• Journal of Ginseng Research
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• v.40 no.2
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• pp.121-126
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• 2016

Background: Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. However, the usage of ginsenoside F1 is restricted owing to the small amount found in Korean ginseng. Methods: To enhance the production of ginsenoside F1 as a 10 g unit with high specificity, yield, and purity, an enzymatic bioconversion method was developed to adopt the commercial enzyme Cellulase KN from Aspergillus niger with food grade, which has ginsenoside-transforming ability. The proposed optimum reaction conditions of Cellulase KN were pH 5.0 and $50^{\circ}C$. Results: Cellulase KN could effectively transform the ginsenosides Re and Rg1 into F1. A scaled-up biotransformation reaction was performed in a 10 L jar fermenter at pH 5.0 and $50^{\circ}C$ for 48 h with protopanaxatriol-type ginsenoside mixture (at a concentration of 10 mg/mL) from ginseng roots. Finally, 13.0 g of F1 was produced from 50 g of protopanaxatriol-type ginsenoside mixture with $91.5{\pm}1.1%$ chromatographic purity. Conclusion: The results suggest that this enzymatic method could be exploited usefully for the preparation of ginsenoside F1 to be used in cosmetic, functional food, and pharmaceutical industries.

• Korean Journal of Pharmacognosy
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• v.44 no.1
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• pp.10-15
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• 2013

This study was carried to establish a simple isolation and purification method of ginsenoside $F_1$ from leaves of Panax ginseng and was to evaluate the inhibitory effect of purified ginsenoside $F_1$ on the activities of elastase and tyrosinase. The content of ginsenoside $F_1$ was 90-fold higher in leaves than in root of ginseng. Ginsenoside $F_1$ was isolated from EtOAc fraction between EtOAc and alkalized water of 80% EtOH extract after remove of hydrophobic components. The 50% inhibitory concentration ($IC_{50}$) of ginsenoside $F_1$ on elastase activity and tyrosinase activity was 1.07 mM and 1.81 mM, respectively. Especially, inhibitory effect of ginsenoside $F_1$ on tyrosinase activity was higher than that of arbutin ($IC_{50}$; 2.20 mM). These results indicate that ginsenoside $F_1$ have a potential for industrial cosmetic materials.

• Journal of Microbiology and Biotechnology
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• v.17 no.12
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• pp.1937-1943
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• 2007

A new strain, GS603, having ${\beta}$-glucosidase activity was isolated from soil of a ginseng field, and its ability to convert major ginsenoside $Rb_1$ to minor ginsenoside or gypenoside was studied. Strain GS603 was identified as an Intrasporangium species by phylogenetic analysis and showed high ginsenoside-converting activity in LB and TSA broth but not in nutrient broth. The culture broth of the strain GS603 could convert ginsenoside $Rb_1$i into two metabolites, which were analyzed by TLC and HPLC and shown to be the minor ginsenoside $F_2$ and gypenoside XVII by NMR.

• Korean Journal of Medicinal Crop Science
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• v.26 no.6
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• pp.464-470
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• 2018

Background: Ginseng produced by hydroponics can be cultivated without using agricultural chemicals; thus, it can be used as a raw materials for functional foods, medicines, and cosmetics. This study aimed to determine the optimal harvesting time to obtain the highest levels of ginsenoside and ginseng, as this was not previously unknown. Methods and Results: One-year-old organic ginseng seedlings were transplanted and cultivated using hydroponics for 150 days in a venlo-type greenhouse, using ginseng nursery bed soil and a nutrient solution ($NO_3{^-}-N$; 6.165, P; 3.525, K; 5.625, Ca; 4.365, Mg; 5.085, S; $5.31mEq/{\ell}$). Ginsenoside content and fresh and dry weights were higher at 120 days after transplanting than at 30, 60, 90, and 150 days. Total ginsenoside content was 11.86 times higher in the leaf and stem than in the root at 120 days after transplanting. Ginsenosides F1, F2, F3, and F5 were detected in ginseng leaves and stems. These chemical compounds are known to be effective in altering skin properties, including whitening, anti-inflammation, and anti-aging. Conclusions: Optimal harvesting time for ginseng cultivated using hydroponics was 120 days after transplanting when the biomass and ginsenoside content were highest.

