• 한국미생물·생명공학회지
• /
• 제10권4호
• /
• pp.267-273
• /
• 1982

미생물성 효소를 이용하여 인삼saponin중 조성비율이 가장 큰 ginsenoside-Rb$_1$을 약효면에서 보다 우수한 ginsenoside-Rd로 전환하고자 인삼부패균 중 Rhizopus 속의 한 균주를 선정하여 이 균주에서 얻은 효소를 ammonium sulfate 분별 침전법으로 조정제하여 사용하였다. 기질로 사용하기 위해 홍미삼 extract로부터 ginsenoside-Rb$_1$이 36.4%, ginsenoside-Rd 가 12.2%의 조성비율을 갖인 total saponin을 정제하였고 이어 ginsenoside-Rb$_1$의 함량을 증가시키기 위해 더욱 정제한 결과 ginsenoside-Rb$_1$이 54. 5%, ginsenoside-Rd가 1.1%인 ginsenoside Rb group saponin을 얻었다. 이들 기질 saponin에 본 효소를 작용시켜 본 결과 두 기질 모두 다른 ginsenoside pattern에는 변화없이 ginsenoside-Rb$_1$만이 선택적으로 감소하고 반면에 ginsenoside-Rd의 함량이 비례적으로 증가됨을 TLC 및 HPLC의 방법으로 조사하였으며 이로써 효소에 의한 인삼saponin의 선택적전환 가능성을 확인하였다.

• 한국균학회지
• /
• 제14권3호
• /
• pp.195-200
• /
• 1986

Rhizopus japonicus의 한 균주가 생산하는 효소에 의해 인삼 사포닌의 ginsenoside 중 조성비율이 가장 큰 ginsenoside $Rb_1$을 약리 효능면에서 보다 우수한 ginseuoside $Rb_1$로 선택적으로 전환할 수 있음을 TLC 및 HPLC로 정량적으로 확인하였다. Total saponin을 기질로 사용하였을 경우 ginsenoside $Rb_1$은 그 함량의 82.5%까지 ginsenoside Rd로 전환되어 ginsenoside Rd의 함량을 원래 함량에 비해 4.75배까지 증가시킬 수 있었으며, ginsenoside-Rb group saponin 기질의 경우는 80.8%의 ginsenoside $Rb_1$이 ginsenoside Rd로 전환되어 ginsenoside Rd의 함량을 34.7배까지 처리효소의 농도에 비례해서 증가시킬 수 있었다. 한편 다른 ginsenoside 함량변화 없이 오직 ginsenoside $Rb_1$에서 ginsenoside Rd만으로 선택적 전환을 한다는 사실이 당이나 sapogenin의 검출로도 증명되었다.

• 한국균학회지
• /
• 제17권1호
• /
• pp.31-34
• /
• 1989

인삼 saponin중 조성비율이 가장 큰 ginsenoside Rb1만을 약효면에서 보다 우수한 ginsenoside Rd로 선택적 전환시킬 수 있는 Rhizopus japonicus를 대상으로 해서 인삼 saponin 전환효소의 최적생산조건을 검토하였다. Wheat bran 배지를 기본으로 할 경우 배양 5일에 가장 많은 효소가 생산되었으며, 인삼류의 천연유기물중에는 홍삼분말을, 저급당류중에는 xylose를, 다당류중에는 laminarin을 flavonoids중에는 naringin을, 질소원중에는 beef extract와 $KNO_3$를 첨가할 경우 인삼 saponin 전환효소가 가장 많이 생산되었다.

• Journal of Ginseng Research
• /
• 제24권3호
• /
• pp.134-137
• /
• 2000

Spontaneous bursting activity was studied in rat thalamocortical slices using extracellular field potential recording to test the potential utilization of ginsenoside Rb$_1$ in controlling overactivated neural systems. In order to induce bursting activity, slices were perfused with Mg$\^$2+/-free artificial cerebrospinal fluid (ACSF). Two major types of spontaneous bursting activity, simple thalamocortical burst complexes (sTBCs) and complex thalamocortical burst complexes (cTBCs), were recorded in Mg$\^$2+/ -free ACSF. Ginsenoside Rb$_1$ selectively suppressed cTBCs. Duration and occurrence rate of cTBCs were reduced by 87.3${\pm}$10.2% and 85.3${\pm}$ 14.7% in the presence of 90 ${\mu}$M ginsenoside Rb$_1$ respectively, while amplitude and intraburst frequency were slightly changed by ginsenoside Rb$_1$. In contrast, ginsenoside Rb$_1$was much less effective in reducing duration and occurrence rate of sTBCs. We also tested effects of ginsenoside Rb$_1$ on bursting activity in the presence of a GABA$\sub$A/ receptor antagonist, bicuculline methiodide (BMI). Ginsenoside Rb$_1$ had no effect in suppressing BMI-induced bursting activities. These results suggest that ginsenoside Rbi may be useful in controlling seizure-like bursting activity under pathological conditions.

