• Title/Summary/Keyword: $ginsenoside-{Rg_1}$

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Ginsenosides Inhibit Endothelium - dependent Contraction in the Spontaneously Hypertensive Rat Aorta isn vitro (선천성 고혈압 랫드에서 ginsenosides에 의한 내피의존성수축의 억제작용)

  • 김낙두;최원선
    • Journal of Ginseng Research
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    • v.21 no.2
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    • pp.125-132
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    • 1997
  • Our previous study showed that in vivo treatment of spontaneously hypertensive rats (SHR) with protopanaxatriol ginsenosides (PPT) reduces the blood pressure and inhibits the con- tractions induced by endothelium-derived contracting factor (prostaglandin endoperoxide ($PGH_2$) and superoxide anion) in aorta isolated from SHR. The aim of the present study is to examine whether PPT improves endothelial functions in the isolated thoracic aorta of SHR in vitro. Treatments of aortic rings with PPT, purified ginsenoside $Rg_1$ ($Rg_1$) or indomethacin normalized endotheliuln-dependent relaxation to acetylcholine, but not with protopanaxadiol ginsenosides (PPD) and purified ginsenoside Rb1 (Rb1). The effects of PPT were dose-dependent. PGH,- and oxygen free radical-inducted contractions in rat aorta without endothelium were inhibited by PPT or $Rg_1$, but not by PPD or $Rb_1$. Contractions induced by PGF2$\alpha$, U-46619, a stable thromboxane A2 agonist or KCI (60 mM) were not inhibited by PPT, $Rg_1$ or $Rb_1$. These findings demonstrate that PPT but not PPD scavenges the oxygen-derived free radicals and/or antagonize the effects of $PGH_2$ in the vascular smooth muscle and may explain the hypotensive effect of ginseng in the SHR.

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Ginsenoside Rg1 activates ligand-independent estrogenic effects via rapid estrogen receptor signaling pathway

  • Gao, Quan-Gui;Zhou, Li-Ping;Lee, Vien Hoi-Yi;Chan, Hoi-Yi;Man, Cornelia Wing-Yin;Wong, Man-Sau
    • Journal of Ginseng Research
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    • v.43 no.4
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    • pp.527-538
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    • 2019
  • Background: Ginsenoside Rg1 was shown to exert ligand-independent activation of estrogen receptor (ER) via mitogen-activated protein kinase-mediated pathway. Our study aimed to delineate the mechanisms by which Rg1 activates the rapid ER signaling pathways. Methods: ER-positive human breast cancer MCF-7 cells and ER-negative human embryonic kidney HEK293 cells were treated with Rg1 ($10^{-12}M$, $10^{-8}M$), $17{\beta}$-estradiol ($10^{-8}M$), or vehicle. Immunoprecipitation was conducted to investigate the interactions between signaling protein and ER in MCF-7 cells. To determine the roles of these signaling proteins in the actions of Rg1, small interfering RNA or their inhibitors were applied. Results: Rg1 rapidly induced $ER{\alpha}$ translocation to plasma membrane via caveolin-1 and the formation of signaling complex involving linker protein (Shc), insulin-like growth factor-I receptor, modulator of nongenomic activity of ER (MNAR), $ER{\alpha}$, and cellular nonreceptor tyrosine kinase (c-Src) in MCF-7 cells. The induction of extracellular signal-regulated protein kinase and mitogen-activated protein kinase kinase (MEK) phosphorylation in MCF-7 cells by Rg1 was suppressed by cotreatment with small interfering RNA against these signaling proteins. The stimulatory effects of Rg1 on MEK phosphorylation in these cells were suppressed by both PP2 (Src kinase inhibitor) and AG1478 [epidermal growth factor receptor (EGFR) inhibitor]. In addition, Rg1-induced estrogenic activities, EGFR and MEK phosphorylation in MCF-7 cells were abolished by cotreatment with G15 (G protein-coupled estrogen receptor-1 antagonist). The increase in intracellular cyclic AMP accumulation, but not Ca mobilization, in MCF-7 cells by Rg1 could be abolished by G15. Conclusion: Ginsenoside Rg1 exerted estrogenic actions by rapidly inducing the formation of ER containing signalosome in MCF-7 cells. Additionally, Rg1 could activate EGFR and c-Src ER-independently and exert estrogenic effects via rapid activation of membrane-associated ER and G protein-coupled estrogen receptor.

