ginsenoside-$Rk_{1}$.

• Analytical Science and Technology
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• v.26 no.4
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• pp.221-227
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• 2013

A sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed for the investigation of the ginsenoside Rg1 in human plasma. After addition of internal standard (digoxin), plasma was diluted with acetone and methanol (80:20), the supernatant was concentrated and analyzed by LC-MS/MS. The optimal chromatographic separation was achieved on an Agilent Eclipse XDB-C18 column ($4.6{\times}150mm$, $5{\mu}m$) with a mobile phase of 0.1% formic acid in water and 0.1% formic acid in methanol at a flow rate of 0.9 mL/min gradient mode. The standard calibration curve for ginsenoside Rg1 was linear ($r^2=0.9995$) over the concentration range 1~500 ng/mL in human plasma. The intra- and inter-day precision over the concentration range of ginsenoside Rg1 was lower than 7.53% (correlation of variance, CV), and accuracy exceeded 98.28%. This LC-MS/MS assay of ginsenoside Rg1 in human plasma is applicable for quantifying in the pharmacokinetic study.

• Food Science and Biotechnology
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• v.14 no.4
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• pp.509-513
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• 2005

The purpose of this study was to develop a new preparation process of ginseng extract using high concentrations of ginsenoside $Rg_3$, a special component in red ginseng. From when the ginseng saponin glycosides transformed into the prosapogenins chemically, they were analyzed using the HPLC method. The ginseng and ginseng extract were processed with several treatment conditions of an edible brewing vinegar. The results indicated that ginsenoside $Rg_3$ quantities increased over 4% at the pH 2-4 level of vinegar treatment. This occurred at temperatures above $R90^{\circ}C$, but not occurred at other pH and temperature condition. In addition, the ginseng and ginseng extract were processed with the twice-brewed vinegar (about 14% acidity). This produced about 1.5 times more ginsenoside $Rg_3$ than those processed with regular amounts of brewing vinegar (about 7% acidity) and persimmon vinegar (about 3% acidity). Though the white ginseng extract was processed with the brewing vinegar over four hr, there was no change for ginsenoside $Rg_3$. However, the VG8-7 was the highest amount of ginsenoside $Rg_3$ (4.71%) in the white ginseng extract, which was processed with the twice-brewed vinegar for nine hr. These results indicate that ginseng treated with vinegar had 10 times the quantity of ginsenoside $Rg_3$, compared to the amount of ginsenoside $Rg_3$ in the generally commercial red ginseng, while ginsenoside $Rg_3$ was not found in raw and white ginseng.

• Journal of Pharmacopuncture
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• v.11 no.2
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• pp.87-95
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• 2008

Objectives The aim of this experiment is to provide an differentiation of ginseng, red ginseng, cultivated wild ginseng(CWG), and red wild ginseng(RWG) through component analysis using HPLC(High Performance Liquid Chromatography, hereafter HPLC). Methods Comparative analyses of ginsenoside $Rg_3$, ginsenoside $Rh_2$, and ginsenosides $Rb_1$ and $Rg_1$ of various ginsengs were conducted using HPLC. Results 1. CWG was relatively heat-resistant and showed slow change in color during the process of steaming and drying, compared to cultivated ginseng. 2. Ginsenoside $Rg_3$ was not detected in cultivated ginseng and CWG, whereas it was high in red ginseng and RWG. Ginsenoside $Rg_3$ was more generated in red ginseng than in RWG. 3. Ginsenoside $Rh_2$ appreared during steaming and drying of cultivated ginseng, whereas it was more increased during steaming and drying of CWG. 4. Ginsenoside $Rg_1$ content was more increased during steaming and drying of cultivated ginseng, whereas it was more decreased during steaming and drying of CWG. 5. Ginsenoside $Rb_1$ content was increased about 500% during steaming and drying of cultivated ginseng, whereas it was increased about 30% during steaming and drying of CWG, indicating that ginsenoside $Rb_1$ was more generated in red ginseng than in RWG. 6. Ginsenoside $Rg_3$ content was higher, whereas ginsenoside $Rg_1$ content was lower in 11th RWG than in 9th RWG, indicating that ginsenoside $Rg_3$ content was increased and $Rg_1$ content was decreased as steaming and drying continued to proceed. Ginsenoside $Rh_2$ and $Rb_1$ contents began to be increased, followed by decreased after 9th steaming and drying process. Conclusions Above experiment data can be an important indicator for the dentification of ginseng, red ginseng, CWG, and RWG. And the following studies will be need for making good product using CWG.

