• Biomolecules & Therapeutics
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• 제16권3호
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• pp.277-285
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• 2008

Panax ginseng C.A. Mayer (Araliaceae, P. ginseng) has been used for the enhancement of vascular and immune functions in Korea and Japan for a long time. Ginsenoside $Rb_1$ and $Rg_3$ isolated from P. ginseng head-part butanolic extract (PGHB) were investigated for anti-inflammatory activity. Ginsenosides and PGHB did not affect the cell viability within $0\;-\;100\;{\mu}g/ml$ concentration to RAW 264.7 murine macrophage cells. Ginsenosides and PGHB inhibited partly lipopolysaccharide (LPS)-induced nitrite production in a dose-dependent manner. The ginsenosides and PGHB showed partially chemical nitric oxide (NO) quenching (maximum 40%) in the cell-free system. Also, ginsenoside $Rb_1$ and $Rg_3$ inhibited markedly approximately 74 and 54% of inducible nitric oxide synthase (iNOS) mRNA transcription from LPS-induced RAW 264.7 cells. Taken together, the inhibitory effect of ginsenosides and PGHB on NO production did not occur as a result of cell viability, but was caused by both the chemical NO quenching and the regulation of iNOS. Additionally, the ginsenoside $Rb_1$ and PGHB inhibited prostaglandin $E_2$ ($PGE_2$) synthesis in a concentration-dependent manner, showed approximately 70-98% inhibition at $100\;{\mu}g/ml$ concentration. And the treatment with ginsenosides and PGHB attenuated partially LPS-upregulated cyclooxygenase-2 (COX-2) gene transcription. Ginsenoside $Rg_3$ suppressed LPS-stimulated interleukin-6 (IL-6) level to the basal in RAW 264.7 cells. From these results, ginsenoside $Rb_1,\;Rg_3$, and PGHB may be useful for the relief and retardation of immunological inflammatory responses and its action may occur through the reduction of inflammatory mediators, including NO, $PGE_2$, and IL-6 production.

• Mass Spectrometry Letters
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• 제12권2호
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• pp.53-58
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• 2021

Previous in vitro studies have demonstrated that ginsenoside Rc inhibits UGT1A9, but there are no available data to indicate that ginsenoside Rc inhibits UGT1A9 in vivo. The effect of single and repeated intravenous injection of ginsenoside Rc was evaluated on the pharmacokinetics of mycophenolic acid. After injection of ginsenoside Rc (5 mg/kg for one day or 3 mg/kg for five days), 2-mg mycophenolic acid was intravenously injected, and the pharmacokinetics of mycophenolic acid and mycophenolic acid-β-glucuronide were determined. Concentrations of mycophenolic acid and its metabolite from rat plasma were analyzed using a liquid chromatography-triple quadrupole mass spectrometry. Single or repeated pretreatment with ginsenoside Rc had no significant effects on the pharmacokinetics of mycophenolic acid (P > 0.05): The mean difference in maximum plasma concentration (C_max) and area under the concentration-time curve (AUC_inf) were within 0.83- and 0.62-fold, respectively, compared with those in the absence of the ginsenoside Rc. These results indicate that ginsenoside Rc has a negligible effect on the disposition of mycophenolic acid in vivo despite in vitro findings indicating that ginsenoside Rc is a selective UGT1A9 inhibitor. As a result, ginsenoside Rc has little possibility of interacting with drugs that are metabolized by UGT1A9, including mycophenolic acid.

• Journal of Applied Biological Chemistry
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• 제62권1호
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• pp.87-91
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• 2019

The contents of major ginsenosides (ginsenosides Rb1, ginsenoside Rc, ginsenoside Rd, ginsenoside Re, ginsenoside Rf, and ginsenoside Rg1) in ginseng cultivated in different areas in Korea, ginseng that underwent different cultivation processes and ages, and ginseng cultivated in different countries were determined using high-performance liquid chromatography equipped with UV/VIS detector. Ginsenoside Rc was the most abundant ginsenoside in all different ginseng samples. The highest total concentration of major ginsenosides was found in the ginseng cultivated in Jinan (0.931 mg/g) and 4-year grown red ginseng (1.785 mg/g). Major ginsenosides were the most abundant in Korean ginseng (1.264 mg/g), compared to those in Chinese and American ginseng. The results of this study showed the different contents of major ginsenosides in the ginseng samples tested and emphasized which sample could contain high yield of ginsenosides.

• Journal of Ginseng Research
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• 제38권1호
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• pp.47-51
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• 2014

The transformation of ginsenoside Rb1 into a specific minor ginsenoside using Aspergillus niger KCCM 11239, as well as the identification of the transformed products and the pathway via thin layer chromatography and high performance liquid chromatography were evaluated to develop a new biologically active material. The conversion of ginsenoside Rb1 generated Rd, Rg3, Rh2, and compound K although the reaction rates were low due to the low concentration. In enzymatic conversion, all of the ginsenoside Rb1 was converted to ginsenoside Rd and ginsenoside Rg3 after 24 h of incubation. The crude enzyme (b-glucosidase) from A. niger KCCM 11239 hydrolyzed the ${\beta}$-($1{\rightarrow}6$)-glucosidic linkage at the C-20 of ginsenoside Rb1 to generate ginsenoside Rd and ginsenoside Rg3. Our experimental demonstration showing that A. niger KCCM 11239 produces the ginsenoside-hydrolyzing b-glucosidase reflects the feasibility of developing a specific bioconversion process to obtain active minor ginsenosides.

• Journal of Ginseng Research
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• 제18권1호
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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.