Easy Red Ginseng Production Using Household Microwave Ovens (가정용 전자레인지를 이용한 간편 홍삼 제조)

  • Kim, Mi Hyun;Kim, Kyung Tack;Cho, Chang-Won;Rho, Jeonghae
    • Korean journal of food and cookery science
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    • v.28 no.5
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    • pp.623-628
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    • 2012
  • The study was about to produce red ginsengs easily, using a household microwave oven to promote the consumption of fresh ginsengs in the home. Producing red ginsengs with a household microwave oven 'defrost function' takes 13 minutes (A), 'cook function' 6 minutes (B), and finally, 'defrost function' 44 minutes (C). For characteristics of microwave-produced red ginsengs, total saponin loss, color of powder, polyphenol content and saponin composition were compared with common red ginsengs. The color test for red ginseng powder showed that the color of household microwave-produced 6-minute cooked red ginseng (B) or 44-minute defrosted red ginseng (C) was closer to that of the common red ginsengs (E). The total saponin content in water eluted during red ginseng production showed that the saponin loss in microwave red ginseng was negligible compared to the common red ginsengs. Microwave red ginsengs showed no difference in phenol content that of the and higher total ginsenoside content than common red ginsengs. The ginsenoside $Rg_1$, Re, Rf, $Rg_2+Rh_1$, $Rb_1$, Rc, $Rb_2$, $Rb_3$, Rd and $Rg_3$ contents of microwave red ginsengs (A, B) were higher compared to that of the common red ginsengs; the ginsenoside Re, Rc, $Rb_2$, $Rb_3$, Rd and $Rg_3$ contents of 44-minute defrosted red ginseng (C) were higher compared to the common red ginsengs. It is considered that red ginseng production, using microwave oven at home, can be a fast and convenient way to produce highly functional red ginsengs with high ginsenoside content.

Ginsenoside Rg1 modulates medial prefrontal cortical firing and suppresses the hippocampo-medial prefrontal cortical long-term potentiation

  • Ghaeminia, Mehdy;Rajkumar, Ramamoorthy;Koh, Hwee-Ling;Dawe, Gavin S.;Tan, Chay Hoon
    • Journal of Ginseng Research
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    • v.42 no.3
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    • pp.298-303
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    • 2018
  • Background: Panax ginseng is one of the most commonly used medicinal herbs worldwide for a variety of therapeutic properties including neurocognitive effects. Ginsenoside Rg1 is one of the most abundant active chemical constituents of this herb with known neuroprotective, anxiolytic, and cognition improving effects. Methods: We investigated the effects of Rg1 on the medial prefrontal cortex (mPFC), a key brain region involved in cognition, information processing, working memory, and decision making. In this study, the effects of systemic administration of Rg1 (1 mg/kg, 3 mg/kg, or 10 mg/kg) on (1) spontaneous firing of the medial prefrontal cortical neurons and (2) long-term potentiation (LTP) in the hippocampal-medial prefrontal cortical (HP-mPFC) pathway were investigated in male Sprague-Dawley rats. Results: The spontaneous neuronal activity of approximately 50% the recorded pyramidal cells in the mPFC was suppressed by Rg1. In addition, Rg1 attenuated LTP in the HP-mPFC pathway. These effects were not dose-dependent. Conclusion: This report suggests that acute treatment of Rg1 impairs LTP in the HP-mPFC pathway, perhaps by suppressing the firing of a subset of mPFC neurons that may contribute to the neurocognitive effects of Rg1.