• Proceedings of the Ginseng society Conference
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• 1978.09a
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• pp.55-66
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• 1978

Five ginsenosides $(A_1,\;A_2,\;B_1,\;B_2,\;C)$ and a yellow pigment were isolated from American ginseng stems and leaves. Ginsenoside $A_2,\;B_1,\;B_2$ and C were proven to be identical with Korean ginseng root ginsenoside $Rg_1,$ Rd, Re and $Rb_2,$ respectively. The yellow pigment proved identical with panasenoside isolated from Korean ginseng leaves. Ginsenoside $A_1$, which was also present in American ginseng roots, was not identical to any of the known root (ginsenoside $R_{0}-Rg_{2}$) and leaf (ginsenoside $F_{1}-F_{3}$) Korean ginseng saponins. A gas-liquid chromatographic method was developed to analyze ginsenosides and sapogenins in rabbit plasma and urine samples. Panasenoside and stigmasterol were found to be the best internal standards for ginsenosides and sapogenihs, respectively. Ginsenoside C had a significantly longer half-life, higher plasma protein binding, lower metabolic and renal clearance than ginsenoside $A_1,\;A_2\;and\;B_2$. Ginsenosides were not found in rabbit plasma and urine samples after oral administration. Ginsenoside C had a higher toxicity than ginsenoside $A_2$ after intraperitoneal administration to mice. Toxicity was not observed after oral administration of the ginsenosides.

• Journal of Ginseng Research
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• v.35 no.3
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• pp.344-351
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• 2011

Ginsenoside $Rb_1$ is the main component in ginsenosides. It is a protopanaxadiol-type ginsenoside that has a dammarane-type triterpenoid as an aglycone. In this study, ginsenoside $Rb_1$ was transformed into gypenoside XVII, ginsenoside Rd, ginsenoside $F_2$ and compound K by glycosidase from Leuconostoc mesenteroides DC102. The optimum time for the conversion was about 72 h at a constant pH of 6.0 to 8.0 and the optimum temperature was about $30^{\circ}C$. Under optimal conditions, ginsenoside $Rb_1$ was decomposed and converted into compound K by 72 h post-reaction (99%). The enzymatic reaction was analyzed by highperformance liquid chromatography, suggesting the transformation pathway: ginsenoside $Rb_1$ ${\rightarrow}$ gypenoside XVII and ginsenoside Rd${\rightarrow}$ginsenoside $F_2{\rightarrow}$compound K.

• Journal of Ginseng Research
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• v.36 no.4
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• pp.418-424
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• 2012

This study focused on the enzymatic biotransformation of the major ginsenoside Rb1 into Rd for the mass production of minor ginsenosides using a novel recombinant ${\beta}$-glucosidase from Flavobacterium johnsoniae. The gene (bglF3) consisting of 2,235 bp (744 amino acid residues) was cloned and the recombinant enzyme overexpressed in Escherichia coli BL21(DE3) was characterized. This enzyme could transform ginsenoside Rb1 and gypenoside XVII to the ginsenosides Rd and F2, respectively. The glutathione S-transferase (GST) fused BglF3 was purified with GST-bind agarose resin and characterized. The kinetic parameters for ${\beta}$-glucosidase had apparent $K_m$ values of $0.91{\pm}0.02$ and $2.84{\pm}0.05$ mM and $V_{max}$ values of $5.75{\pm}0.12$ and $0.71{\pm}0.01{\mu}mol{\cdot}min^{-1}{\cdot}mg$ of $protein^{-1}$ against p-nitrophenyl-${\beta}$-D-glucopyranoside and Rb1, respectively. At optimal conditions of pH 6.0 and $37^{\circ}C$, BglF3 could only hydrolyze the outer glucose moiety of ginsenoside Rb1 and gypenoside XVII at the C-20 position of aglycon into ginsenosides Rd and F2, respectively. These results indicate that the recombinant BglF3 could be useful for the mass production of ginsenosides Rd and F2 in the pharmaceutical or cosmetic industry.

