• Title/Summary/Keyword: ginsenoside Rh3

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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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Antioxidant and Antimicrobial Activities of Various Solvent Fractions of Fine Ginseng Root

  • Lim, Jae-Kag;Kang, Ho-Jin;Kang, Suk-Nam;Lee, Boo-Yong
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.513-518
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    • 2009
  • This study was carried out to investigate the changes of yield, total phenolics, saponin content and composition, antimicrobial, and antioxidant activities of various fractions of fine ginseng root (Panax ginseng C.A. Mayer) by maceration method in the order of increasing polarity (hexane, chloroform, ethyl acetate, butanol, and water). Butanol fraction showed the highest total saponin content compare to other fractions. Hexane fraction could harvest significantly high ginsenoside Rg2, Rg1, and Rf (p<0.05). And the contents of ginsenoside Rh1, Rg3, and Rg1 showed relatively higher in the fraction of ethyl acetate than other fractions. The system of hexane-chloroform-ethyl aceate-butanol showed relatively high content of ginsenoside Re, Rd, Rc, Rb3, and Rb1. However, the last fraction of water still remained lots of Rb2 content. The fraction of water was the highest phenolics. The 1,1-diphenyl-2-picryhydrazil, superoxide, and hydroxyl radical scavenging activity of water fraction was higher than the other fractions. In antimicrobial activity, the fraction of hexane showed relatively high antimicrobial activity against Pseudomonas aeruginosa, Salmonella typhimurium, Staphylococcus aureus, Bacillus cereus, and Escherichia coli. And the fractions of the chloroform and ethyl acetate showed higher antimicrobial activities than the other samples in against P. aeruginosa and S. typhimurium.

The effect of extrusion conditions on the acidic polysaccharide, ginsenoside contents and antioxidant properties of extruded Korean red ginseng

  • Gui, Ying;Ryu, Gi Hyung
    • Journal of Ginseng Research
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    • v.37 no.2
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    • pp.219-226
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    • 2013
  • This study was conducted to investigate the effect of extrusion conditions (moisture content 20% and 30%, screw speed 200 and 250 rpm, barrel temperature $115^{\circ}C$ and $130^{\circ}C$) on the acidic polysaccharide, ginsenoside contents and antioxidant properties of extruded Korean red ginseng (KRG). Extruded KRGs showed relatively higher amounts of acidic polysaccharide (6.80% to 9.34%) than non-extruded KRG (4.34%). Increased barrel temperature and screw speed significantly increased the content of acidic polysaccharide. The major ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, Rg2s, Rg3s, Rh1, and Rg3r) of KRG increased through extrusion, while the ginsenoside (Rg1) decreased. The EX8 (moisture 30%, screw speed 250 rpm, and temperature $130^{\circ}C$) had more total phenolics and had a better scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals than those of extruded KRG samples. The extrusion cooking showed a significant increase (6.8% to 20.9%) in reducing power. Increased barrel temperature significantly increased the values of reducing power, the highest value was 1.152 obtained from EX4 (feed moisture 20%, screw speed 250 rpm, and temperature $130^{\circ}C$). These results suggest that extrusion conditions can be optimized to retain the health promoting compounds in KRG products.

20(S)-ginsenoside Rh2 induces caspase-dependent promyelocytic leukemia-retinoic acid receptor A degradation in NB4 cells via Akt/Bax/caspase9 and TNF-α/caspase8 signaling cascades

