• Title/Summary/Keyword: ginsenoside Rg3

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A Structure-Function Relationship Exists for Ginsenosides in Reducing Cell Proliferation and Inducing Apoptosis in THP-1 Cells

  • Popovich David G.;Kitts David D.
    • Proceedings of the Ginseng society Conference
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    • 2002.10a
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    • pp.545-555
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    • 2002
  • Ginsenosides of 20(S)-protopanaxadiol and 20(S)-protopanaxatriol classification including the aglycones, PD, PI and ginsenosides Rh2, Rhl were shown to posses characteristic effects on proliferation of THP-l human leukaemia cells. A similar result was not apparent for ginsenoside Rg3 or dexamathasone. The concentration to inhibit $50\%$ of cells $(LC_{50})$ for PD, Rh2, PI and Rhl were 13 ${\mu}g/mL,\;15{\mu}g/mL,\;19{\mu}g/mL\;and\;210\;{\mu}g/mL$ respectively. Cell cycle analysis showed apoptosis with PD and PI treatment of THP-1 cells resulting in a build up of sub-G1 cells after 24, 48 and 72 hours of treatment. Rh2, and dexamathasone treatments also increased apoptotic cells after 24 hours, where as Rhl did not. After 48 and 72 hours Rh2, Rhl and dexamathasone similarly increased apoptosis, but these effects were significantly (P<0.05) lower than observed for both PD and PI treatments. Furthermore, treatments that produced the largest build up of apoptotic cells were also found to have the largest release of lactate dehydrogenase (LDH). It can be concluded from these studies that the presence of sugars to PD and PI aglycone structure reduces the potency to induce apoptosis, and alternately alter membrane integrity. These cytotoxic effects to THP-l cells were different from dexamethasone.

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Methods on improvements of the poor oral bioavailability of ginsenosides: Pre-processing, structural modification, drug combination, and micro- or nano- delivery system

  • Qi-rui Hu;Huan Hong;Zhi-hong Zhang;Hua Feng;Ting Luo;Jing Li;Ze-yuan Deng;Fang Chen
    • Journal of Ginseng Research
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    • v.47 no.6
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    • pp.694-705
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    • 2023
  • Panax ginseng Meyer is a traditional Chinese medicine that is widely used as tonic in Asia. The main pharmacologically active components of ginseng are the dammarane-type ginsenosides, which have been shown to have anti-cancer, anti-inflammatory, immunoregulatory, neuroprotective, and metabolic regulatory activities. Moreover, some of ginsenosides (eg, Rh2 and Rg3) have been developed into nutraceuticals. However, the utilization of ginsenosides in clinic is restrictive due to poor permeability in cells and low bioavailability in human body. Obviously, the dammarane skeleton and glycosyls of ginsenosides are responsible for these limitations. Therefore, improving the oral bioavailability of ginsenosides has become a pressing issue. Here, based on the structures of ginsenosides, we summarized the understanding of the factors affecting the oral bioavailability of ginsenosides, introduced the methods to enhance the oral bioavailability and proposed the future perspectives on improving the oral bioavailability of ginsenosides.

Effects of Compositions of Saponin Fraction from Korean Red Ginseng in the Relaxation of Rabbit and Rat Corpus Cavernosum (토끼와 흰쥐 음경해면체 이완작용에 미치는 홍삼사포닌 분획별 효과)

