• Archives of Pharmacal Research
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• 제26권11호
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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.

• 생약학회지
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• 제46권4호
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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.

• 약학회지
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• 제49권6호
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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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• 제20권3호
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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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• 제32권4호
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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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• 제17권2호
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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.

• 한국유기농업학회지
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• 제23권3호
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• pp.509-522
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• 2015

유기농 인삼 재배는 소비자들의 안정적인 농산물의 요구에 따라 급증한다. 반면에 유기농과 관행 인삼재배의 토양 무기성분 및 인삼의 진세노사이드함량 차이에 관한 연구는 아직 까지 미흡한 실정이다. 따라서 본 연구는 토양화학성 및 진세노사이드 함량을 비교해 관행인삼과 유기농인삼의 차이를 구명하는데 목적을 두고 있다. 질산태 질소, 가용성인산, 치환성 칼륨함량은 유기농재배와 관행재배 간에 유의성 있는 차이를 보였다. 비록 유의성 있게 차이는 없었지만 총 진세노사이드함량 뿐만 아니라 대부분 개별 진세노사이드는 관행재배 인삼보다 유기농재배 인삼에서 더 높은 함량을 보였다. 특히 유기농 인삼은 관행인삼에 비해 PT계열의 사포닌 보다 PD계열의 사포닌 함량이 더 높았다. 질산태 질소는 Ginsenoside $Rb_2$, Rd와 부의 상관관계를 보였다. 반면에 유효인산함량은 $Rb_1$, Rc, PD/PT비율과 부의 상관관계를 보였다. 인삼의 Ginsenosdie 성분들을 증가시키려면 질산태 질소과 인삼함량을 줄이고 유기물함량을 높여야 한다.

• Molecules and Cells
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• 제21권1호
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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.

• 한국응용과학기술학회지
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• 제38권6호
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• pp.1466-1475
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• 2021

Compound K (20-O-β-(_D-glucopyranosyl)-20(S)-protopanaxadiol)는 진세노사이드의 활성성분이다. Compound K는 경구 투여 후 Rb₁, Rb₂ 및 Rc가 사람의 장내 미생물의 β-glucosidase에 의해 생물전환 과정을 거쳐 생성된다고 알려져 있다. 본 연구는 생물전환된 인삼농축액에서 얻은 compound K를 이용해 항염증 및 독성을 조사하였다. 세포독성평가 결과, compound K는 0.001~1 ㎍/mL의 농도범위에서 유의적인 세포독성은 나타나지 않았으며, LPS로 염증이 유발된 RAW 264.7 세포에서 TNF-α, MCP-1, IL-6 및 NO의 생성을 억제하는 것으로 확인되었다. 동일 농도범위에서 TNF-α 및 IFN-γ로 염증이 유발된 HaCaT 세포는 compound K의 처리로 인해 IL-8의 생성을 감소시키는 것으로 나타났지만, IL-6의 경우 일부 농도에서 생성을 감소시켰으나, 통계적인 유의성은 나타나지 않았다. Brine shrimp를 이용한 치사율 검정법에서 compound K의 LC₅₀는 0.37mg/mL로 다소의 독성을 함유하고 있는 것으로 나타났으나 compound K가 35% 고함유된 생물전환물은 LC₅₀가 0.87mg/mL로 나타나 상대적으로 낮은 독성을 보였다. 따라서 이 생성물은 향후 여드름 완화용 화장품 개발에 사용할 수 있는 매우 우수한 기능성 소재가 될 수 있을 것으로 기대된다.

• Molecular & Cellular Toxicology
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• 제3권4호
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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.