Ginsenoside Rg1 from Panax ginseng enhances myoblast differentiation and myotube growth

  • Go, Ga-Yeon;Lee, Sang-Jin;Jo, Ayoung;Lee, Jaecheol;Seo, Dong-Wan;Kang, Jong-Sun;Kim, Si-Kwan;Kim, Su-Nam;Kim, Yong Kee;Bae, Gyu-Un
    • Journal of Ginseng Research
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    • v.41 no.4
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    • pp.608-614
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    • 2017
  • Background: Ginsenoside Rg1 belongs to protopanaxatriol-type ginsenosides and has diverse pharmacological activities. In this report, we investigated whether Rg1 could upregulate muscular stem cell differentiation and muscle growth. Methods: C2C12 myoblasts, MyoD-transfected 10T1/2 embryonic fibroblasts, and HEK293T cells were treated with Rg1 and differentiated for 2 d, subjected to immunoblotting, immunocytochemistry, or immunoprecipitation. Results: Rg1 activated promyogenic kinases, p38MAPK (mitogen-activated protein kinase) and Akt signaling, that in turn promote the heterodimerization with MyoD and E proteins, resulting in enhancing myogenic differentiation. Through the activation of Akt/mammalian target of rapamycin pathway, Rg1 induced myotube growth and prevented dexamethasone-induced myotube atrophy. Furthermore, Rg1 increased MyoD-dependent myogenic conversion of fibroblast. Conclusion: Rg1 upregulates promyogenic kinases, especially Akt, resulting in improvement of myoblast differentiation and myotube growth.

Changes in Effective Components of Ginseng by Puffing (팽화에 의한 인삼 유효성분의 변화)

  • Kim, Ji-Hye;Ahn, Soon-Cheol;Choi, Sung-Won;Hur, Nam-Youn;Kim, Byung-Yong;Baik, Moo-Yeol
    • Applied Biological Chemistry
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    • v.51 no.3
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    • pp.188-193
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    • 2008
  • This study was conducted to investigate the effect of moisture content and pressure on extraction yield, crude saponins and ginsenoside contents of puffed Korean ginseng. Puffed ginsengs showed relatively higher extraction yield ($50.0{\sim}62.1%$) and amounts of crude saponins ($19.6{\sim}48.8$ mg/g ginseng) than no-puffed ginseng ($37.6{\pm}0.8%$ and $11.0{\pm}1.0$ mg/g ginseng), respectively. The highest extraction yield and amounts of crude saponins were obtained in 8.0% moisture content sample puffed at 10 $kg_f/cm^2$. In HPLC analysis, amounts of measured major ginsenosides (Rb1, Rb2, Rc, Rd, Re, and Rg1) decreased with increasing puffing pressure, yet contents of almost all major gin senosides were higher than control (no-puffed). On the other hand, ginsenoside Rg3 were produced after puffing suggesting that chemical structure of some ginsenosides might be altered during the puffing process. These results indicate that puffing can increase the extraction yield and crude saponin contents and it could influence the ginsenoside composition.

Antimelanogenic effect of ginsenoside Rg3 through extracellular signal-regulated kinase-mediated inhibition of microphthalmia-associated transcription factor

  • Lee, Seung Jae;Lee, Woo Jin;Chang, Sung Eun;Lee, Ga-Young
    • Journal of Ginseng Research
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    • v.39 no.3
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    • pp.238-242
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    • 2015
  • Background: Panax ginseng has been used to prolong longevity and is believed to be useful for improving skin complexion. Ginsenosides are the most active components isolated from ginseng, and ginsenoside Rg3 (G-Rg3) in particular has been demonstrated to possess antioxidative, antitumorigenic, and anti-inflammatory properties. The aim of this study was to examine the ability of G-Rg3 to inhibit melanogenesis. Methods: The effects of G-Rg3 on melanin contents and the protein levels of tyrosinase, microphthalmia-associated transcription factor (MITF), and tyrosinase-related protein 1 (TRP1) were evaluated. Melanogenesis-regulating signaling molecules such as Akt and extracellular signal-regulated kinase (ERK) were also examined to explore G-Rg3-induced antimelanogenic mechanisms. Results: G-Rg3 was found to significantly inhibit the synthesis of melanin in normal human epidermal melanocytes and B16F10 cells in a dose-dependent manner. The activity of cellular tyrosinase and the expression of MITF, tyrosinase, and TRP1 were all reduced, whereas ERK was strongly activated. PD98059 (a specific inhibitor of ERK) attenuated the G-Rg3-induced inhibition of melanin synthesis and tyrosinase activity. Conclusion: Taken together, these results showed that G-Rg3 induces the activation of ERK, which accounts for its antimelanogenic effects. G-Rg3 may be a promising safe skin-whitening agent, adding to the long list of uses of P. ginseng for the enhancement of skin beauty.