• Korean Journal of Medicinal Crop Science
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• v.16 no.3
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• pp.155-160
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• 2008

Ginsenosides have been regarded as the principal components, responsible for the pharmacological and biological activities of ginseng. Absorption of major ginsenosides at the gastrointestinal tract was extremely low, when ginseng taken orally. In order to improve the absorption and bioavailability, transformation of major ginsenosides into more active and valuable minor ginsenoside is much required. In this present study, We isolated a lactic acid bacteria Leuconostoc fallax LH3 from the Korean fermented food Kimchi, which have higher ${\beta}$-glucosidase activity. Using the ethanol precipitated curd enzyme of Leuconostoc fallax LH3, we investigated the biotransformation of ginsenoside Rd at different experimental condition to increase transformation. The maximum convertion was supported at 30 $^{\circ}C$ and decreased when temperatures increased. In order to optimize the effect of pH, the curd enzyme was mixed 20 mM sodium phosphate buffer (pH 3.5 to pH 8.0). Ginsenoside Rd was almost hydrolyzed between pH 7.0 and pH 9.0, but not hydrolyzed above pH 10.0. Ginsenoside Rd was hydrolyzed after 24 hrs incubation, but whereas the ginsenoside F2 was appeared from 36 hrs, and all ginsenoside Rd was transformed to F2 after the 60 hrs incubation. Based on this study, the curd enzyme of Leuconostoc fallax LH3 transformed the ginsenoside Rd at the 30$^{\circ}C$ and the pH optimum of 7.0 to 9.0 after the 60 hrs incubation time.

• Natural Product Sciences
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• v.14 no.3
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• pp.171-176
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• 2008

Column chromatographic separation of 70% EtOH extract of the roots of Korean cultivated-wild ginseng led to the isolation of ten ginsenosides (1 - 10). The isolated compounds were identified as ginsenoside $Rg_1$ (1), ginsenoside Re (2), ginsenoside Rc (3), ginsenoside $Rb_1$ (4), ginsenoside $Rb_2$ (5), ginsenoside Rd (6), ginsenoside $Rg_3$ (7), ginsenoside $F_2$ (8), ginsenoside $Rb_3$ (9), and ginsenoside $Rd_2$ (10) by physicochemical and spectroscopic methods. The compounds (1 - 10) were for the first time isolated from the roots of Korean cultivated-wild ginseng.

• Journal of Microbiology and Biotechnology
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• v.27 no.7
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• pp.1233-1241
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• 2017

The ginsenoside Rh2 has strong anti-cancer, anti-inflammatory, and anti-diabetic effects. However, the application of ginsenoside Rh2 is restricted because of the small amounts found in Korean white and red ginsengs. To enhance the production of ginsenoside Rh2-MIX (comprising 20(S)-Rh2, 20(R)-Rh2, Rk2, and Rh3 as a 10-g unit) with high specificity, yield, and purity, a new combination of enzymatic conversion using the commercial enzyme Viscozyme L followed by acid treatment was developed. Viscozyme L treatment at pH 5.0 and $50^{\circ}C$ was used initially to transform the major ginsenosides Rb1, Rb2, Rc, and Rd into ginsenoside F2, followed by acid-heat treatment using citric acid 2% (w/v) at pH 2.0 and $121^{\circ}C$ for 15 min. Scale-up production in a 10-L jar fermenter, using 60 g of the protopanaxadiol-type ginsenoside mixture from ginseng roots, produced 24 g of ginsenoside Rh2-MIX. Using 2 g of Rh2-MIX, 131 mg of 20(S)-Rh2, 58 mg of 20(R)-Rh2, 47 mg of Rk2, and 26 mg of Rh3 were obtained at over 98% chromatographic purity. Then, the anti-cancer effect of the four purified ginsenosides was investigated on B16F10, MDA-MB-231, and HuH-7 cell lines. As a result, these four rare ginsenosides markedly inhibited the growth of the cancer cell lines. These results suggested that rare ginsenoside Rh2-MIX could be exploited to prepare an anti-cancer supplement in the functional food and pharmaceutical industries.