• Archives of Pharmacal Research
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• v.26 no.11
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• pp.906-911
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• 2003

We previously reported that the butanol (BuOH) fraction of the head of Panax ginseng exhibited gastroprotective activity in peptic and chronic ulcer models. In order to identify the active constituent, an activity-guided isolation of the BuOH faction was conducted with a HCI$.$ethanol-induced gastric lesion model. The BuOH fraction was passed through a silica-gel column using a chloroform-methanol gradient solvent system, and six fractions (frs. 1-6) were obtained. The active fr. 5 was further separated by silica-gel column, to yield 6 subfractions (subfrs. a-f). Subfr. d was composed of ginsenosides Re, Rc and $Rb_1$. The most active constituent was ginsenoside $Rb_1$ ($GRb_1$), a protopanaxadiol glycoside, which was investigated for its anti-ulcer effect. Gastric injury induced by HCI$.$ethanol, indomethacin and pyloric ligation (Shay ulcer) was apparently reduced with oral $GRb_1$ doses of 150 and 300 mg/kg. $GRb_1$ at these dosage significantly increased the amount of mucus secretion in an ethanol-induced model. The anti-ulcer effects were consistent with the result of histological examination. These results suggest that the major active constituent in the head of Panax ginseng is $GRb_1$ and that anti-ulcer effect is produced through an increase in mucus secretion.

• Korean Journal of Pharmacognosy
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• v.46 no.4
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• pp.279-282
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• 2015

In order to quantify compound K(CK), anticancer component of Panax ginseng C. A. Meyer, high titer rabbit polyclonal antibodies (pAbs) were raised against a conjugate of CK and bovine serum albumin coupled by a periodate oxidation method. Coating antigen (CK-OVA) was also prepared by the same method with OVA. As a result of optimization of antiserum dilution (2,000 fold), coating antigen ($25{\mu}g/ml$) and other condition (incubation time, temperature and washing method), ELISA method for the determination of CK was established. The measuring range extended from 0.5 ng/ml to 25 ng/ml of CK. The antibodies exhibited minor or even no cross reactivities with protopanaxatriol (1.56%) and other tested ginsenosides, $GRb_1$ (0.11%), $GRg_1$ (0.07%) except protopanaxadiol (87.2%) from the structural similarity. And the antibody showed good correlation (r=0.987) between the assay values obtained by this ELISA method and HPLC. Therefore, the ELISA method could be very useful tools for the determination of CK in biological fluids because of their high sensitivity and specificity.

• YAKHAK HOEJI
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• v.49 no.6
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• pp.490-494
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• 2005

The objective of this study is to provide the basic information for developing a high-value ginseng product using ginseng saponin and prosapogenin. In order to achieve such aim, Ginsenoside compositions of black ginseng (BG) extracts with various solvent conditions were examined by HPLC. The total saponin and the prosapogenin content of 95$\%$ ethyl alcohol extract were higher than that of the either 50$\%$ ethyl alcohol extract or distilled water extract. As a result, the order of the total saponin and the prosapogenin content was 1) 95$\%$ ethyl alcohol,2) 50$\%$ ethyl alcohol,3) the first and second mixture of 95$\%$ ethyl alcohol, distilled water, and 4) distilled water extract. In the case of fine black ginseng (FBG), the first and second mixture extracts of 95$\%$ ethyl alcohol and distilled water were the highest. In addition, the ratio of the protopanaxadiol group and the protopanaxatriol group (PD/PT) showed that the ratio of BG ranged from 0.304 to 0.601, while the ratio of FBG ranged from 1.166 to 1.657.

• Journal of Ginseng Research
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• v.20 no.3
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• pp.269-273
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• 1996

We investigated the effects of ginseng glycosides and their aglycones on processes of single ion channel formation and channel properties. The glycosides, Rg, and Rb, , and their aglycones, 20-(S)-protopanaxatriol (PT) and 20-(S)-protopanaxadiol (PD) increased the membrane permeability for ions. PT, PD, Rg1, and Rb1; at concentrations of 0.5, 3.0, 10.0 and 30.0 $\mu\textrm{g}$/ml respectively; Induced single ion channel fluctuations with the life times in the range of 0.1~1005 in open states and conductances from 5 to 30 pS in 1 M KCI. At high concentrations of these substances, rapid fluctuations of transmembrane ion current with amplitude from hundred pS to dozen nS were observed. Against other substances, ginsenoside Rbl began to increase the membrane conductance at concentration of about 60 $\mu\textrm{g}$/ml without fluctuation of single ion channel. Membranes treated with PT, PD, Rg1 and Rb1 are more permeable to K+, than to Cl while zero current membrane potentials with 10 gradients of KCI were 12, 16, 8, 25 mV respectively. Key words : Membrane conductance, single ion channel, ginsenosides.

• BMB Reports
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• v.32 no.4
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• pp.339-344
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• 1999