  • Choi Young Deuk;Park Jin Ah;Choi Hyung Ki;Nam Ki Yeul
    • Journal of Ginseng Research
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    • v.23 no.1 s.53
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    • pp.13-20
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    • 1999
  • We previously reported that Korean red ginseng (KRG) has a relaxation effect on the smooth muscles of corpus cavernosum via nitric oxide (NO) pathway and calcium and potassium channels. However, it is suggested that the active ingredients of KRG might be different depending on the sources of preparation, and there might be differences in actions for different compositions. We first investigated the composition of KRG saponins according to the extractions of the various sources of KRG, then with these extractions the relaxation effects were evaluated in vitro and hemodynamical in vivo using New Zealand white rabbit and rat corpus cavernosum. The total compositions of ginsenoside $(G-Rb_1,\;-Rb_2,\;-Rc,\;-Rd,\;G-Re,\;-Rf,\;-Rg_1)$ in fractionated KRG saponin designated as TS-1, TS-2, TS-3 were $41\%,\;40\%,\;and\;62\%,$ respectively, and the ratios of PD saponin and PT saponin (PD/PT) were 1,55, 1.72, 2.25, and 2.61, the values of which were statistically significant. In vitro studies using the rabbit corpus cavernosal muscle strips, the KRG saponin relaxed cavernosal strips in a dose-dependent manner, and same results were observed in in vivo studies, that KRG saponin increased the intracavernosal pressure in the rat. There was difference in the efficacy according to fractionation techniques. The differences in the total contents of ginsenosides did not affect relaxation, rather PT saponin content was statistically related to the degree of cavernosal relaxation, and this action presumed to be mediated by NO pathway and calcium and potassium channels. In conclusion, KRG exerts relaxation which is a key step in erection via combination of effects on NO system or calcium and potassium channels. The efficacy of this action is different to the sources of ginseng, which is affected by the different composition of ginsenosides $(G-Rb_1,\;-Rb_2,\;-Rc,\;-Rd,\;G-Re,\;-Rf,\;-Rg_1).$ Thus the further studies on the active ingredients such as minor ginsenosides and non-saponin components of red ginseng with maximum potency should be sought.

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Effects of High Temperature Heating on the Some Physicochemical Properties of Korean Red Ginseng (Panax ginseng C.A. Meyer) Water Extract (고온 열처리가 홍삼물추출물의 이화학적 특성에 미치는 영향)

  • Kwak, Yi-Seong;Choi, Keum-Hee;Kyung, Jong-Soo;Won, Jun-Yeon;Rhee, Man-Hee;Lee, Jae-Gon;Hwang, Mi-Sun;Kim, Seok-Chang;Park, Chae-Kyu;Song, Kyung-Bin;Han, Gyeong-Ho
    • Journal of Ginseng Research
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    • v.32 no.2
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    • pp.120-126
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    • 2008
  • This study was carried out to investigate the some physicochemical properties of Korean red ginseng (Panax ginseng C.A. Meyer) water extract (RGWE) after heated with high temperatures above $100^{\circ}C$ for 2 hours. RGWEs were heated at 100, 110 and $120^{\circ}C$ for 2 hours by using autoclave. After RGWEs were heated at high temperature for 2 hours without not adjustment of pH, the changes of saponin, free sugars, mineral and color in the RGWEs were investigated. Total ginsenoside content in control was 1.99%, while those of RGWE were 1.65, 1.49 and 1.29% when treated at 100, 110 and $120^{\circ}C$, respectively. The contents of total ginsenoside showed decreased tendency as heating temperatures were increased. The ginsenoside-$Rh_{2}$ and $-Rg_{3}$, which have been reported as very stable red ginseng ginsenosides, showed relatively strong spots on TLC when RGWEs were heated at 110 and $120^{\circ}C$. In case of free sugars in RGWEs, fructose, glucose and maltose showed high contents when compared with control, while Fe, Ca and Mg ions showed very low contents. Value of L in RGWE treated with high temperature was almost the same with control, while values of a and b were increased. Values of a were increased from -0.86 of control to +0.04, +0.05 and +1.14 when treated with 100, 110 and $120^{\circ}C$, respectively. Values of b also were increased from 27.68 of control to 33.61, 33.61 and 37.42 when treated with 100, 110 and $120^{\circ}C$, respectively. Values of total color in RGWEs treated with high temperatures, E, were finally increased by values of a and b.

