• Journal of Ginseng Research
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• 제32권3호
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• pp.264-269
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• 2008

Ginsenosides are major components in Panax ginseng and known to have numerous pharmacological activities such as anti-cancer, anti-diabetes, anti-viral and anti-atherosclerosis effects. In this study, the regulatory activities of G-Rg3 and its derivative 25-hydroxy Rg3 (G-Rg3-2H) on the production of nitric oxide (NO) in macrophages and the proliferation of lymphocytes prepared from spleen and bone marrow under treatment of lipopolysaccharide (LPS) or concanavalin (Con) A were examined. G-Rg3 and G-Rg3-2H dose-dependently inhibited NO production from LPS-activated RAW264.7 cells and in agreement, these compounds protected RAW264.7 cells from LPS-mediated cytotoxicity. In contrast, G-Rg3-2H dose-dependently inhibited lymphocyte proliferation induced by both LPS and Con A, while there was no inhibition by G-Rg3. Therefore, our data suggest that these compounds may be applied for NO-mediated or lymphocyte-mediated immunological diseases.

• Journal of Microbiology and Biotechnology
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• 제16권11호
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• pp.1791-1798
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• 2006

When ginsenoside Rg5, a main component isolated from red ginseng, was incubated with three human fecal microflora for 24 h, all specimens showed hydrolyzing activity: all specimens produced ginsenoside Rh3 as a main metabolite, but a minor metabolite $3{\beta},12{\beta}$-dihydroxydammar-21(22),24-diene (DD) was observed in two specimens. To evaluate the antiallergic effect of ginsenoside Rg5 and its metabolites, the inhibitory effect of ginsenoside Rg5 and its metabolite ginsenoside Rh3 against RBL-2H3 cell degranulation, mouse passive cutaneous anaphylaxis (PCA) reaction induced by the IgE-antigen complex, and mouse ear skin dermatitis induced by 12-O-tetradecanoilphorbol-13-acetate (TPA) were measured. Ginsenosides Rg5 and Rh3 potently inhibited degranulation of RBL-2H3 cells. These ginsenosides also inhibited mRNA expression of proinflammatory cytokines IL-6 and $TNF-{\alpha}$ in RBL-2H3 cells stimulated by IgE-antigen. Orally and intraperitoneally administered ginsenoside Rg3 and orally administered ginsenoside Rg5 to mice potently inhibited the PCA reaction induced by IgE-antigen complex. However, intraperitoneally administered ginsenoside Rg5 nearly did not inhibit the PCA reaction. These ginsenosides not only suppressed the swelling of mouse ears induced by TPA, but also inhibited mRNA expression of cyclooxygenase-2, $TNF-{\alpha}$, and IL-4 and activation of transcription factor NF-kB. These inhibitions of ginsenoside Rh3 were more potent than those of ginsenoside Rg5. These findings suggest that ginsenoside Rg5 may be metabolized in vivo to ginsenoside Rh3 by human intestinal microflora, and ginsenoside Rh3 may improve antiallergic diseases, such as rhinitis and dermatitis.

• 한국자원식물학회지
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• 제19권1호
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• pp.139-143
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• 2006