Evaluation of 20(S)-ginsenoside Rg3 loaded hydrogel for the treatment of perianal ulcer in a rat model

  • Jin, Longhai;Liu, Jinping;Wang, Shu;Zhao, Linxian;Li, Jiannan
    • Journal of Ginseng Research
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    • v.46 no.6
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    • pp.771-779
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    • 2022
  • Background: As a kind of common complication of the surgery of perianal diseases, perianal ulcer is known as a nuisance. This study aims to develop a kind of 20(S)-ginsenoside Rg3 (Rg3)-loaded hydrogel to treat perianal ulcers in a rat model. Methods: The copolymers PLGA1600-PEG1000-PLGA1600 were synthesized by ring-opening polymerization process and Rg3-loaded hydrogel was then developed. The perianal ulcer rat model was established to analyze the treatment efficacy of Rg3-loaded hydrogel for ulceration healing for 15 days. The animals were divided into control group, hydrogel group, free Rg3 group, Rg3-loaded hydrogel group, and Lidocaine Gel® group. The residual wound area rate was calculated and the blood concentrations of interleukin-1 (IL-1), interleukin-6 (IL-6), and vascular endothelial growth factor (VEGF) were recorded. Hematoxylin and eosin (H&E) staining, Masson's Trichrome (MT) staining, and tumor necrosis factor α (TNF-α), Ki-67, CD31, ERK1/2, and NF-κB immunohistochemical staining were performed. Results: The biodegradable and biocompatible hydrogel carries a homogenous interactive porous structure with 10 ㎛ pore size and five weeks in vivo degradation time. The loaded Rg3 can be released sustainably. The in vitro cytotoxicity study showed that the hydrogel had no effect on survival rate of murine skin fibroblasts L929. The Rg3-loaded hydrogel can facilitate perianal ulcer healing by inhibiting local and systematic inflammatory responses, swelling the proliferation of nuclear cells, collagen deposition, and vascularization, and activating ERK signal pathway. Conclusion: The Rg3-loaded hydrogel shows the best treatment efficacy of perianal ulcer and may be a candidate for perianal ulcer treatment.

Protective Effects of Ginsenoside Rg3 against Cholesterol Oxide-Induced Neurotoxicity in the Rat

  • Kim, Jong-Hoon
    • Journal of Ginseng Research
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    • v.33 no.4
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    • pp.294-304
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    • 2009
  • Ginsenosides are among the most well-known traditional herbal medicines frequently used for the treatment of various symptoms in South Korea. The neuroprotective effects of ginsenoside $Rg_3$ (G-$Rg_3$) on cholesterol-oxide-(CO)-induced neurotoxicity were investigated through the analyses of rat brains. The recently accumulated reports show that ginseng saponins (GTS), the major active ingredients of Panax ginseng, have protective effects against neurotoxin insults. In the present study, the neuroprotective effects of G-$Rg_3$ on CO-induced hippocampal excitotoxicity were examined in vivo. The in-vitro studies using rat cultured hippocampal neurons revealed that G-$Rg_3$ treatment significantly inhibited CO-induced hippocampal cell death. G-$Rg_3$ treatment not only significantly reduced CO-induced DNA damage but also attenuated CO-induced apoptosis. The in-vivo studies that were conducted revealed that the intracerebroventricular (i.c.v.) pre-administration of G-$Rg_3$ significantly reduced i.c.v. CO-induced hippocampal damage in rats. To examine the mechanisms underlying the in-vitro and in-vivo neuroprotective effects of G-$Rg_3$ against CO-induced hippocampal excitotoxicity, the effect of G-$Rg_3$ on the CO-induced elevations of the apoptotic cells in cultured hippocampal cells was examined, and it was found that G-$Rg_3$ treatment inhibited CO-induced apoptosis. The histopathological evaluation demonstrated that G-$Rg_3$ significantly diminished the apoptosis in the hippocampus and also spared the hippocampal CA1, CA3, and dentate gyrus neurons. G-$Rg_3$ also significantly improved the CO-caused behavioral impairment. G-$Rg_3$ itself had no effect, however, on the CO-induced inhibition of succinate dehydrogenase activity (data not shown). These results collectively indicate the G-$Rg_3$-induced neuroprotection against CO in rat hippocampus. With regard to the wide use of G-$Rg_3$, this agent is potentially beneficial in treating CO-induced brain injury.

