• 한국약용작물학회지
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• 제16권3호
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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.

• 한국균학회지
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• 제17권1호
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• pp.31-34
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• 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
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• 제38권1호
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• pp.47-51
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• 2014

The transformation of ginsenoside Rb1 into a specific minor ginsenoside using Aspergillus niger KCCM 11239, as well as the identification of the transformed products and the pathway via thin layer chromatography and high performance liquid chromatography were evaluated to develop a new biologically active material. The conversion of ginsenoside Rb1 generated Rd, Rg3, Rh2, and compound K although the reaction rates were low due to the low concentration. In enzymatic conversion, all of the ginsenoside Rb1 was converted to ginsenoside Rd and ginsenoside Rg3 after 24 h of incubation. The crude enzyme (b-glucosidase) from A. niger KCCM 11239 hydrolyzed the ${\beta}$-($1{\rightarrow}6$)-glucosidic linkage at the C-20 of ginsenoside Rb1 to generate ginsenoside Rd and ginsenoside Rg3. Our experimental demonstration showing that A. niger KCCM 11239 produces the ginsenoside-hydrolyzing b-glucosidase reflects the feasibility of developing a specific bioconversion process to obtain active minor ginsenosides.

• 대한수의학회지
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• 제44권2호
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• pp.179-184
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• 2004

The purpose of the study was to investigate the effect of ginseng saponins (panaxadiol, ginsenoside $Rb_1$, $Rb_2$, Rc, Rd) on jejunal crypt survival, endogenous spleen colony formation and apoptosis in jejunal crypt cells of mice irradiated with gamma-ray. ICR mice were given each saponin (i.p. 50 mg/kg of body weight) at 24 hours before irradiation. The radioprotective effects of saponins were compared with the irradiation control respectively. The jejunal crypts were protected by pretreatment with ginsenoside Rc (p<0.05) and Rd (p<0.05). The spleen colony was increased by pretreatment with panaxadiol (p<0.05) and ginsenoside Rd (p<0.05). And the frequency of radiation induced apoptosis was significantly reduced by pretreatment with panaxadiol (p<0.05), ginsenoside Rb2 (p<0.05), Rc (p<0.05) and Rd (p<0.01). These results suggest that ginsenoside Rc, Rd might have a major radioprotective effect.

• Journal of Ginseng Research
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• 제46권5호
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• pp.700-709
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• 2022

Background: Ginsenoside Rd is a natural compound with promising neuroprotective effects. However, the underlying mechanisms are still not well-understood. In this study, we explored whether ginsenoside Rd exerts protective effects on cerebral endothelial cells after oxygen-glucose deprivation/reoxygenation (OGD/R) treatment and its potential docking proteins related to the underlying regulations. Method: Commercially available primary human brain microvessel endothelial cells (HBMECs) were used for in vitro OGD/R studies. Cell viability, pyroptosis-associated protein expression and tight junction protein degradation were evaluated. Molecular docking proteins were predicted. Subsequent surface plasmon resonance (SPR) technology was utilized for validation. Flow cytometry was performed to quantify caspase-1 positive and PI positive (caspase-1+/PI+) pyroptotic cells. Results: Ginsenoside Rd treatment attenuated OGD/R-induced damage of blood-brain barrier (BBB) integrity in vitro. It suppressed NLRP3 inflammasome activation (increased expression of NLRP3, cleaved caspase-1, IL-1β and GSDMD-N terminal (NT)) and subsequent cellular pyroptosis (caspase-1+/PI + cells). Ginsenoside Rd interacted with SLC5A1 with a high affinity and reduced OGD/R-induced sodium influx and potassium efflux in HBMECs. Inhibiting SLC5A1 using phlorizin suppressed OGD/R-activated NLRP3 inflammasome and pyroptosis in HBMECs. Conclusion: Ginsenoside Rd protects HBMECs from OGD/R-induced injury partially via binding to SLC5A1, reducing OGD/R-induced sodium influx and potassium efflux, thereby alleviating NLRP3 inflammasome activation and pyroptosis.

• Journal of Ginseng Research
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• 제37권2호
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• pp.201-209
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• 2013

Ginsenoside, one of the active ingredients of Panax ginseng, has a variety of physiologic and pharmacologic effects. The purpose of this study was to explore the effects of ginsenoside Rd (G-Rd) on melastatin type transient receptor potential 7 (TRPM7) channels with respect to the proliferation and survival of AGS and MCF-7 cells (a gastric and a breast cancer cell line, respectively). AGS and MCF-7 cells were treated with different concentrations of G-Rd, and caspase-3 activities, mitochondrial depolarizations, and sub-G1 fractions were analyzed to determine if cell death occurred by apoptosis. In addition, human embryonic kidney (HEK) 293 cells overexpressing TRPM7 channels were used to confirm the role of TRPM7 channels. G-Rd inhibited the proliferation and survival of AGS and MCF-7 cells and enhanced caspase-3 activity, mitochondrial depolarization, and sub-G1 populations. In addition, G-Rd inhibited TRPM7-like currents in AGS and MCF-7 cells and in TRPM7 channel overexpressing HEK 293 cells, as determined by whole cell voltage-clamp recordings. Furthermore, TRPM7 overexpression in HEK 293 cells promoted G-Rd induced cell death. These findings suggest that G-Rd inhibits the proliferation and survival of gastric and breast cancer cells by inhibiting TRPM7 channel activity.