• Journal of Ginseng Research
• /
• 제14권2호
• /
• pp.112-116
• /
• 1990

As a part of studies on the quality control of crude drug preparation drinks, ginseng saponins were identified by HPLC. Ginsenoside-Rb1 was determined quantitatively by HPLC. Ginsenoside MeOH/H2O(65:35:10, v/v) on Si-gel plate. Ginsenoside-Rb1 content determined by HPLC on Lichrosorbtract drinks was 57.5-70.4% compared to the content in the red ginseng extract.

• 약학회지
• /
• 제24권1호
• /
• pp.15-25
• /
• 1980

The investigation is concerned with the action of ginseng saponin on the contractile force in the rat heart and with the elucidation of the mechanism of the action. The effect of total ginseng saponin, ginsenoside Rb$_{1}$ of protopanaxadiol derivatives and ginsenoside Re of protopanaxatriol derivatives on the contractile force in isolated spontaneously beating normal rat heart was investigated. Total ginseng saponin was obtained from white ginseng by the method of Shibata and Namba. Ginsenoside Rb$_{1}$ and ginsenoside Re were isolated by the method of and Han, respectively. Total ginseng saponin exhibited a slight increase of the contractile force. Ginsenoside Rb$_{1}$ increased markedly the contractile force and dose dependent increase in contractile force was observed. However, ginsenoside Re did not increase the contractile force, but it prevented spontaneous decrease of the contractility of the heart. The mixture of the same dose of ginsenoside Rb$_{1}$ and Re showed a slight increase in the contractile force and its effect was similar to that obtained by total ginseng saponin. Pretreatment with propranolol abolished the positive inotropic effect of ginsenoside Rb$_{1}$ and the positive inotropic effect of ginsenoside Rb$_{1}$ was not observed in a reserpinized rat heart. Pretreatment with ginsenoside Re decreased or abolished the positive inotropic effect of epinephrine. Activities of Na+, K+ -ATPase were inhibited by ginsenoside Rb$_{1}$, total ginseng saponin and ginsenoside Re and these inhibitory effects were dose dependent. The results suggest that catecholamine release or inhibition of Na+, K+ -ATPase activities may be involved in the positive inotropic effect of gindenoside Rb$_{1}$. Ginsenoside Re counteracted the positive inotropic effect of ginsenoside Rb$_{1}$.

• Journal of Ginseng Research
• /
• 제40권2호
• /
• pp.105-112
• /
• 2016

Background: Minor saponins or human intestinal bacterial metabolites, such as ginsenosides Rg3, F2, Rh2, and compound K, are more pharmacologically active than major saponins, such as ginsenosides Rb1, Rb2, and Rc. In this work, enzymatic hydrolysis of ginsenoside Rb1 was studied using enzyme preparations from cultured mycelia of mushrooms. Methods: Mycelia of Armillaria mellea, Ganoderma lucidum, Phellinus linteus, Elfvingia applanata, and Pleurotus ostreatus were cultivated in liquid media at $25^{\circ}C$ for 2 wk. Enzyme preparations from cultured mycelia of five mushrooms were obtained by mycelia separation from cultured broth, enzyme extraction, ammonium sulfate (30-80%) precipitation, dialysis, and freeze drying, respectively. The enzyme preparations were used for enzymatic hydrolysis of ginsenoside Rb1. Results: Among the mushrooms used in this study, the enzyme preparation from cultured mycelia of A. mellea (AMMEP) was found to convert ginsenoside Rb1 into compound K with a high yield, while those from G. lucidum, P. linteus, E. applanata, and P. ostreatus produced remarkable amounts of ginsenoside Rd from ginsenoside Rb1. The enzymatic hydrolysis pathway of ginsenoside Rb1 by AMMEP was $Rb1{\rightarrow}Rd{\rightarrow}F2{\rightarrow}$ compound K. The optimum reaction conditions for compound K formation from ginsenoside Rb1 were as follows: reaction time 72-96 h, pH 4.0-4.5, and temperature $45-55^{\circ}C$. Conclusion: AMMEP can be used to produce the human intestinal bacterial metabolite, compound K, from ginsenoside Rb1 with a high yield and without food safety issues.

