• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2004년도 추계 학술대회 및 정기총회
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• pp.7-11
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• 2004

We previously reported that ginseng inhibited NMDA receptors in cultured hippocampal neurons. Here, we further examined the detailed mechanism of ginseng-mediated inhibition using its main active ingredient, ginsenoside Rg$_3$. Co-application of ginsenoside Rg$_3$ with increasing concentrations of NMDA did not change the EC$_{50}$ of NMDA to the receptor, suggesting ginsenoside Rg$_3$ inhibits NMDA receptors without competing with the NMDA-binding site. Ginsenoside Rg$_3$-mediated inhibition also occurred in a distinctive manner from the well-characterized NMDA receptor open channel blocker, MK-801, However, ginsenoside Rg$_3$ produced its effect in a glycine concentration-dependent manner and shifted the glycine concentration-response curve to the right without changing the maximal response, suggesting the role of ginsenoside Rg$_3$ as a competitive NMDA receptor antagonist. We also demonstrated that ginsenoside Rg$_3$ significantly protected neurons against NMDA insults. Therefore, these results suggest that ginsenoside Rg$_3$ protects NMDA-induced neuronal death via a competitive interaction with the glycine-binding site of NMDA receptors in cultured hippocampal neurons.

• Journal of Ginseng Research
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• 제29권3호
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• pp.119-125
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• 2005

The previous reports demonstrated that ginseng saponins, active ingredient of Panax ginseng, inhibited blood vessel contraction induced by various hormones or high $K^+$. Recently, we demonstrated that 20(R)- and 20(S)-ginsenoside $Rg_3$. regulate ion channel activities with differential manners. The aim of this study was to examine whether ginsenoside $Rg_3$ isomers also show differential effects on swine coronary artery contractionresponses induced by high $K^+$, serotonin (5-HT) or acetylcholine. Treatment of 20(S)- but not 20(R)-ginsenoside $Rg_3$ caused a concentration-dependent relaxation of coronary artery contracted by 25mM KCI. 20(S)- and 20(R)-ginsenoside $Rg_3$ induced significant relaxations of coronary artery contraction induced by 5-HT $(3{\mu}M)$ in the presence of endothelium with concentration-dependent manner and, also in the absence of endothelium only 20(S)-ginsenoside $Rg_3$ induced a strong Inhibition of coronary artery contraction induced by 5-HT in a concentration-dependent manner. 20(S)-ginsenoside $Rg_3$ caused relaxation of coronary artery in the absence and presence of endothelium. In contrast, treatment of 20(S)- and 20(R)-ginsenoside $Rg_3\;(100{\mu}M)$ did not show significant inhibition of coronary artery contraction induced by acetylcholine $(0.01\;to\;30{\mu}M)$ in the presence of endothelium, whereas both isomers caused significant inhibition of coronary artery contraction induced by acetylcholine $(0.01\;to\;30{\mu}M)$ in the absence of endothelium in a concentration-dependent manner. These findings indicate that 20(S)-or 20(R)-ginsenoside $Rg_3$ exhibits differential relaxation eff3cts of swine coronary artery contractions caused by high $K^+$, acetylcholine, and 5-HT treatment and that this differential vasorelaxing effects of ginsenoside $Rg_3$ isomers also might be dependent on endothelium.

• 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.

• 대한화장품학회지
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• 제46권4호
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• pp.349-360
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• 2020

