• Journal of Ginseng Research
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• v.41 no.3
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• pp.330-338
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• 2017

Background: Ginsenoside Rh2 (G-Rh2) is a ginseng saponin that is widely investigated because of its remarkable antitumor activity. However, the molecular mechanism by which (20S) G-Rh2 triggers its functions and how target animals avoid its cytotoxic action remains largely unknown. Methods: Phage display was used to screen the human targets of (20S) G-Rh2. Fluorescence spectroscopy and UV-visible absorption spectroscopy were used to confirm the interaction of candidate target proteins and (20S) G-Rh2. Molecular docking was utilized to calculate the estimated free energy of binding and to structurally visualize their interactions. MTT assay and immunoblotting were used to assess whether human serum albumin (HSA), bovine serum albumin (BSA), and bovine serum can reduce the cytotoxic activity of (20S) G-Rh2 in HepG2 cells. Results: In phage display, (20S) G-Rh2-beads and (20R) G-Rh2-beads were combined with numerous kinds of phages, and a total of 111 different human complementary DNAs (cDNA) were identified, including HSA which had the highest rate. The binding constant and number of binding site in the interaction between (20S)-Rh2 and HSA were $3.5{\times}10^5M^{-1}$ and 1, and those in the interaction between (20S) G-Rh2 and BSA were $1.4{\times}10^5M^{-1}$ and 1. The quenching mechanism is static quenching. HSA, BSA and bovine serum significantly reduced the proapoptotic effect of (20S) G-Rh2. Conclusion: HSA and BSA interact with (20S) G-Rh2. Serum inhibited the activity of (20S) G-Rh2 mainly due to the interaction between (20S) G-Rh2 and serum albumin (SA). This study proposes that HSA may enhance (20S) G-Rh2 water solubility, and thus might be used as nanoparticles in the (20S) G-Rh2 delivery process.

• Herbal Formula Science
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• v.30 no.3
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• pp.175-182
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• 2022

Objective : This study aims to investigate the active ingredients and potential mechanisms of the beneficial herb on human cancers such as the liver by employing network pharmacology. Methods : Ingredients and their target information was obtained from various databases such as TM-MC, TTD, and Drugbank. Related protein for liver cancer was retrieved from the Comparative Toxicogenomics Database and literature. A hypergeometric test and gene set enrichment analysis were conducted to evaluate associations between protein targets of red ginseng (Panax ginseng C. A. Meyer) and liver cancer-related proteins and identify related signaling pathways, respectively. Network proximity was employed to identify active ingredients of red ginseng on liver cancer. Results : A compound-target network of red ginseng was constructed, which consisted of 363 edges between 53 ingredients and 121 protein targets. MAPK signaling pathway, PI3K-Akt signaling pathway, p53 signaling pathway, TGF-beta signaling pathway, and cell cycle pathway was significantly associated with protein targets of red ginseng. Network proximity results indicated that Ginsenoside Rg1, Acetic Acid, Ginsenoside Rh2, 20(R)-Ginsenoside Rg3, Notoginsenoside R1, Ginsenoside Rk1, 2-Methylfuran, Hexanal, Ginsenoside Rd, Ginsenoside Rh1 could be active ingredients of red ginseng against liver cancer. Conclusion : This study suggests that network-based approaches could be useful to explore potential mechanisms and active ingredients of red ginseng for liver cancer.

• Journal of Pharmacopuncture
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• v.13 no.2
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• pp.33-49
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• 2010

Objectives: The aim of this experiment is to provide an objective differentiation of cultivated ginseng, mountain ginseng through component analysis, and to know the change of gin senoside components in the process of heating and fermentation Methods: Comparative analyses of ginsenoside $Rb_1$, $Rb_2$, Rc, Rd, Re, Rf, $Rg_1$, $Rg_3$, $Rh_1$, and $Rh_2$, from the cultivated ginseng 4 and 6 years, and mountain cultivated ginseng were conducted using HPLC (High Performance Liquid Chromatography, hereafter HPLC). And the same analyses were conducted in the process of heating and fermentation using mixed Lactobacillus rhamnosus, Lactobacillus plantarum, Bifidobacterium lactis for 7 days. Results: The change of ginsenosides to the process of red ginseng and fermentation, cultivated ginseng and mountain cultivated ginseng were showed another results. Mountain ginseng showed a lot of change compared with cultivated ginsengs. In the 7 days of fermentation, mountain ginseng showed that ginsenoside $Rg_1$, $Rb_1$, $Rb_2$, Rc, and Rd were decreased and increased ginsenoside Re, Rf, $Rg_3$ and $Rh_1$ were increased compared with cultivated ginseng Conclusions: It seemed that ginsenosides of mountain cultivated ginseng was better resolved than cultivated ginseng because the difference of structure or distribution of ginsenosides in the condition of fermentation.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.213-213
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• 1994

배풍등, 등혹 및 ginsenoside Rh$_1$의 간암세포에 대한 세포독성작용, 인삼 Rh$_1$의 세포보호작용, 비파의 ursolic acid 생체방어기전 활성화 및 산화억제작용, ononin의 radical 제거능을 검토하였다. 그 결과 배풍등 CHCl$_3$분획 및 등혹 CHCl$_3$분획의 간암세포에 대한 강한 세포독성작용을 나타내었으며 배풍등 CHCl$_3$은 sarcoma 180 이식 종양조직의 성장을 유의성있게 억제하였다. Ursolic acid는 지질과산화, 단백질 산화억제와 catalase, GSH S-transferase를 활성화시켰다. 인삼 saponin은 SOD 및 nonprotein-SH를 증가시키고, 지질과산화를 억제시켰다. Ginsenoside Rh$_1$ 및 Rh$_2$는 각각 radical에 대한 세포보호작용과 간암세포 세포독작용을 나타내었다.