We studied the effects of ginsenosides in immature rats based upon the previous results that ginseng has a suppressive or anticonvulsive activity. To examine the suppressive effect of ginsenosides on kainic acid-induced seizures, the severities and frequencies were observed for 4 h after injection of kainic acid (KA; i.p., 2 mg/kg b.w.) using 10-day-old male Sprague-Dawley rats ($22{\pm}2\;g$). Protopanaxadiol saponins such as ginsenoside-Rb1 (Rb1), ginsenoside-Rb2 (Rb2), ginsenoside-Rc (Rc), and ginsenoside-Rd(Rd) generally reduced the seizure activities while protopanaxatriol saponins such as ginsenoside-Rg1 (Rg1) and ginsenoside-Re (Re) rather increased stereotypic "paddling-like" movements. When vinyl-GABA (v-G) was injected together with Rb1 or Rc, KA-induced seizure severities were additionally reduced only by the injection of Rc, but not by Rb1. The level of gamma isozyme of protein kinase C (PKC-${\gamma}$) in the hippocampus increased about three times as much as that of normal rats at 4 h after KA injection. The increased level of PCK-${\gamma}$ by KA was significantly reduced to about 35% by the coinjection with v-G alone, but it was not changed by v-G together with Rb1 or Rc. The increased level of PKC-${\gamma}$ at 4 h after injection of KA was not consistent with the reduction of seizure severities between Rb1 and Rc. These results suggest that Rc and Rb1 may reduce seizure severity independent of PKC-${\gamma}$ levels, and Rc may additionally act with v-G regarding the GABA metabolism during the stage of KA-induced seizures in the immature rats.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.2
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• pp.127-132
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• 2013

Ginsenosides, one of the active ingredients of Panax ginseng, show various pharmacological and physiological effects, and they are converted into compound K (CK) or protopanaxatriol (M4) by intestinal microorganisms. CK is a metabolite derived from protopanaxadiol (PD) ginsenosides, whereas M4 is a metabolite derived from protopanaxatriol (PT) ginsenosides. The ${\gamma}$-aminobutyric acid $receptor_C$ ($GABA_C$) is primarily expressed in retinal bipolar cells and several regions of the brain. However, little is known of the effects of ginsenoside metabolites on $GABA_C$ receptor channel activity. In the present study, we examined the effects of CK and M4 on the activity of human recombinant $GABA_C$ receptor (${\rho}$ 1) channels expressed in Xenopus oocytes by using a 2-electrode voltage clamp technique. In oocytes expressing $GABA_C$ receptor cRNA, we found that CK or M4 alone had no effect in oocytes. However, co-application of either CK or M4 with GABA inhibited the GABA-induced inward peak current ($I_{GABA}$). Interestingly, pre-application of M4 inhibited $I_{GABA}$ more potently than CK in a dose- dependent and reversible manner. The half-inhibitory concentration ($IC_{50}$) values of CK and M4 were $52.1{\pm}2.3$ and $45.7{\pm}3.9{\mu}M$, respectively. Inhibition of $I_{GABA}$ by CK and M4 was voltage-independent and non-competitive. This study implies that ginsenoside metabolites may regulate $GABA_C$ receptor channel activity in the brain, including in the eyes.

• Korean Journal of Organic Agriculture
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• v.23 no.3
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• pp.509-522
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• 2015

Organic ginseng farming has rapidly increased in response to consumer demand for a safe product which improves health. Differences in soil nutrient concentration and ginsenoside content between organic and conventional ginseng farming have, however, not yet been properly studied. Therefore the aim of the present study was to compare soil nutrient concentration and ginsenoside content between these two farming systems. $NO_3-N$, $P_2O_5$, and K were significantly different between organic and conventional ginseng farming. The total content of ginsenoside and individual ginsenoside components were higher in organically grown ginseng than in ginseng from conventional farming, although there is no significant difference. Particularly, protopanaxadiol saponins were higher than protopanaxatriol saponins in ginseng from organic farming compared to ginseng produced by conventional farming. $NO_3-N$ content in soils showed a negative correlation with the content of ginsenosides $Rb_2$ and Rd. In addition, $P_2O_5$ showed a negative correlation with ginsenosides $Rb_1$, Rc, and PD/PT ratio. Organic matter showed a positive crrelation with ginsenosides Re. To increase the ginsenoside content of ginseng, we recommend increasing organic matter and decreasing $NO_3-N$ and $P_2O_5$ contents in the soil.

• 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.

• Journal of the Korean Applied Science and Technology
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• v.38 no.6
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• pp.1466-1475
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• 2021

Compound K (20-O-β-(_D-glucopyranosyl)-20(S)-protopanaxadiol) is an active ingredient of ginsenosides. Compound K has been known to produce from biotransformation by β-glucosidase action of human intestinal microbes after oral admistration of ginseng. We have investigated the cytotoxicity of compound K obtained from bio-converted ginseng extract. As a result, compound K showed no significant cytotoxicity in the concentration of 0.001 to 1 ㎍/mL and inhibited the production of TNF-α, MCP-1, IL-6 and NO in RAW 264.7 cells induced by LPS inflamation. In the same concentration, HaCaT cells induced by inflammation with TNF-α and IFN-γ decreased IL-8 production due to compound K treatment. In the brine shrimp lethality assay, the LC₅₀ of compound K was 0.37 mg/mL indicating some toxicity, but the bioconverted product containing 35% compound K showed relatively low toxicity with an LC₅₀ of 0.87 mg/mL. These results suggest that the compound K enriched extract is a potential functional material for acne relief cosmetic products.

• Molecular & Cellular Toxicology
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• v.3 no.4
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• pp.254-261
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• 2007

20-O-($\beta$-D-Glucopyranosyl)-20 (S)-protopanaxadiol (IH-901) is one of the major metabolites of ginsenosides from Panax ginseng, and is suggested that IH-901 has been associated with various pharmacological and physiological activities. In this study, we demonstrate that IH-901 induced anti-inflammation in HT-29 human colon adenocarcinoma cells. Our results showed that IH-901 inhibited cell proliferation of HT-29 in a time- and dose-dependent manner. We also found that IH-901 was significantly decreased expression of iNOS compared with non-treated. We observed effect of IH-901 related with inflammatory genes using by cDNA microarray. We were known that the 34 inflammatory genes such as E2F, CDK6, TNF-$\alpha$, and PKC were down-regulated. Thus, these results suggest that IH-901 may have a potential preventive factor to improving cancer induced by chronic inflammation.