• Journal of Ginseng Research
• /
• 제39권4호
• /
• pp.304-313
• /
• 2015

Background: Ginsenoside Rg3 is a promising anticancer agent. It is usually produced by heat treatment of ginseng, in which ginsenoside Rb1 is the major ginsenoside. A kinetic study was conducted to optimize ginsenoside Rg3 production by the heat treatment of ginsenoside Rb1. Methods: Ginsenoside Rb1 was heated using an isothermal machine at $80^{\circ}C$ and $100^{\circ}C$ and analyzed using HPLC. The kinetic parameters were calculated from the experimental results. The activation energy was estimated and used to simulate the process. The optimized parameters of ginsenoside Rg3 production are suggested based on the simulation. Results: The rate constants were $0.013h^{-1}$ and $0.073h^{-1}$ for the degradation of ginsenosides Rb1 and Rg3 at $80^{\circ}C$, respectively. The corresponding rate constants at $100^{\circ}C$ were $0.045h^{-1}$ and $0.155h^{-1}$. The estimated activation energies of degradation of ginsenosides Rb1 and Rg3 were 69.2 kJ/mol and 40.9 kJ/mol, respectively. The rate constants at different temperatures were evaluated using the estimated activation energies, and the kinetic profiles of ginsenosides Rb1 and Rg3 at each temperature were simulated based on the proposed kinetic model of consecutive reaction. The optimum strategies for producing ginsenoside Rg3 from ginsenoside Rb1 are suggested based on the simulation. With increased temperature, a high concentration of ginsenoside Rg3 is formed rapidly. However, the concentration decreases quickly after the reaching the maximal concentration value. Conclusion: The optimum temperature for producing ginsenoside Rg3 should be the highest temperature technically feasible below $180^{\circ}C$, in consideration of the cooling time. The optimum reaction time for heat treatment is 30 min.

• Journal of Ginseng Research
• /
• 제37권4호
• /
• pp.451-456
• /
• 2013

Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro. However, previous studies have focused on the pharmacokinetics of a single metabolite or the parent compound and have not described the pharmacokinetics of both compounds in humans. To investigate the pharmacokinetics of ginsenoside Rb1 and compound K, we performed an open-label, single-oral dose pharmacokinetic study using Korean Red Ginseng extract. We enrolled 10 healthy Korean male volunteers in this study. Serial blood samples were collected during 36 h after Korean Red Ginseng extract administration to determine plasma concentrations of ginsenoside Rb1 and compound K. The mean maximum plasma concentration of compound K was $8.35{\pm}3.19$ ng/mL, which was significantly higher than that of ginsenoside Rb1 ($3.94{\pm}1.97$ ng/mL). The half-life of compound K was 7 times shorter than that of ginsenoside Rb1. These results suggest that the pharmacokinetics, especially absorption, of compound K are not influenced by the pharmacokinetics of its parent compound, except the time to reach the maximum plasma concentration The delayed absorption of compound K support the evidence that the intestinal microflora play an important role in the transformation of ginsenoside Rb1 to compound K.

• Journal of Ginseng Research
• /
• 제37권1호
• /
• pp.80-86
• /
• 2013

Korean red ginseng has been shown to possess a variety of biological activities. However, little is known about antiviral activity of ginsenosides of Korean red ginseng. Here, we investigated the protective effect by oral administration of various ginsenosides on the lethal infection of haemagglutinating virus of Japan (HVJ) in mice. In a lethal infection model in which almost all mice infected with HVJ died within 15 days, the mice were administered orally (per os) with 1 mg/mouse of dammarane-type (ginsenoside-Rb1, -Rb2, -Rd, -Re, and -Rg2) or oleanolic acid-type (ginsenoside-Ro) ginsenosides 3, 2, and 1 d before virus infection. Ginsenoside-Rb2 showed the highest protective activity, although other dammarane-type and oleanolic acid-type ginsenosides also induced a significant protection against HVJ. However, neither the consecutive administration with a lower dosage (300 ${\mu}g$/mouse) nor the single administration of ginsenoside-Rb2 (1 mg/mouse) was active. In comparison of the protective activity between ginsenoside-Rb2 and its two hydrolytic products [20(S)- and 20(R)-ginsenoside-Rg3], 20(S)-ginsenoside-Rg3, but not 20(R)-ginsenoside-Rg3, elicited a partial protection against HVJ. The protective effect of ginsenoside-Rb2 and 20(S)-ginsenoside-Rg3 on HVJ infection was confirmed by the reduction of virus titers in the lungs of HVJ-infected mice. These results suggest that ginsenoside-Rb2 is the most effective among ginsenosides from red ginseng to prevent the lethal infection of HVJ, so that this ginsenoside is a promising candidate as a mucosal immunoadjuvant to enhance antiviral activity.