• Journal of Ginseng Research
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• v.42 no.3
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• pp.277-287
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• 2018

Background: Temperature is an essential condition in red ginseng processing. The pharmacological activities of red ginseng under different steam temperatures are significantly different. Methods: In this study, an ultrahigh-performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry was developed to distinguish the red ginseng products that were steamed at high and low temperatures. Multivariate statistical analyses such as principal component analysis and supervised orthogonal partial least squared discrimination analysis were used to determine the influential components of the different samples. Results: The results showed that different steamed red ginseng samples can be identified, and the characteristic components were 20-gluco-ginsenoside Rf, ginsenoside Re, ginsenoside Rg1, and malonyl-ginsenoside Rb1 in red ginseng steamed at low temperature. Meanwhile, the characteristic components in red ginseng steamed at high temperature were 20R-ginsenoside Rs3 and ginsenoside Rs4. Polar ginsenosides were abundant in red ginseng steamed at low temperature, whereas higher levels of less polar ginsenosides were detected in red ginseng steamed at high temperature. Conclusion: This study makes the first time that differences between red ginseng steamed under different temperatures and their ginsenosides transformation have been observed systematically at the chemistry level. The results suggested that the identified chemical markers can be used to illustrate the transformation of ginsenosides in red ginseng processing.

• Journal of Ginseng Research
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• v.22 no.3
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• pp.216-221
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• 1998

We examined the anti-invasive activity of ginsenosides Rhl, Rha on the highly metastatic HT1080 human fibrosarcoma cell line. In vitro invasion assay showed ginsenoside Rhr reduced tumor cell invasion through a reconstituted basement membrane in a transwell chamber more than ginsenoside Rh1. Significant down-regulation of matrix metalloproteinase-9 (MMP-9) by ginsenosides Rh, and Rh2 was detected by Northern blot analysis. However, the expression of MMP-2 was not affected by Rh, and Rhr. The expression of tissue inhibitor of metalloproteinase-2 (TIMP-2) was increased by Rhl after 0.5, 1 or 3 day-treatment but reduced after 6 day-treatment. However, the expression of TIMP-2 was not changed by treatment with Rh2. Plasminogen activator inhibitor (PAI) and urokinase-type plasmlnogen activator (uPA) were not changed by treatment with Rh1 and Rh2 for 3 and 6 days. Quantitative gelatin-based zymography confirmed a markedly reduced expression of MMP-9 but MMP-2 after treatments with ginsenosides Rhl and Rha. These results suggest that down-regulation of MMP-9 contributes to the anti-invasive activity of ginsenosides Rhl and Rhr in the HT1080 cells.

• Applied Biological Chemistry
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• v.51 no.3
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• pp.188-193
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• 2008

This study was conducted to investigate the effect of moisture content and pressure on extraction yield, crude saponins and ginsenoside contents of puffed Korean ginseng. Puffed ginsengs showed relatively higher extraction yield ($50.0{\sim}62.1%$) and amounts of crude saponins ($19.6{\sim}48.8$ mg/g ginseng) than no-puffed ginseng ($37.6{\pm}0.8%$ and $11.0{\pm}1.0$ mg/g ginseng), respectively. The highest extraction yield and amounts of crude saponins were obtained in 8.0% moisture content sample puffed at 10 $kg_f/cm^2$. In HPLC analysis, amounts of measured major ginsenosides (Rb1, Rb2, Rc, Rd, Re, and Rg1) decreased with increasing puffing pressure, yet contents of almost all major gin senosides were higher than control (no-puffed). On the other hand, ginsenoside Rg3 were produced after puffing suggesting that chemical structure of some ginsenosides might be altered during the puffing process. These results indicate that puffing can increase the extraction yield and crude saponin contents and it could influence the ginsenoside composition.