Effect of aeration process on changes of prosapogenin content and antioxidant activity of red ginseng powder extract (Aeration 공정 처리가 홍삼분말 추출물의 프로사포게닌의 함량 변화와 항산화 활성에 미치는 영향)

  • Ryu, Hee-Jeong;Jung, Chul-Jong;Seo, Jeong-Gyun;Li, Xian;Yu, Yeong-Eun;Beik, Gyung-Yun
    • Korean Journal of Food Science and Technology
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    • v.51 no.6
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    • pp.576-583
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    • 2019
  • The effect of aeration process in causing changes in the prosapogenin content and the antioxidant activity of red ginseng powder extracts was investigated. With respect to the color change of the extracts, the L-value and b-value decreased significantly with the lapse of extraction time both with and without the aeration process. The a-value increased with the lapse of the extraction time in the non-aeration process but decreased in the aeration process. This result suggests that when the aeration process was performed, the lightness, yellowness, and redness decreased with the lapse of the extraction time, resulting in a darker color. The total polyphenolic and total flavonoid contents were the highest at 0.84 and 0.96 mg Gallic Acid Equivalent (GAE)/mL, 21.77 and 21.93 mg GAE/mL at 24 h and 36 h, respectively for the aerated red ginseng powder extracts. The DPPH, ABTS, H2O2 scavenging activity, and reducing power were measured to confirm the antioxidant effects of red ginseng powder extracts after the aeration process. Thus, the antioxidant activity was increased in the aerated red ginseng powder extracts. In addition, when comparing the contents of Rb1, Rg1, and Rg3, the content of Rg3 was significantly different, and it was confirmed that a large amount was produced in the aerated red ginseng extracts. These results indicate that the red ginseng extracts subjected to the aeration process are superior than the ones processed by the non-aeration process.

FURTHER PURIFIED GINSENG EXTRACT FRACTION (D-O-ANA) FOR INSULIN RELEASE AND ITS MODE OF ACTION COMPARED WITH THE ISOLATED RESIDUAL COMPONENTS (인삼성분 D-O-ANa이 인슐린 분비에 미치는 영향 및 작용기전에 관한연구)

  • KIMURA Masayasu;SUZUKI Jun;WAKI Isami;KIMURA Ikuko;TANAKA Osamu;MATSU-URA Hiromichi
    • Proceedings of the Ginseng society Conference
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    • 1984.09a
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    • pp.191-197
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    • 1984
  • A further purified fraction (D-O-ANa) was obtained from DPG 3-2 fraction of Ginseng Radix by complete removal of saponins, nucleosides, nucleic acid bases, amino acids, and sugars. D-O-ANa - induced insulin release was investigated to compare with that of DPG 3-2 and other isolated components. Among the sub fractions of DPG 3-2, D-O-ANa exhibited the most potent release of insulin with or without high concentrations of glucose, and it particularly enhanced the second phase of glucose-induced insulin release. DGP 3-2 potentiated significantly the glucose-induced insulin release from the isolated islets of diabetic mice at increasing concentrations of extracellular calcium ions (0.16 - 2.5 mM). A definite relationship was found between calcium $(^{45}Ca)$ uptake and insulin release. Ginsenoside $(G)-Rb_1\;and\;G-Rg_1$ did not enhance the glucose-induced insulin release. The effect of ginseng saponins was blocked by glucose (16.7 mM), being distinctly different from the glucose-potentiated effect of DPG 3-2. The insulin release effect of $G-Rg_1$ was unaffected by the presence or absence of extracellular $Ca^{2+}$ and theophylline. Adenosine also increased insulin release from isolated islets, but had no effect on perfused rat pancreas. Arginine stimulated insulin release less evidently than D-O-ANa, though arginineand adenosine-induced glucagon releases were more remarkable. In conclusion, D-O-ANa appears to be a major fraction in insulin release activity of ginseng and its mode of action may be related to $Ca^{2+}$ ion uptake. This physiological mechanism was distinct from that of the abnormal release induced by ginseng saponins.

