• Journal of Ginseng Research
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• 제38권3호
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• pp.180-186
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• 2014

Background: This study evaluated changes in ginsenoside compositions and antioxidant activities in hydroponic-cultured ginseng roots (HGR) and leaves (HGL) with heating temperature. Methods: Heat treatment was performed at temperatures of $90^{\circ}C$, $110^{\circ}C$, $130^{\circ}C$, and $150^{\circ}C$ for 2 hours Results: The ginsenoside content varied significantly with heating temperature. The levels of ginsenosides Rg1 and Re in HGR decreased with increasing heating temperature. Ginsenosides F2, F4, Rk3, Rh4, Rg3 (S form), Rg3 (R form), Rk1, and Rg5, which were absent in the raw ginseng, were formed after heat treatment. The levels of ginsenosides Rg1, Re, Rf, and Rb1 in HGL decreased with increasing heating temperature. Conversely, ginsenosides Rk3, Rh4, Rg3 (R form), Rk1, and Rg5 increased with increasing heating temperature. In addition, ginsenoside contents of heated HGL were slightly higher than those of HGR. The highest extraction yield was 14.39% at $130^{\circ}C$, whereas the lowest value was 10.30% at $150^{\circ}C$ After heating, polyphenol contents of HGR and HGL increased from 0.43 mg gallic acid equivalent/g (mg GAE eq/g) and 0.74 mg GAE eq/g to 6.16 mg GAE eq/g and 2.86 mg GAE eq/g, respectively. Conclusion: Antioxidant activities of HGR and HGL, measured by 1,1-diphenyl-2-picrylhydrazyl and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging ability, increased with increasing heating temperature. These results may aid in improving the biological activity and quality of ginseng subjected to heat treatments.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2002년도 학술대회지
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• pp.376-384
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• 2002

Object To find out which of the 27 ginsenosides isolated from Panax ginseng C.A. Mey that may inhibit the proliferation of human osteosaocoma cell line $U_2OS$. Methods Effects of each individual ginsenoside on the proliferation of $U_2OS$ cell were studied by determining the viability of cancer cells during culture with or without the presence of the test compound. DNA assay was determined by flow cytometry. Results Ginsonosides -Ro, $-Rh_l,\;-Rh_2,\;-F_1\;and\;-L_8$ at concentrations of 5 ,umol/L could obviously suppress the proliferation of $U_2OS$ cells while ginsenosides $-Rg_1,\;-F_3,$ -Rf, PPT and PT significantly inhibited the cancer cells. Flow cytometry revealed that ginsenosides $-Ro,-Rg_1-Rf,-F_1-Rh_2,PPT$ and PT induced cell cycle arrest at $G_0/G_1$ phase with obvious decrease of cell count at Sand $G_2+M$ phase, Moreover, ginsenosides $-Rf_1,-Rg_1,\;-F_1$ and PPT induced significantly high rates of cell death as compared with the control. Conclusion These data suggested that ginsenosides inhibited $U_2OS$ proliferation Via cell cycle arrest or induction of cell death.

• 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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.115-115
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• 1993

i) total ginsenoside의 분리 시판백삼(900g)을 상법에 따라 처리, 조 saponin을 얻었으며 (24g) 이를 20(S)-protopanaxadiol을 얻는 원료로 사용하였다. ii) 20(S)-protopanaxadiol의 분리연구 본 연구에서 가장 중요한 단계는 20(S)-protopanaxadiol을 다량 얻는 것이다. 그러나 인삼 saponin을 산으로 가수분해하면 진성 aglycone 인 20(S)-protopanaxadiol이 얻어지지 않고 artifact sapogenol인 panaxadiol이 얻어진다. 이를 해결하기 위하여 sodium ethoxide의 ethanol 용액, sodium butoxide의 butanol 용액, sodium methoxide의 pyridine 용액, sodium methoxide의 DMSO 용액등의 조건에서의 가수분해를 검토한 결과 aprotic polar splvent인 DMSO용매중에서의 분해가 가장 좋음을 알았다. iii) ginsenoside Rh$_2$의 합성연구 Koenigs-Knorr 법에 의하여 bromosugar와 20(S)-protopanaxadiol의 glycosidation 반응결과 약 40%의 수득률로 합성됨을 확인하였다.