• Journal of Ginseng Research
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• v.42 no.2
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• pp.199-207
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• 2018

Background: Ginseng is a well-known traditional Chinese medicine that has been widely used in a range of therapeutic and healthcare applications in East Asian countries. Microbial transformation is regarded as an effective and useful technology in modification of nature products for finding new chemical derivatives with potent bioactivities. In this study, three minor derivatives of ginsenoside compound K were isolated and the inducing effects in the Wingless-type MMTV integration site (Wnt) signaling pathway were also investigated. Methods: New compounds were purified from scale-up fermentation of ginsenoside Rb1 by Paecilomyces bainier sp. 229 through repeated silica gel column chromatography and high pressure liquid chromatography. Their structures were determined based on spectral data and X-ray diffraction. The inductive activities of these compounds on the Wnt signaling pathway were conducted on MC3T3-E1 cells by quantitative real-time polymerase chain reaction analysis. Results: The structures of a known 3-keto derivative and two new dehydrogenated metabolites were elucidated. The crystal structure of the 3-keto derivative was reported for the first time and its conformation was compared with that of ginsenoside compound K. The inductive effects of these compounds on osteogenic differentiation by activating the Wnt/b-catenin signaling pathway were explained for the first time. Conclusion: This study may provide a new insight into the metabolic pathway of ginsenoside by microbial transformation. In addition, the results might provide a reasonable explanation for the activity of ginseng in treating osteoporosis and supply good monomer ginsenoside resources for nutraceutical or pharmaceutical development.

• Journal of Ginseng Research
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• v.36 no.3
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• pp.291-297
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• 2012

Ginsenoside (ginseng saponin), the principal component of ginseng, is responsible for the pharmacological and biological activities of ginseng. We isolated lactic acid bacteria from Kimchi using esculin agar, to produce ${\beta}$-glucosidase. We focused on the bio-transformation of ginsenoside. Phylogenetic analysis was performed by comparing the 16S rRNA sequences. We identified the strain as Lactobacillus (strain 6105). In order to determine the optimal conditions for enzyme activity, the crude enzyme was incubated with 1 mM ginsenoside Rb1 to catalyse the reaction. A carbon substrate, such as cellobiose, lactose, and sucrose, resulted in the highest yields of ${\beta}$-glucosidase activity. Biotransformations of ginsenoside Rb1 were analyzed using TLC and HPLC. Our results confirmed that the microbial enzyme of strain 6105 significantly transformed ginsenoside as follows: Rb1${\rightarrow}$gypenoside XVII, Rd${\rightarrow}$F2 into compound K. Our results indicate that this is the best possible way to obtain specific ginsenosides using microbial enzymes from 6105 culture.

• Archives of Pharmacal Research
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• v.29 no.2
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• pp.145-151
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• 2006

We investigated the effects of Ginsenoside $R_e$ on human sperm motility in fertile and asthenozoospermic infertile individuals in vitro and the mechanism by which the Ginsenosides play their roles. The semen samples were obtained from 10 fertile volunteers and 10 asthenozoospermic infertile patients. Spermatozoa were separated by Percoll and incubated with 0, 1, 10 or $100\;{\mu}M$ of Ginsenoside $R_e$. Total sperm motility and progressive motility were measured by computer-aided sperm analyzer (CASA). Nitric oxide synthase (NOS) activity was determined by the $^{3}H$-arginine to $^{3}H$-citrulline conversion assay, and the NOS protein was examined by the Western blot analysis. The production of sperm nitric oxide (NO) was detected using the Griess reaction. The results showed that Ginsenoside $R_e$ significantly enhanced both fertile and infertile sperm motility, NOS activity and NO production in a concentration-dependent manner. Sodium nitroprusside (SNP, 100 nM), a NO donor, mimicked the effects of Ginsenoside $R_e$. And pretreatment with a NOS inhibitor $N^{w}$-Nitro-L-arginine methyl ester (L-NAME, $100\;{\mu}M$) or a NO scavenger N-Acetyl-L-cysteine (LNAC, 1 mM) completely blocked the effects of Ginsenoside $R_e$. Data suggested that Ginsenoside $R_e$ is beneficial to sperm motility, and that induction of NOS to increase NO production may be involved in this benefit.