• Journal of Ginseng Research
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• v.37 no.1
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• pp.124-134
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• 2013

The authentication of the physico-chemical properties of ginsenosides reference materials as well as qualitative and quantitative batch analytical data based on validated analytical procedures is a prerequisite for certifying good manufacturing practice (GMP). Ginsenoside Rb1 and Rg1, representing protopanaxadiol and protopanaxatriol ginsenosides, respectively, are accepted as marker substances in quality control standards worldwide. However, the current analytical methods for these two compounds recommended by Korean, Chinese, European, and Japanese pharmacopoeia do not apply to red ginseng preparations, particularly the extract, because of the relatively low content of the two agents in red ginseng compared to white ginseng. In manufacturing fresh ginseng into red ginseng products, ginseng roots are exposed to a high temperature for many hours, and the naturally occurring ginsenoside Rb1 and Rg1 are converted to artifact ginsenosides such as Rg3, Rg5, Rh1, and Rh2 during the heating process. The analysis of ginsenosides in commercially available ginseng products in Korea led us to propose the inclusion of the (20S)- and (20R)-ginsenoside Rg3, including ginsenoside Rb1 and Rg1, as additional reference materials for ginseng preparations. (20S)- and (20R)-ginsenoside Rg3 were isolated by Diaion HP-20 adsorption chromatography, silica gel flash chromatography, recrystallization, and preparative HPLC. HPLC fractions corresponding to those two ginsenosides were recrystallized in appropriate solvents for the analysis of physico-chemical properties. Documentation of those isolated ginsenosides was achieved according to the method proposed by Gaedcke and Steinhoff. The ginsenosides were subjected to analyses of their general characteristics, identification, purity, content quantification, and mass balance tests. The isolated ginsenosides showed 100% purity when determined by the three HPLC systems. Also, the water content was found to be 0.534% for (20S)-Rg3 and 0.920% for (20R)-Rg3, meaning that the net mass balances for (20S)-Rg3 and (20R)-Rg3 were 99.466% and 99.080%, respectively. From these results, we could assess and propose a full spectrum of physico-chemical properties of (20S)- and (20R)-ginsenoside Rg3 as standard reference materials for GMP-based quality control.

• Journal of Ginseng Research
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• v.40 no.1
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• pp.9-17
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• 2016

Background: Alzheimer's disease (AD) is a progressive brain disease, for which there is no effective drug therapy at present. Ginsenoside Rg1 (G-Rg1) and G-Rg2 have been reported to alleviate memory deterioration. However, the mechanism of their anti-AD effect has not yet been clearly elucidated. Methods: Ultra performance liquid chromatography tandem MS (UPLC/MS)-based metabolomics was used to identify metabolites that are differentially expressed in the brains of AD mice with or without ginsenoside treatment. The cognitive function of mice and pathological changes in the brain were also assessed using the Morris water maze (MWM) and immunohistochemistry, respectively. Results: The impaired cognitive function and increased hippocampal $A{\beta}$ deposition in AD mice were ameliorated by G-Rg1 and G-Rg2. In addition, a total of 11 potential biomarkers that are associated with the metabolism of lysophosphatidylcholines (LPCs), hypoxanthine, and sphingolipids were identified in the brains of AD mice and their levels were partly restored after treatment with G-Rg1 and G-Rg2. G-Rg1 and G-Rg2 treatment influenced the levels of hypoxanthine, dihydrosphingosine, hexadecasphinganine, LPC C 16:0, and LPC C 18:0 in AD mice. Additionally, G-Rg1 treatment also influenced the levels of phytosphingosine, LPC C 13:0, LPC C 15:0, LPC C 18:1, and LPC C 18:3 in AD mice. Conclusion: These results indicate that the improvements in cognitive function and morphological changes produced by G-Rg1 and G-Rg2 treatment are caused by regulation of related brain metabolic pathways. This will extend our understanding of the mechanisms involved in the effects of G-Rg1 and G-Rg2 on AD.

• Journal of Ginseng Research
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• v.33 no.3
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• pp.183-188
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• 2009

To produce ginsenoside-Rg$_3$ enriched edible yeast, ginseng steaming effluent (GSE) was used for yeast cultivation in this study. Four kinds of edible yeasts were cultured in sterilized GSE (2% w/v, pH 6.5), without any nutrient, for 48 h at 30$^{\circ}C$, and their growth and ginsenoside compositions were determined. Among the yeasts, Saccharomyces cerevisiae showed the highest growth in the GSE medium. 267.1 mg of Saccharomyces cerevisiae biomass was produced from 1 g of GSE solid and ginsenoside-Rg$_3$ contents was determined with 0.033 mg. Saccharomyces cerevisiae also showed the best overall acceptability, with a herbal and fermentative flavor and a slightly bitter taste. From these data, we conclude that Saccharomyces cerevisiae is the excellent strain for production of ginsenoside-Rg$_3$ enriched edible yeast using GSE.