• 한국응용과학기술학회지
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• 제35권4호
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• pp.1213-1223
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• 2018

본 연구는 인삼 잎의 이용증대를 위해 마이크로웨이브에 의한 인삼 잎의 잔류농약 추출효과와 발효 인삼 잎의 ginsenoside 유용 유도체의 전환 검토 및 품질 특성을 분석 하였다. 인삼 잎에 잔류되어 있는 tolclofos-methyl와 azoxystrobin을 microwave로 추출하기 위한 용매는 hexane이 가장 효율적 이었다. tolclofos-methyl와 azoxystrobin이 잔류되어 있는 인삼 잎에서의 microwave를 이용한 추출 최적 조건은 power 50~95 watts, 추출용매는 hexane, 추출시간은 3분으로 나타났다. 인삼 잎 추출물의 발효에서 발효전과 비교하여 $Rg_1$과 $Rb_1$은 감소한 반면 $Rh_1$, $Rg_3$, $Rk_1$ 및 $Rh_2$는 발효 후 모두 증가한 것으로 나타났다. 특히 홍삼에서 대표적인 성분으로 알려져 있는 $Rg_3$의 경우 발효전 $2.77{\mu}g/g$에서 발효 후 균주의 종류에 따라 $70.62{\sim}77.61{\mu}g/g$으로 증가하였다. 7일간 발효 후 인삼 잎의 총 페놀성 화합물 및 전자공여능은 일부 균주에서는 발효전과 비교하여 감소하다가 다시 증가하는 경향을 나타내었으나, 발효가 진행됨에 따라 전반적으로 감소되는 경향을 나타내었다.

• Journal of Ginseng Research
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• 제37권1호
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• pp.108-116
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• 2013

For the improvement of ginsenoside bioavailability, the ginsenosides of fermented red ginseng by Phellinus linteus (FRG) were examined with respect to bioavailability and physiological activity. The polyphenol content of FRG ($19.14{\pm}0.50$ mg/g) was significantly higher (p<0.05) compared with that of non-fermented red ginseng (NFRG, $11.31{\pm}1.15$ mg/g). The antioxidant activities in FRG, such as 2,2'-diphenyl-1-picrylhydrazyl, 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid, and ferric reducing antioxidant power, were significantly higher (p<0.05) than those in NFRG. The HPLC analysis results showed that the FRG had a high level of ginsenoside metabolites. The total ginsenoside contents in NFRG and FRG were $41.65{\pm}1.53$ mg/g and $50.12{\pm}1.43$ mg/g, respectively. However, FRG had a significantly higher content ($33.90{\pm}0.97$ mg/g) of ginsenoside metabolites (Rg3, Rg5, Rk1, compound K, Rh1, F2, and Rg2) compared with NFRG ($14.75{\pm}0.46$ mg/g). The skin permeability of FRG was higher than that of NFRG using Franz diffusion cell models. In particular, after 3 h, the skin permeability of FRG was significantly higher (p<0.05) than that of NFRG. Using a rat everted intestinal sac model, FRG showed a high transport level compared with NFRG after 1 h. FRG had dramatically improved bioavailability compared with NFRG as indicated by skin permeation and intestinal permeability. The significantly greater bioavailability of FRG may have been due to the transformation of its ginsenosides by fermentation to more easily absorbable forms (ginsenoside metabolites).

• Journal of Ginseng Research
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• 제44권5호
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• pp.725-737
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• 2020

Background: T-cell acute lymphoblastic leukemia (T-ALL) is a kind of aggressive hematological cancer, and the PI3K/Akt/mTOR signaling pathway is activated in most patients with T-ALL and responsible for poor prognosis. 20(S)-Ginsenoside Rh2 (20(S)-GRh2) is a major active compound extracted from ginseng, which exhibits anti-cancer effects. However, the underlying anticancer mechanisms of 20(S)-GRh2 targeting the PI3K/Akt/mTOR pathway in T-ALL have not been explored. Methods: Cell growth and cell cycle were determined to investigate the effect of 20(S)-GRh2 on ALL cells. PI3K/Akt/mTOR pathway-related proteins were detected in 20(S)-GRh2-treated Jurkat cells by immunoblotting. Antitumor effect of 20(S)-GRh2 against T-ALL was investigated in xenograft mice. The mechanisms of 20(S)-GRh2 against T-ALL were examined by cell proliferation, apoptosis, and autophagy. Results: In the present study, the results showed that 20(S)-GRh2 decreased cell growth and arrested cell cycle at the G1 phase in ALL cells. 20(S)-GRh2 induced apoptosis through enhancing reactive oxygen species generation and upregulating apoptosis-related proteins. 20(S)-GRh2 significantly elevated the levels of pEGFP-LC3 and autophagy-related proteins in Jurkat cells. Furthermore, the PI3K/Akt/mTOR signaling pathway was effectively blocked by 20(S)-GRh2. 20(S)-GRh2 suppressed cell proliferation and promoted apoptosis and autophagy by suppressing the PI3K/Akt/mTOR pathway in Jurkat cells. Finally, 20(S)-GRh2 alleviated symptoms of leukemia and reduced the number of white blood cells and CD3 staining in the spleen of xenograft mice, indicating antitumor effects against T-ALL in vivo. Conclusion: These findings indicate that 20(S)-GRh2 exhibits beneficial effects against T-ALL through the PI3K/Akt/mTOR pathway and could be a natural product of novel target for T-ALL therapy.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1993년도 학술대회지
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• pp.74-83
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• 1993