• Journal of Ginseng Research
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• 제35권3호
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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 Microbiology and Biotechnology
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• 제30권3호
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• pp.391-397
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• 2020

In this study, we used a novel α-L-arabinopyranosidase (AbpBs) obtained from ginsenoside-converting Blastococcus saxobsidens that was cloned and expressed in Escherichia coli BL21 (DE3), and then applied it in the biotransformation of ginsenoside Rb₂ into Rd. The gene, termed AbpBs, consisting of 2,406 nucleotides (801 amino acid residues), and with a predicted translated protein molecular mass of 86.4 kDa, was cloned into a pGEX4T-1 vector. A BLAST search using the AbpBs amino acid sequence revealed significant homology with a family 2 glycoside hydrolase (GH2). The over-expressed recombinant AbpBs in Escherichia coli BL21 (DE3) catalyzed the hydrolysis of the arabinopyranose moiety attached to the C-20 position of ginsenoside Rb₂ under optimal conditions (pH 7.0 and 40℃). Kinetic parameters for α-L-arabinopyranosidase showed apparent K_m and V_max values of 0.078 ± 0.0002 μM and 1.4 ± 0.1 μmol/min/mg of protein against p-nitrophenyl-α-L-arabinopyranoside. Using a purified AbpBs (1 ㎍/ml), 0.1% of ginsenoside Rb₂ was completely converted to ginsenoside Rd within 1 h. The recombinant AbpBs could be useful for high-yield, rapid, and low-cost preparation of ginsenoside Rd from Rb₂.

• Journal of Ginseng Research
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• 제24권4호
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• pp.162-167
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• 2000

40주령의 생쥐에게 홍삼 총사포닌, PD, PT ginsenoside G-Rd, 5-Re 및 C-K 등을 경구투여하여 생쥐 간에 미치는 항산화효과를 알아보기 위하여 SOD와 CAT활성도 변화와 과산화수소 함량, MDA수준의 변화를 조사하였다. SOD와CAT 활성도는 모든 홍삼 사포닌 투여군에서 증가하였지만 PD투여군에서만 유의성(p<0.01) 있는 증가를 보였다. 과산화수소 함량은 홍삼 사포닌의 투여로 모두 감소하였으며, 특히 PD, PT G-Rd(p<0.01) 및 G-Re 투여군(p<0.05)에서 유의성 있게 감소하였다. CAT 활성도는 G-Rd 투여군에서 유의성(p<0.05) 있게 증가하였다. 지질과산화의 최종산물인MDA수준은 홍삼 투여군 모두에서 감소되었으며, 특히 G-Rd투여군에서 유의성(p<0.05) 있게 감소하였다. 따라서 홍삼 사포닌 성분은 40주령의 생쥐 간에서 항산화효소의 합성증가를 유도하거나 활성을 촉매하여 활성산소들을 효율적으로 소거하는 기능과 지질과산화를 억제하는 항산화물질의 합성능력을 강화하여 산화적 손상으로부터 생체를 방어하는 효과가 있다고 생각되었다. 특히 홍삼 사포닌 중에서도 PD와G-Rd투여군은 항산화 효소활성을 증가시키는 반면 지질과산화를 .억제하였다.

• 약학회지
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• 제57권1호
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• pp.37-42
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• 2013

In this present study, we determined the immunoregulatory activity of ginsenoside Rd extract from Panax ginseng. To determine the activity, we tested Rd against $CD4^+$ Th cells in a murine model of type 1 diabetes, which involves Th1-dominant immunity. The type 1 diabetes was caused by streptozotocin (STZ) and the severity of the diabetes was evaluated by measuring the degree of hyperglycemia, a major symptom of diabetes. The data resulting from experiments showed that ginsenoside Rd induced a greater level of Th1 type cytokines [IFN-${\gamma}$ & IL-2] than Th2 type [IL-4 & IL-10] (P<0.05), which was determined by cytokine profile analysis. In the animal model of diabetes, the depletion of $CD4^+$ Th cells by a treatment of anti-CD4 mAb resulted in considerably lower values of blood-glucose levels than those of the mAb-untreated mice, which indicates that the Th1 immune response from $CD4^+$ Th cells are responsible for diabetes. Based on these observations, the effect of Rd on diabetes was examined in the same animal model. Results showed that Rd-treated mice groups had increased levels of blood glucose compared to Rd-untreated mice groups that were used as a negative control (P<0.05). In other words, Rd aggravated the diabetes via the Th1 immune response. In conclusion, ginsenoside Rd had an immunoregulatory activity of Th1-dominant immunity.