  • Zhu, Sirui;Liu, Xiaoli;Xue, Mei;Li, Yu;Cai, Danhong;Wang, Shijun;Zhang, Liang
    • Journal of Ginseng Research
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    • v.45 no.2
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    • pp.295-304
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    • 2021
  • Background: Acute promyelocytic leukemia (APL) is a hematopoietic malignancy driven by promyelocytic leukemia-retinoic acid receptor A (PML-RARA) fusion gene. The therapeutic drugs currently used to treat APL have adverse effects. 20(S)-ginsenoside Rh2 (GRh2) is an anticancer medicine with high effectiveness and low toxicity. However, the underlying anticancer mechanisms of GRh2-induced PML-RARA degradation and apoptosis in human APL cell line (NB4 cells) remain unclear. Methods: Apoptosis-related indicators and PML-RARA expression were determined to investigate the effect of GRh2 on NB4 cells. Z-VAD-FMK, LY294002, and C 87, as inhibitors of caspase, and the phosphatidylinositol 3-kinase (PI3K) and tumor necrosis factor-α (TNF-α) pathways were used to clarify the relationship between GRh2-induced apoptosis and PML-RARA degradation. Results: GRh2 dose- and time-dependently decreased NB4 cell viability. GRh2-induced apoptosis, cell cycle arrest, and caspase3, caspase8, and caspase9 activation in NB4 cells after a 12-hour treatment. GRh2-induced apoptosis in NB4 cells was accompanied by massive production of reactive oxygen species, mitochondrial damage and upregulated Bax/Bcl-2 expression. GRh2 also induced PML/PML-RARA degradation, PML nuclear bodies formation, and activation of the downstream p53 pathway in NB4 cells. Z-VAD-FMK inhibited caspase activation and significantly reversed GRh2-induced apoptosis and PML-RARA degradation. GRh2 also upregulated TNF-α expression and inhibited Akt phosphorylation. LY294002, an inhibitor of the PI3K pathway, enhanced the antitumor effects of GRh2, and C 87, an inhibitor of the TNF-α pathway, reversed NB4 cell viability, and GRh2-mediated apoptosis in a caspase-8-dependent manner. Conclusion: GRh2 induced caspase-dependent PML-RARA degradation and apoptosis in NB4 cells via the Akt/Bax/caspase9 and TNF-α/caspase8 pathways.

Characteristics of Acid Pre-treated Red Ginseng and Its Decoction (산처리 홍삼과 추출물의 특성)

  • Kim, Mi-Hyun;Lee, Young-Chul;Choi, Sang-Yoon;Cho, Chang-Won;Rho, Jeong-Hae
    • Journal of Ginseng Research
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    • v.33 no.4
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    • pp.343-348
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    • 2009
  • This study was conducted to produce a new red ginseng by steaming ginseng using a new pre-treatment method, so as to develop ginseng products with improved flavor and thereby expand ginseng's consumer base. The color parameters (Hunter value), free sugar contents, and ginsenoside contents of the powder from the dried red ginseng, and the sensory test of the semi-dried red ginseng and the decoction from the dried red ginseng, were measured to investigate the effect of acid (ascorbic acid or citric acid) impregnation pre-treatment on red ginseng. The powder from the acid-pretreated red ginseng became lighter and more yellow than the red ginseng that was not pre-treated, but the redness (avalue) of the powder from the acid-pre-treated red ginseng increased. The ginsenoside contents of $Rg_2+Rh_1$ and $Rg_3$ increased with the acid treatment. There was a significant difference in the color and sweetness of the semi-dried acidtreated and non-treated red ginsengs in the sensory test. As the results of the sensory test were expressed in the hedonic scale, however, there were significant differences in the degrees of bitterness, astringency, sourness, odor, and color of the red ginseng decollation. Especially, the acid-treated red ginseng extract tasted less bitter, which shows the potential of new red ginseng products with improved ginseng flavor.

Biotransformation of Ginsenoside Rb1, Crocin, Amygdalin, Geniposide, Puerarin, Ginsenoside Re, Hesperidin, Poncirin, Glycyrrhizin, and Baicalin by Human Fecal Microflora and Its Relation to Cytotoxicity Against Tumor Cells

  • Kim, Young-Suk;Kim, Jung-Jin;Cho, Ki-Ho;Jung, Woo-Sang;Moon, Sang-Kwan;Park, Eun-Kyung;Kim, Dong-Hyun
    • Journal of Microbiology and Biotechnology
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    • v.18 no.6
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    • pp.1109-1114
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    • 2008
  • To understand the role of intestinal microflora in the biological effect of functional herbs, which have been used in Korea, Japan, and China as traditional medicines, and suggest new bioactive compounds transformed from herbal constituents, the metabolic activities of the functional herb components (ginsenoside Rb1, crocin, amygdalin, geniposide, puerarin, ginsenoside Re, poncirin, hesperidin, glycyrrhizin, and baicalin) toward their bioactive compounds (compound K, crocetin, benzaldehyde, genipin, daidzein, ginsenoside Rh1, ponciretin, hesperetin, 18b-glycyrrhetic acid, and baicalein) were measured in fecal specimens. The metabolic activities of these components were $882.7{\pm}814.5$, $3,938.1{\pm}2,700.8$, $2,375.5{\pm}913.7$, $1,179.4{\pm}795.7$, $24.6{\pm}10.5$, $11.4{\pm}10.8$, $578.8{\pm}206.1$, $1,150.0{\pm}266.1$, $47.3{\pm}58.6$, and $12,253.0{\pm}6,527.6\;{\mu}mol/h/g$, respectively. No differences were found in the metabolic activities of the tested components between males and females, although these metabolic activities between individuals are extensively different. The metabolites of functional herb components showed more potent cytotoxicity against tumor cells than nonmetabolites. These findings suggest that intestinal microflora may activate the pharmacological effect of herbal food and medicines and must be the biocatalytic converter for the transformation of herbal components to bioactive compounds.