In an attempt toward the synthesis of the difficulty accessible ginseng saponins the four dammarane glycosides identical to the natural $ginsenosides-Rh_2,$ - F2, compound K and chikusetsusaponin - LT8 have been prepared from betulafolienetriol(=dammar-24-ene-$3{\alpha},12{\beta}\;20(S)-triol).\;3-O-{\beta}-D-Glucopyranoside$ of 20(S) - protopanaxadiol $(=ginsenoside-Rh_2)$ have been obtained by the regio - and stereoselective glycosylation of the $12-O-acetyldammar-24-ene-3{\beta},\;12{\beta},$ 20(S)-triol. The 12-ketoderivative of 20(S)-protopanaxadiol has been used as aglycon in synthesis of chikusetsusaponin - LT8. Attempted regio - and stereoselective glycosylation of the less reactive tertiary C - 20 - hydroxyl group in order to synthesize the $20-O-{\beta}-D-glucopyranoside$ of 20(S)-protopanaxadiol(=compound K) using 3, 12 - di - O - acetyldammar - 24 - ene - $3{\beta},12{\beta},20(S)$-trial as aglycon was unsuccessful. Glycosylation of 3, 12 - diketone of betulafolienetriol followed by $NaBH_4$ reduction yielded the $20-O-{\beta}-D-glucopyranoside\;of\;dammar-24-ene-3{\beta},12{\alpha},$ 20(S)-triol, the $12{\alpha}-epimer$ of 20(S) - protopanaxadiol. Moreover, a number of semisynthetic ocotillol - type glucosides, analogs of natural pseudoginsenosides, have been prepared.

• Journal of Ginseng Research
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• 제40권2호
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• pp.105-112
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• 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 Microbiology and Biotechnology
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• 제21권10호
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• pp.1057-1063
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• 2011

Herein, a novel ginsenosidase, named ginsenosidase type IV, hydrolyzing 6-O-multi-glycosides of protopanaxatriol-type ginsenosides (PPT), such as Re, R1, Rf, and Rg2, was isolated from the Aspergillus sp. 39g strain, purified, and characterized. Ginsenosidase type IV was able to hydrolyze the 6-O-${\alpha}$-L-($1{\rightarrow}2$)-rhamnoside of Re and the 6-O-${\beta}$-D-($1{\rightarrow}2$)-xyloside of R1 into ginsenoside Rg1. Subsequently, it could hydrolyze the 6-O-${\beta}$-D-glucoside of Rg1 into F1. Similarly, it was able to hydrolyze the 6-O-$_{\alpha}$-L-($1{\rightarrow}2$)-rhamnoside of Rg2 and the 6-O-${\beta}$-D-($1{\rightarrow}2$)-glucoside of Rf into Rh1, and then further hydrolyze Rh1 into its aglycone. However, ginsenosidase type IV could not hydrolyze the 3-O- or 20-O-glycosides of protopanaxadiol-type ginsenosides (PPD), such as Rb1, Rb2, Rb3, Rc, and Rd. These exhibited properties are significantly different from those of glycosidases described in Enzyme Nomenclature by the NC-IUBMB. The optimal temperature and pH for ginsenosidase type IV were $40^{\circ}C$ and 6.0, respectively. The activity of ginsenosidase type IV was slightly improved by the $Mg^{2+}$ ion, and inhibited by $Cu^{2+}$ and $Fe^{2+}$ ions. The molecular mass of the enzyme, based on SDS-PAGE, was noted as being approximately 56 kDa.