최근 피부 기능 개선과 관련한 다양한 가능성으로 인해 화장품 소재로서 수요가 높아지고 있는 인삼 유래 사포닌의 한 종류인 ginsenoside Rd를 위한 생물 전환 제조 기술을 확립하였다. 홍삼 사포닌(RGS)에 포함된 ginsenoside Rb1을 Rd로 전환하기 위하여 상업용 효소를 탐색하였고 그 중 Viscoflow MG가 가장 효율적인 것을 확인하였다. Ginsenoside Rd로의 전환에 영향을 주는 요인을 최적화하기 위하여 반응표면분석법(RSM)을 통하여 실험 조건을 설계하였다. 주요 독립변수는 RGS 농도, 효소 농도와 반응 시간이었고 Box-Behnken design (BBD) 모델설계법에 따라 선정된 17 가지 조건으로 ginsenoside Rd로 전환을 수행하고 최적화 조건을 분석하였다. 전환된 Ginsenoside Rd의 농도는 0.3113 g/L에서 최대 0.5277 g/L까지였고 RGS 2%, 효소 1.25%를 13.5 h 반응시킨 조건에서 가장 높은 생성량을 보였다. 결론적으로, ginsenoside Rd 생물전환의 독립변수인 RGS 농도, 효소 농도는 p-value가 0.05보다 작은 값으로 유의미한 값을 나타내었고 각 독립변수 사이의 교호작용 중에서는 효소 농도와 반응 시간 사이의 교호 작용이 가장 큰 영향력을 갖고 있음을 확인하였다.

• Applied Biological Chemistry
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• 제36권4호
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• pp.260-264
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• 1993

인삼을 조미제품의 첨가성분으로 이용할 때 그 NaCl 농도에서 인삼성분의 안정성을 규명하기 위하여, 미삼과 홍삼정을 NaCl 농도별로 처리하여 pH, 색상 및 ginsenosides 함량을 조사한 결과, 미삼의 경우 NaCl 농도가 증가 할수록 pH는 높아졌으나 홍삼정 시험구에서는 유의적인 변화가 없었다. 색상은 NaCl 농도가 증가 될수록 감소하였다. n-BuOH extract 수율은 5% NaCl 농도에서 감소하였고 그 이상의 농도에서는 증가하는 경향을 나타내었으며, 증감 범위는 홍삼정이 컸다. Ginsenosides 함량은 diol계 saponin인 ginsenoside-Re, $-Rb_1$, $-Rb_2$, -Rc, -Rd 및 triol계 saponin인 ginsenoside-Re 모두 5% NaCl 농도에서 감소하였고 그 이상의 농도에서 증가하는 경향이었으며, 특히 ginsenoside-Re가 가장 민감한 증감의 변화를 보였다.

• 동의생리병리학회지
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• 제17권1호
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• pp.209-212
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• 2003

A wide variety of cancer chemotherapeutic agents have been shown to induce programmed cell death (PCD, apoptosis) in various tumor cell fines in vitro. This study was performed to know how ginsenoside Rc affect on SK-MEL-28 cell line, and how they induce the apoptosis. SK-MEL-28 cell lines were treated with various concentrations of ginsenoside Rc and cultured for various times. At cell cycle analysis, cells arrested at G2/M phase by ginsenoside Rc and apotosis percentage increased along with increasing concentration and time. TUNEL assay was performed to know whether SK-MEL-28 cell fine die as apoptosis or necrosis by ginsenoside Rc. As a result, fluorescence increased along with increasing time and concentration. Fas expressed on SK-MEL-28 cell lines membrane by ginsenoside Rc was identified using flow cytometer. Ginsenoside Rc induced apoptosis against SK-MEL-28 cell fines, and the apoptosis mechanism was identified as Fas-mediated apotosis.

• Journal of Ginseng Research
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• 제35권4호
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• pp.497-503
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• 2011

In order to enhance bioactive functionalities of ginseng, an acid impregnation processing was applied as a pre-treatment in producing red ginseng. Acid impregnation studies were conducted, and acids (ascorbic, malic, and citric acid) were selected. The optimal concentration of each acid was investigated in this study in terms of ginsenoside contents. The most concerned ginsenoside, $Rg_3$ was increased by ascorbic, malic, and citric acid pre-treated red ginseng up to 1 M acid concentration. In the case of ascorbic acid pre-treated red ginseng, $Rg_2$ concentration was increased depending on acid concentrations. Citric acid pre-treatment enhanced $Rg_2$, $Rg_3$, and $Rh_1+Rh_2$ formation in red ginseng. Therefore, ginsenoside patterns in red ginseng could be changed by acid impregnation pre-treatment depending on acid concentration and acid types. This research is expected to contribute to the development of the ginseng industry via new red ginseng products with selective and intensified functionality.