Effects of Ginsenosides and Their Metabolites on Voltage-dependent Ca2+ Channel Subtypes

  • Lee, Jun-Ho;Jeong, Sang Min;Kim, Jong-Hoon;Lee, Byung-Hwan;Yoon, In-Soo;Lee, Joon-Hee;Choi, Sun-Hye;Lee, Sang-Mok;Park, Yong-Sun;Lee, Jung-Ha;Kim, Sung Soo;Kim, Hyoung-Chun;Lee, Boo-Yong;Nah, Seung-Yeol
    • Molecules and Cells
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    • v.21 no.1
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    • pp.52-62
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    • 2006
  • In previous reports we demonstrated that ginsenosides, active ingredients of Panax ginseng, affect some subsets of voltage-dependent $Ca^{2+}$ channels in neuronal cells expressed in Xenopus laevis oocytes. However, the major component(s) of ginseng that affect cloned $Ca^{2+}$ channel subtypes such as ${\alpha}_{1C}$(L)-, ${\alpha}_{1B}$(N)-, ${\alpha}_{1A}$(P/Q)-, ${\alpha}_{1E}$(R)- and ${\alpha}_{1G}$(T) have not been identified. Here, we used the two-microelectrode voltage clamp technique to characterize the effects of ginsenosides and ginsenoside metabolites on $Ba^{2+}$ currents ($I_{Ba}$) in Xenopus oocytes expressing five different $Ca^{2+}$ channel subtypes. Exposure to ginseng total saponins (GTS) induced voltage-dependent, dose-dependent and reversible inhibition of the five channel subtypes, with particularly strong inhibition of the ${\alpha}_{1G}$-type. Of the various ginsenosides, $Rb_1$, Rc, Re, Rf, $Rg_1$, $Rg_3$, and $Rh_2$, ginsenoside $Rg_3$ also inhibited all five channel subtypes and ginsenoside $Rh_2$ had most effect on the ${\alpha}_{1C}$- and ${\alpha}_{1E}$-type $Ca^{2+}$ channels. Compound K (CK), a protopanaxadiol ginsenoside metabolite, strongly inhibited only the ${\alpha}_{1G}$-type of $Ca^{2+}$ channel, whereas M4, a protopanaxatriol ginsenoside metabolite, had almost no effect on any of the channels. $Rg_3$, $Rh_2$, and CK shifted the steady-state activation curves but not the inactivation curves in the depolarizing direction in the ${\alpha}_{1B}$- and ${\alpha}_{1A}$-types. These results reveal that $Rg_3$, $Rh_2$ and CK are the major inhibitors of $Ca^{2+}$ channels in Panax ginseng, and that they show some $Ca^{2+}$ channel selectivity.

Kinetic Studies on the Thermal Degradation of Ginsenosides in Ginseng Extract (Ginsenosides의 처리온도(處理溫度) 및 시간(時閭)에 따른 반응속도론적(反應速度論的) 연구(硏究))

  • Choi, Jin-Ho;Kim, Doo-Ha;Sung, Hyun-Soon;Kim, Woo-Jung;Oh, Sung-Ki
    • Korean Journal of Food Science and Technology
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    • v.14 no.3
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    • pp.197-202
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    • 1982
  • Kinetic study for the thermal degradation of ginsenosides in ginseng extract was conducted. The results indicate that the thermal degradation followed first order kinetics and rate constants varied substantially depending on the types of ginsenosides and heat treatment temperatures. Activation energy calculated by Arrhenius plots ranged from 16.80 kcal/mole to 30.10 kcal/mole and $Q_{10}$ values ranged from 2.01 to 3.49. Correlation coefficients between the change of ginsenoside contents by thermal degradation and heat treatment temperature were $0.995{\sim}0.999$. The dependence on temperatures of the decomposition rate constant of total ginsenoside can be expressed as $k=4.574{\times}10^8$ exp(8898.8/T).

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