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Characteristic study on the chemical components of Korean curved ginseng products

  • Cho, Chang-Won;Kim, Young-Chan;Kang, Jin-Hee;Rhee, Young Kyoung;Choi, Sang Yoon;Kim, Kyung-Tack;Lee, Young-Chul;Hong, Hee-Do
    • Journal of Ginseng Research
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    • v.37 no.3
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    • pp.349-354
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    • 2013
  • Dried ginseng (DG) is in fact the representing ginseng product in the worldwide market. Although it is made in various packages depending on the processing method, size and age of DG, basic scientific data reporting the chemical components are limited. In this study, 4-year-old curved ginseng (CG), one of the domestic DG products, was selected for further investigation. Eighty-six samples of 30 and 50 piece-grade CG, which are the most widely distributed in the market, were collected for 5 yr. Their major components, such as moisture, total sugar, acidic polysaccharides, total phenolic compounds, and saponins, were analyzed to figure out the standard quality characteristics. The moisture content of all CG samples was less than 15%. The total water-soluble sugar contents were 22.9% to 47.8% and 23.2% to 49.5% in the 30 and 50 piece-grade CG, respectively. The acidic polysaccharide contents were 3.6% to 6.7% and 2.9% to 6.9% in the 30 and 50 piece-grade CG, respectively. The total phenolic compound content was 0.4% to 0.5% in CG, regardless of the piece-grade. The crude saponin content, which represents the active component of ginseng, was over 2% in all samples. In 30 piece-grade CG samples, the contents of major ginsenosides, Rb1, Rf, and Rg1, were 2.2 to 4.7 mg/g, 0.4 to 1.3 mg/g, and 1.6 to 4.0 mg/g, respectively. The ginsenoside contents in 50 piece-grade CG samples were 2.1 to 3.9 mg/g (Rb1), 0.5 to 1.2 mg/g (Rf), and 1.3 to 3.4 mg/g (Rg1). Overall, since there were relatively high standard deviation and coefficient of variation in all the chemical component contents that were assessed, we found some difficulties in showing the CG standard chemical component characteristics by average, standard deviation, and other statistical analysis factors.

Effect of the Extruded Ginseng on Antioxidant Activity (압출 성형 인삼의 항산화 활성 증강 효과)

  • Kim, Sung-Hwan
    • Journal of the East Asian Society of Dietary Life
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    • v.17 no.3
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    • pp.402-408
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    • 2007
  • This study was conducted in order to evaluate the antioxidant activity of extruded ginseng in different extracted fractions. Each of the fractions obtained from extruded ginseng and ginseng (control) were extracted with 80% ethanol, and then the lipophilic components were removed with ether while the hydrophilic components were separated with water-saturated butanol. Each of the 80% ethanol/butanol/water layers were collected and evaporated to acquire samples for tests of saponin content and antioxidant activity. The antioxidant activity of extruded ginseng fractions and ginseng fractions were determined via the oxygen radical absorbance capacity (ORAC) assay. Overall, the extruded ginseng samples harbored saponin contents of 2.2 (Rg1), 2.3 (Re), 1.2 (Rc), 1.3 (Rb2), and 2.2 (Rd) times that measured in the ginseng prior to extrusion. Antioxidant capacity was also higher, not only in the 80% ethanol/butanol which harbor a significant quantity of saponin, but also in the water fractions, which harbor relatively low quantities of saponin as compared to the control samples. All three of the fractions extracted from extruded ginseng evidence significantly higher antioxidant capacity than the controls (0.05

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Simultaneous determination and difference evaluation of 14 ginsenosides in Panax ginseng roots cultivated in different areas and ages by high-performance liquid chromatography coupled with triple quadrupole mass spectrometer in the multiple reaction-monitoring mode combined with multivariate statistical analysis