• Applied Biological Chemistry
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• v.23 no.4
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• pp.199-205
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• 1980

Relatively large quantity of the major components of saponin, $ginsenoside-Rb_1,\;-Rb_2,\;-Rc,\;-Rd,\;-Re\;and\;-Rg_1$ from Panax ginseng C.A. Meyer were isolated using preparative and semipreparative high performance liquid chromatography, and analyzed by analytical HPLC. The application of HPLC for isolation of ginsenosides was not only very effective for rapid analysis but also reduced the isolation time. The isolation capacity of pure ginsenosides was $30{\sim}50mg/hr$.

• Journal of Ginseng Research
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• v.43 no.1
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• pp.10-19
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• 2019

Background: Frequent overdose of paracetamol (APAP) has become the major cause of acute liver injury. The present study was designed to evaluate the potential protective effects of ginsenoside Rk1 on APAP-induced hepatotoxicity and investigate the underlying mechanisms for the first time. Methods: Mice were treated with Rk1 (10 mg/kg or 20 mg/kg) by oral gavage once per d for 7 d. On the 7th d, allmice treated with 250mg/kg APAP exhibited severeliverinjury after 24 h, and hepatotoxicitywas assessed. Results: Our results showed that pretreatment with Rk1 significantly decreased the levels of serum alanine aminotransferase, aspartate aminotransferase, tumor necrosis factor, and interleukin-$1{\beta}$ compared with the APAP group. Meanwhile, hepatic antioxidants, including superoxide dismutase and glutathione, were elevated compared with the APAP group. In contrast, a significant decrease in levels of the lipid peroxidation product malondialdehyde was observed in the ginsenoside Rk1-treated group compared with the APAP group. These effects were associated with a significant increase of cytochrome P450 E1 and 4-hydroxynonenal levels in liver tissues. Moreover, ginsenoside Rk1 supplementation suppressed activation of apoptotic pathways by increasing Bcl-2 and decreasing Bax protein expression levels, which was shown using western blotting analysis. Histopathological observation also revealed that ginsenoside Rk1 pretreatment significantly reversed APAP-induced necrosis and inflammatory infiltration in liver tissues. Biological indicators of nitrative stress, such as 3-nitrotyrosine, were also inhibited after pretreatment with Rk1 compared with the APAP group. Conclusion: The results clearly suggest that the underlying molecular mechanisms in the hepatoprotection of ginsenoside Rk1 in APAP-induced hepatotoxicity may be due to its antioxidation, antiapoptosis, anti-inflammation, and antinitrative effects.

• Journal of Convergence Korean Medicine
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• v.2 no.1
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• pp.5-12
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• 2021

Objectives: The purpose of this study is to fabricate an ultra-fine ginsenoside particle atomizer that can provide a new treatment method by delivering ginsenoside components that have a therapeutic effect on respiratory diseases directly to the lungs. Methods: We fabricated the AAO vibrating mesh by using the micromachining process. The starting substrate of an AAO wafer has a 350nm pore diameter with 50㎛ thickness. A photomask having several 5㎛ opening holes with a 100㎛ pitch was used to separate each nanopore nozzle. The photoresist structure was optimized to pattern the nozzle area during the lift-off process precisely. The commercial vibrating mesh was removed from OMRON's NE-U100 product, and the fabricated AAO vibrating mesh was installed. A diluted sample of 20mL with 30% red ginseng concentrate was prepared to atomize from the device. Results: As a result of liquid chromatography analysis before spraying the ginsenoside solution, ginsenoside components such as 20S-Rg3, 20R-Rg3, and Rg5 were detected. After spraying through the AAO vibrating mesh, ginsenosides of the same component could be detected. Conclusion: A nutrient solution containing ginsenosides was successfully sprayed through the AAO vibrating mesh with 350 nm selective pores. In particular, during the atomizing experiment of ginsenoside drug solution having excellent efficacy in respiratory diseases, it was confirmed that atomizing through the AAO vibrating mesh while maintaining most of the active ingredients was carried out.