Cancer Chemopreventive Effects of Ginsenoside $Rg_3,\;Rg_5,\;Rh_2$ and BST from Enzymatically Fermented Korean Ginseng Extract

  • Yun Taik-Koo
    • Proceedings of the Ginseng society Conference
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    • 2002.10a
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    • pp.35-46
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    • 2002
  • Panax ginseng C. A. Meyer has been one of the most highly recognized medicinal herbs in the Orient. Previous experiments have demonstrated that $Rg_3,\;and\;Rg_5$ statistically significantly decreased the incidence of benzo(a)pyrene-induced mouse lung tumor, $Rh_2$ showed tendency of decrease and $Rh_1$ showed no effect. It was, therefore, concluded that $Rg_3,\;Rg_5\;and\;Rh_2$ are active cancer chemopreventive components in red ginseng and they either singularly or synergistically act in the prevention of cancer. This study was undertaken to compare the cancer chemopreventive effects of $Rg_3,\;Rg_5\;and\;Rh_2$(purity: more than $60\%$) isolated from fermented ginseng extract and BST fermented ginseng with fortified ginsenoside $Rg_3\;and\;Rh_2$. The cancer chemopreventive effects were investigated in experimental groups treated with benzo(a)pyrene(BP) with ginsenoside $Rg_3,\;Rg_5\;Rh_2\;or\;BST$ at three doses of $50^{\circ}C/ml,\;100^{\circ}C/ml\;and\;200^{\circ}C/ml$ When mice given with $50^{\circ}C/ml$ concentration of ginsenoside $Rg_3$ combined with BP for 6 weeks after BP administration, $Rg_3\;showed\;60\%$ of lung tumor incidence, where as $100^{\circ}C/ml\;and\;200^{\circ}C/ml\;of\;Rg_3$ combined with BP groups had significant decrease of incidence $(40.0\%)$ respectively, with the inhibition rate being $35.5\%.$ While the tumor incidence was not decreased in the group treated with BP and 50 of $Rg_5,$ the incidence was $34.0\%\;and\;32.0\%$ in the group treated with BP and 100 and 200 of $Rg_5$, respectively. These incidences were significantly less than the group treated with BP alone, with the inhibition rate being $45.2\%\;and\;48.4\%,$ respectively. On the other hand, in the group treated with BP and 50 of ginsenoside $Rh_2,$ the tumor incidence was not decreased. However, the incidence was $40.0\%\;and\;38.8\%$ in the experimental treated with BP and 100 and 200 of $Rh_2,$ respectively, with the inhibition rate being $45.2\%\;and\;48.4\%,$ respectively. In addition, the incidence showed the tendency to decrease in the experimental group treated with BP and 50 of BST which contained $16.2\%\;of\;Rh_2,\;15.4\%\;of\;Rg_3\;and\;2.5%\;of\;Rg_5.$ The tumor incidence was $54.0\%$ in this group. In the group treated with 100 and 200 of EST, the incidence was $34.0\%\;and\;30.0\%,$ respectively, the incidences significantly being lower than the group treated with BP alone, with the inhibiting rate being $45.2\%\;and\;51.6\%,$ respectively. The results of this study strongly suggested that ginsenoside $Rg_3,\;Rg_5\;and\;Rh_2$ are the active components of red ginseng having a cancer chemopreventive activity and $Rg_5$ is the strongest cancer chempopreventive among them. On the other hand, the results demonstrating that the incidence of lung tumor was more markedly reduced by BST fermented ginseng with fortified ginsenoside $Rh_2\;or\;Rg_3$ compared to the single component alone, suggest that the combination of these components may remarkablely improve the cancer preventive effect

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