  • Xiu, Yang;Li, Xue;Sun, Xiuli;Xiao, Dan;Miao, Rui;Zhao, Huanxi;Liu, Shuying
    • Journal of Ginseng Research
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    • v.43 no.4
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    • pp.508-516
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    • 2019
  • Background: Ginsenosides are not only the principal bioactive components but also the important indexes to the quality assessment of Panax ginseng Meyer. Their contents in cultivated ginseng vary with the growth environment and age. The present study aimed at evaluating the significant difference between 36 cultivated ginseng of different cultivation areas and ages based on the simultaneously determined contents of 14 ginsenosides. Methods: A high-performance liquid chromatography (HPLC) coupled with triple quadrupole mass spectrometer (MS) method was developed and used in the multiple reaction-monitoring (MRM) mode (HPLC-MRM/MS) for the quantitative analysis of ginsenosides. Multivariate statistical analysis, such as principal component analysis and partial least squares-discriminant analysis, was applied to discriminate ginseng samples of various cultivation areas and ages and to discover the differentially accumulated ginsenoside markers. Results: The developed HPLC-MRM/MS method was validated to be precise, accurate, stable, sensitive, and repeatable for the simultaneous determination of 14 ginsenosides. It was found that the 3- and 5-yr-old ginseng samples were differentiated distinctly by all means of multivariate statistical analysis, whereas the 4-yr-old samples exhibited similarity to either 3- or 5-yr-old samples in the contents of ginsenosides. Among the 14 detected ginsenosides, Rg1, Rb1, Rb2, Rc, 20(S)-Rf, 20(S)-Rh1, and Rb3 were identified as potential markers for the differentiation of cultivation ages. In addition, the 5-yr-old samples were able to be classified in cultivation area based on the contents of ginsenosides, whereas the 3- and 4-yr-old samples showed little differences in cultivation area. Conclusion: This study demonstrated that the HPLC-MRM/MS method combined with multivariate statistical analysis provides deep insight into the accumulation characteristics of ginsenosides and could be used to differentiate ginseng that are cultivated in different areas and ages.

Blood flow-improving activity of methyl jasmonate-treated adventitious roots of mountain ginseng

  • Ban, Young-Hwan;Cha, Yeseul;Choi, Jieun;An, Eun Suk;Lee, Ji Young;Han, Nu Ry;Seo, Da Woom;Jung, Gooyoung;Jeong, Da-Hye;Rhee, Man Hee;Choi, Ehn-Kyoung;Kim, Yun-Bae
    • Laboraroty Animal Research
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    • v.33 no.2
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    • pp.105-113
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    • 2017
  • insenosides from Panax ginseng are well known for their diverse pharmacological effects including antithrombotic activity. Since adventitious roots of mountain ginseng (ARMG) also contain various ginsenosides, blood flow-improving effects of the dried powder and extract of ARMG were investigated. Rats were orally administered with dried powder (PARMG) or ethanol extract (EARMG) of ARMG (125, 250 or 500 mg/kg) or aspirin (30 mg/kg, a reference control) for 3 weeks. Forty min after the final administration, carotid arterial thrombosis was induced by applying a 70% $FeCl_3$-soaked filter paper outside the arterial wall for 5 min, and the blood flow was monitored with a laser Doppler probe. Both PARMG and EARMG delayed the $FeCl_3$-induced arterial occlusion in a dose-dependent manner, doubling the occlusion time at high doses. In mechanism studies, a high concentration of EARMG inhibited platelet aggregation induced by collagen in vitro. In addition, EARMG improved the blood lipid profiles, decreasing triglyceride and cholesterol levels. Although additional action mechanisms remain to be clarified, it is suggested that ARMG containing high amount of ginsenosides such as $Rg_3$ improves blood flow not only by inhibiting oxidative thrombosis, but also by modifying blood lipid profiles.