• Journal of Ginseng Research
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• 제40권2호
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• pp.121-126
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• 2016

Background: Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. However, the usage of ginsenoside F1 is restricted owing to the small amount found in Korean ginseng. Methods: To enhance the production of ginsenoside F1 as a 10 g unit with high specificity, yield, and purity, an enzymatic bioconversion method was developed to adopt the commercial enzyme Cellulase KN from Aspergillus niger with food grade, which has ginsenoside-transforming ability. The proposed optimum reaction conditions of Cellulase KN were pH 5.0 and $50^{\circ}C$. Results: Cellulase KN could effectively transform the ginsenosides Re and Rg1 into F1. A scaled-up biotransformation reaction was performed in a 10 L jar fermenter at pH 5.0 and $50^{\circ}C$ for 48 h with protopanaxatriol-type ginsenoside mixture (at a concentration of 10 mg/mL) from ginseng roots. Finally, 13.0 g of F1 was produced from 50 g of protopanaxatriol-type ginsenoside mixture with $91.5{\pm}1.1%$ chromatographic purity. Conclusion: The results suggest that this enzymatic method could be exploited usefully for the preparation of ginsenoside F1 to be used in cosmetic, functional food, and pharmaceutical industries.

• Preventive Nutrition and Food Science
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• 제13권3호
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• pp.212-218
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• 2008

We extracted red ginseng with various alcohol concentrations and evaluated total carbohydrate, uronic acid, polyphenols compounds and ginsenoside contents, and yields of alcohol extract. The water extraction (0% alcohol extraction) showed a high level of total carbohydrate content. 10% and 20% alcohol extraction showed the highest uronic acid contents (7,978.8 and $7,872.7\;{\mu}g/mL$ of extract, respectively). The efficiency order of the red ginseng extract (RGE) preparations in liberating polyphenols was: $0{\sim}50%$ alcohol${\geq}\;60%$ alcohol> $70{\sim}90%$ alcohol. Solid contents in RGE were decreased with increased alcohol concentration; the same tendency as with the results of total carbohydrate content. Total ginsenoside contents in $20{\sim}50%$ alcohol extracts showed similar levels ($442,962.9{\sim}47,930.8\;{\mu}g/mL$ of extract). Water extraction showed the lowest ginsenoside content ($14,509.4\;{\mu}g/mL$ of extract). The ginsenoside contents at above 60% alcohol were decreased with increased alcohol concentration. Generally, ginsenoside (Rg2, Rg1, Rf, Re, Rd, Rb2, Rc and Rb1) contents were increased with increased alcohol concentrations. However, Rg3 content was decreased with increases in alcohol concentration.

• Journal of Ginseng Research
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• 제44권2호
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• pp.215-221
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• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• Journal of Ginseng Research
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• 제10권1호
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• pp.66-75
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• 1986

Fuiarium solani 와 Phytophthora cactorum 이 인삼 사포닌 성분에 어떠한 영향을 미치는가를 알기 위해서 각 첨가배지에서의 균사생육과 접종된 인삼분말의 사포닌 분석실험으로 다음과 같은 결과를 얻었다. Fuiarium solani는 수삼의 물추출물 농도에 따라 생육이 억제되었으며 조사포닌 20ppm 첨가까지 생육이 촉진되었으나 50ppm이상에서는 불규칙적인 생육 억제효과가 있었다. 그리고 nystatin은 농도에 다라 생육을 억제하였다. Phytophthora cactorum은 수삼의 물추출액, 조사포닌의 농동에 따라서 생육은 촉진되었으며 nystatin은 생육에 영향을 미치지 않았다. F. solani 및 P. cactorum 으로 접종된 인삼분말은 ginsenoside Ra, Ro peak가 나타나지 않았으며 F. solani에 의해 PD 계 ginsenoside가 3.0% 증가되고 PT계 ginsenosides는 34.9% 감소되었다. P. cactorum의 경우는 PD 계 ginsenoside가 21.1% 증가, PT계 ginsenosides는 23.5% 감소하였다. 두 균주에 의해 PD, PT계 ginsenoside의 변화가 다르게 나타났지만 PD/PT비는 동일하게 58.4%씩 각각 높아졌다. 인삼의 총 사포닌 함량은 F. solani에 의해 17.8%, P. cactorum에 의해서 2.5%씩 각각 감소하였다.

• 한방재활의학과학회지
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• 제31권1호
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• pp.95-108
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• 2021

Objectives This study was conducted to investigate the beta-glucan, ginsenoside content, antioxidant activity and safety of modified Kyungohkgo added to Sparassis crispa and Hericium erinaceum. Methods The marker compounds contents, antioxidant activity and safety of modified Kyungohkgo were tested. The contents of beta-glucan and ginsenoside Rb1, Rg1, and Rg3 marker compounds were measured, the antioxidant activity was measured using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, and a safety test was conducted via single dose toxicity assessment. Results Analyzing the contents of marker compounds showed 351.75 mg/g of beta-glucan, 0.0327 mg/g of ginsenoside Rb1 and 0.0802 mg/g of ginsenosai Rg3. In the DPPH free radical scavenging activity, the inhibition concentration 50% of modified Kyungohkgo was 0.2880%. The scavenging activity of modified Kyungohkgo was 5.49% activity at 0.05% concentration, 89.66% activity at 0.5% concentration, 94.68% activity at 1% concentration, and 96.06% activity at 5% concentration. In the single dose toxicity test of modified Kyungohkgo, a dose of 2,000 mg/kg B.W. was set at its highest capacity and observed after oral administration to female and male rats. No toxicological findings were recognized. It was observed that the resulting lethal dose can be set to 2,000 mg/kg B.W. or higher for both females and males. Conclusions The results of the experiment on modified Kyungohkgo showed that the marker compounds contents were beta-glucan and ginsenoside Rb1 and Rg3, that antioxidant activity was observed through the DPPH free radical scavenging activity, and safety was confirmed through the single dose toxicity assessment.