• Journal of Ginseng Research
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• 제37권4호
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• pp.451-456
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• 2013

Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro. However, previous studies have focused on the pharmacokinetics of a single metabolite or the parent compound and have not described the pharmacokinetics of both compounds in humans. To investigate the pharmacokinetics of ginsenoside Rb1 and compound K, we performed an open-label, single-oral dose pharmacokinetic study using Korean Red Ginseng extract. We enrolled 10 healthy Korean male volunteers in this study. Serial blood samples were collected during 36 h after Korean Red Ginseng extract administration to determine plasma concentrations of ginsenoside Rb1 and compound K. The mean maximum plasma concentration of compound K was $8.35{\pm}3.19$ ng/mL, which was significantly higher than that of ginsenoside Rb1 ($3.94{\pm}1.97$ ng/mL). The half-life of compound K was 7 times shorter than that of ginsenoside Rb1. These results suggest that the pharmacokinetics, especially absorption, of compound K are not influenced by the pharmacokinetics of its parent compound, except the time to reach the maximum plasma concentration The delayed absorption of compound K support the evidence that the intestinal microflora play an important role in the transformation of ginsenoside Rb1 to compound K.

• 대한화장품학회지
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• 제49권4호
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• pp.375-383
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• 2023

최근 다양한 피부 기능 개선 효과로 기능성 소재로서 활용도가 높은 홍삼 사포닌의 한 종류인 진세노사이드 Rg3를 위한 사과산(malic acid)활용 전환 방법을 확인하였다. 실험 계획법인 반응 표면 분석법(RSM)을 활용하여 진세노사이드 Rg3로의 전환에 영향을 주는 요인을 최적화하기 위한 실험 조건을 설계 및 검증하였다. 주요 독립변수는 사과산 농도, 반응 온도와 반응 시간이었고 Box-Behnken design (BBD)법에 따라 설계된 실험 조건으로 진세노사이드 Rg3로 전환을 수행하고 최적화 조건을 분석하였다. 전환된 진세노사이드 Rg3의 농도는 1.548 mg/L에서 최대 4.558 mg/L까지 확인되었고 사과산 1%, 50℃, 9 h에서 가장 높은 양의 진세노사이드 Rg3생성량을 보였다. 결론적으로, 진세노사이드 Rg3의 생성에 가장 영향을 미치는 요인은 사과산의 농도, 반응 시간, 온도 순이었다. 또한, 사과산의 농도와 반응 시간의 교호작용이 반응 온도 요인보다 영향도가 큰 것을 확인하였다.

• KSBB Journal
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• 제17권1호
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• pp.110-113
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• 2002

본 연구에서는 고려인삼세포 현탁배양에 의한 회분배양 실험에서 쟈스몬산과 안식향산이 ginsenoside 생산에 미치는 영향을 조사하였다. 세포내에서 이차대사계를 활성화시키는 중간 신호전달 물질(signal transducer)로 알려진 쟈스몬산은 50 $\mu$M 이상의 농도로 투여되었을 때 ginsenoside 생산을 증가시킬 수 있었다. 그 이상의 농도에서는 세포 생장을 저하시키는 결과를 보였다. 쟈스몬산 투여 후 12시간가지 ginsenoside의 생산은 증가하였고, 그 이후에는 더 이상 증가하지 않았다. 안식향산과 쟈스몬산을 동시에 투여하면 ginsenoside 생산이 9.6배 증가하는 결과를 나타내었다. 이는 쟈스몬산 단독투여 때보다 2.2배 증가된 결과였다.