고기능성 홍삼사포닌성분의 함량을 증대시키기 위한 목적으로 홍삼엑스에 열처리, 산(acid)처리하여 그 가능성을 조사하였다. 산도를 조정하지 않은 무처리구(control, pH 4.4)에 $120^{\circ}C$ 열처리한 경우 ginsenoside-$Rg_3$의 함량이 약 2배 정도 증가였다. 구연산으로 pH 2.0으로 조정하고 온도처리한 처리구에서는 2.8배나 많은 ginsenoside-$Rg_3$ 성분이 증가하였으나 다른 유효한 사포닌의 파괴가 두드러져 처음 홍삼엑스에 함유되어 있던 총사포닌의 65% 정도가 소실되었다. $80^{\circ}C$에서 12시간 처리를 한 경우에는 pH를 2.5와 2.0로 조정한 처리구에서는 11.20 mg과 12.50 mg으로 홍삼엑스의 3.3 mg보다 3.3배 이상 ginsenoside-$Rg_3$ 성분이 변환되었다. Ginsenoside-$Rb_1,\;Rb_2$, Rc, Re, $Rg_1$의 함량이 산도가 높아짐에 따라서 급격히 소실되었고 홍삼 특이성분(ginsenoside-$Rg_3,\;Rh_2,\;Rh_1$)의 함량은 현저히 증가되었다. 매실엑스로 pH를 2.5로 조정한 처리구에서는 13.34 mg으로 홍삼엑스의 3.3 mg보다 4배 이상 변환된 것으로 분석되었다. 비록 31%정도의 total saponin의 감소가 있었으나 $120^{\circ}C$의 고온처리에서 처럼 다른 유효한 사포닌의 큰 손실 없이 $60^{\circ}C$에 12시간 처리하는 것만으로도 다량의 ginsenoside-$Rg_3$를 생산하는 것을 확인하였다.

• Journal of Ginseng Research
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• 제39권4호
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• pp.304-313
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• 2015

Background: Ginsenoside Rg3 is a promising anticancer agent. It is usually produced by heat treatment of ginseng, in which ginsenoside Rb1 is the major ginsenoside. A kinetic study was conducted to optimize ginsenoside Rg3 production by the heat treatment of ginsenoside Rb1. Methods: Ginsenoside Rb1 was heated using an isothermal machine at $80^{\circ}C$ and $100^{\circ}C$ and analyzed using HPLC. The kinetic parameters were calculated from the experimental results. The activation energy was estimated and used to simulate the process. The optimized parameters of ginsenoside Rg3 production are suggested based on the simulation. Results: The rate constants were $0.013h^{-1}$ and $0.073h^{-1}$ for the degradation of ginsenosides Rb1 and Rg3 at $80^{\circ}C$, respectively. The corresponding rate constants at $100^{\circ}C$ were $0.045h^{-1}$ and $0.155h^{-1}$. The estimated activation energies of degradation of ginsenosides Rb1 and Rg3 were 69.2 kJ/mol and 40.9 kJ/mol, respectively. The rate constants at different temperatures were evaluated using the estimated activation energies, and the kinetic profiles of ginsenosides Rb1 and Rg3 at each temperature were simulated based on the proposed kinetic model of consecutive reaction. The optimum strategies for producing ginsenoside Rg3 from ginsenoside Rb1 are suggested based on the simulation. With increased temperature, a high concentration of ginsenoside Rg3 is formed rapidly. However, the concentration decreases quickly after the reaching the maximal concentration value. Conclusion: The optimum temperature for producing ginsenoside Rg3 should be the highest temperature technically feasible below $180^{\circ}C$, in consideration of the cooling time. The optimum reaction time for heat treatment is 30 min.

• Archives of Pharmacal Research
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• 제27권1호
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• pp.61-67
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• 2004

When ginseng water extract was incubated at $60^{\circ}C$ in acidic conditions, its protopanaxadiol ginsenosides were transformed to ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$. However, protopanaxadiol glycoside ginsenosides $Rb_1, Rb_2$ and Rc isolated from ginseng were mostly not transformed to ginsenoside $Rg_3$ by the incubation in neutral condition. The transformation of these ginsenosides to ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$ was increased by increasing incubation temperature and time in acidic condition: the optimal incubation time and temperature for this transformation was 5 h and $60^{\circ}C$ resepectively. The transformed ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$ were metabolized to ginsenoside $Rh_2$ and $\Delta^{20}$--ginsenoside $Rh_2$, respectively, by human fecal microflora. Among the bacteria isolated from human fecal microflora, Bacteroides sp., and Bifidobacterium sp. and Fusobacterium sp. potently transformed ginsenoside $Rg_3$ to ginsenoside $Rh_2$. Acid-treated ginseng (AG) extract, fermented AG extract, ginsenoside $Rh_2$ and protopanaxadiol showed potent cytotoxicity against tumor cell lines. AG extract, fermented AG extract and protopanaxadiol potently inhibited the growth of Helicobacter pylori.

• Journal of Ginseng Research
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• 제40권2호
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• pp.151-159
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• 2016

Background: Ginsenoside-Rg3, the pharmacologically active component of red ginseng, has been found to inhibit tumor growth, invasion, metastasis, and angiogenesis in various cancer models. Previously, we found that 20(R)-ginsenoside-Rg3 (Rg3) could inhibit angiogenesis. Since microRNAs (miRNAs) have been shown to affect many biological processes, they might play an important role in ginsenoside-mediated angiomodulation. Methods: In this study, we examined the underlying mechanisms of Rg3-induced angiosuppression through modulating the miRNA expression. In the miRNA-expression profiling analysis, six miRNAs and three miRNAs were found to be up- or down-regulated in vascular-endothelial-growth-factor-induced human-umbilical-vein endothelial cells (HUVECs) after Rg3 treatment, respectively. Results: A computational prediction suggested that mature hsa-miR-520h (miR-520h) targets ephrin receptor (Eph) B2 and EphB4, and hence, affecting angiogenesis. The up-regulation of miR-520h after Rg3 treatment was validated by quantitative real-time polymerase chain reaction, while the protein expressions of EphB2 and EphB4 were found to decrease, respectively. The mimics and inhibitors of miR- 520h were transfected into HUVECs and injected into zebra-fish embryos. The results showed that overexpression of miR-520h could significantly suppress the EphB2 and EphB4 protein expression, proliferation, and tubulogenesis of HUVECs, and the subintestinal-vessel formation of the zebra fish. Conclusion: These results might provide further information on the mechanism of Rg3-induced angiosuppression and the involvement of miRNAs in angiogenesis.

• Food Science and Biotechnology
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• 제17권4호
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• pp.883-887
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• 2008

The purpose of this study was to develop a new preparation process for chemical transformation of ginseng saponin glycosides to prosapogenins. Ginseng and ginseng extracts were processed under several treatment conditions using ascorbic acid solution. Treating with ascorbic acid at pH 2-3 and above $80^{\circ}C$ increased the ginsenoside $Rg_3$ content of samples to over 3% as compared to other pH levels and temperatures. In addition, ginseng and ginseng extracts that were processed under a high ascorbic acid solution treatment condition (pH 2.0, 5 hr) contained more ginsenoside $Rg_3$ (approximately 16 times) than those processed under a low ascorbic acid solution treatment condition (pH 3.0, 5 hr). The highest quantity of ginsenoside $Rg_3$ (3.434%) occurred when a sample of fine ginseng root extract (AG2-9) was processed with the ascorbic acid solution at pH 2.0 for 9 hr. However, there was no change in the amount of ginsenoside $Rg_3$ when fine ginseng root extracts were processed with ascorbic acid solution at pH 2.0 for over 9 hr. In conclusion, the results indicated that ascorbic acid treatment of ginseng extracts can produce a level of ginsenoside $Rg_3$ that is over 90-fold the amount found in commercial red ginseng.

• Food Science and Biotechnology
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• 제14권4호
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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 Ginseng Research
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• 제33권3호
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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.

• 산업식품공학
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• 제14권2호
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• pp.159-165
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• 2010

팽화홍삼으로부터 용매추출, 용매분획 및 silica gel column chromatography를 반복하여 두 개의 화합물을 분리하였다. 이들 두 화합물의 결정특성, 녹는점, 비선광도, Infrared spectrum 분석 결과, TLC에서의 Rf값, HPLC에서의 retention time 및 NMR 데이터를 측정하여 고찰한 결과 두 개의 화합물은 20(S)-ginsenoside Rg3와 ginsenoside Rg5임을 확인할 수 있었다. 특히 $^{1}H$- 및 $^{13}C$-NMR 데이터를 HSQC 및 HMBC와 같은 2D-NMR 실험을 통하여 더욱 정확하게 동정하였다.