• Journal of Pharmacopuncture
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• v.11 no.2
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• pp.87-95
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• 2008

Objectives The aim of this experiment is to provide an differentiation of ginseng, red ginseng, cultivated wild ginseng(CWG), and red wild ginseng(RWG) through component analysis using HPLC(High Performance Liquid Chromatography, hereafter HPLC). Methods Comparative analyses of ginsenoside $Rg_3$, ginsenoside $Rh_2$, and ginsenosides $Rb_1$ and $Rg_1$ of various ginsengs were conducted using HPLC. Results 1. CWG was relatively heat-resistant and showed slow change in color during the process of steaming and drying, compared to cultivated ginseng. 2. Ginsenoside $Rg_3$ was not detected in cultivated ginseng and CWG, whereas it was high in red ginseng and RWG. Ginsenoside $Rg_3$ was more generated in red ginseng than in RWG. 3. Ginsenoside $Rh_2$ appreared during steaming and drying of cultivated ginseng, whereas it was more increased during steaming and drying of CWG. 4. Ginsenoside $Rg_1$ content was more increased during steaming and drying of cultivated ginseng, whereas it was more decreased during steaming and drying of CWG. 5. Ginsenoside $Rb_1$ content was increased about 500% during steaming and drying of cultivated ginseng, whereas it was increased about 30% during steaming and drying of CWG, indicating that ginsenoside $Rb_1$ was more generated in red ginseng than in RWG. 6. Ginsenoside $Rg_3$ content was higher, whereas ginsenoside $Rg_1$ content was lower in 11th RWG than in 9th RWG, indicating that ginsenoside $Rg_3$ content was increased and $Rg_1$ content was decreased as steaming and drying continued to proceed. Ginsenoside $Rh_2$ and $Rb_1$ contents began to be increased, followed by decreased after 9th steaming and drying process. Conclusions Above experiment data can be an important indicator for the dentification of ginseng, red ginseng, CWG, and RWG. And the following studies will be need for making good product using CWG.

• Proceedings of the Plant Resources Society of Korea Conference
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• 1999.10a
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• pp.46-57
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• 1999

Ginseng(Panax ginseng C.A. Meyer) is important medicinal plant but requires 4-year cultivation for root harvest because of slow growth. In contrast, ginseng callus and hairy roots grow vigorously and may Produce the same or more biologically active compounds for human health than natural ginseng roots. Therefore, ginseng callus and hairy roots can be used for commercial purposes. Polyacetylene, one of anti-cancer compounds in ginseng, was not detected in the callus cultured on the medium containing 2, 4-B, but cells derived from the callus growth was excellent, The ginseng calli cultured on the medium containing 2mg11 CPA and 0.05mg/1 BA was grown vigorously and produced panaxydol, one of ginseng polyacetylene. The biosynthesis of polyacetylene in callus was not affected by addition of NAA and sucrose in media. The SH medium was better than the MS medium for ginseng callus growth and biosynthesis of panaxydol. Another ginseng anti-cancer compounds, ginsenoside-Rg$_3$, Rh$_1$and Rh$_2$ were detected in ginseng hairy roots by heat treatment. Those of Panax ginseng were obtained after root disks of three-year old roots were infected with Agrobacterium rhizogenes Rl000 $A_4$T in dark condition after one month of culture. The optimum growth of hairy roots was achieved in the culture of 1/2 MS liquid medium in dark(22$^{\circ}C$) under 60 rpm gyratory shaking. Hairy roots grew well in 5 ι Erlenmeyer flasks, 1ι roller drums, 10ι jar-fermenters, and especially in 20ι air-lift .culture vessels. All heat treatments had remarkably different ginsenoside contents. Eleven ginsenosides were determined in heat treatment, eight in freeze dried hairy roots. Contents of ginsenoside-Rbl , Rb2, Rc, Rd. Re, Rf, and Rg$_1$tested in all heat treatments were less than those of freeze dried hairy roots. Contents of glnsenoside-Rg$_2$ in heat treatment for 1 hour at 105$^{\circ}C$ was 4.92mg/g dry wt, 3.9 times higher than 1.27 mg/g dry wt of freeze dried hairy roots. The optimum condition of heat treatment for the production of ginsenoside-Rg$_3$and Rhl was 2 hours at 105$^{\circ}C$, and ginsenoside content was 2.58mg/g dry wt and 3.62mg/g dry wt, respectively. The production of ginsenoside-Rh2 was the highest in heat treatment for 2 hours at 105$^{\circ}C$ among treatments examined, and ginsenoside-Rh$_2$content was 1.08mg/g dry wt.

• Korean Journal of Plant Resources
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• v.19 no.1
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• pp.139-143
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• 2006

To increase the contents of functional ginsenosides by conversion, especially ginsenoside-$Rg_3$ and $Rh_2$, the extracts of red ginseng were treated with high temperature and citric acid or apricot extract. When the extracts were subject to $120^{\circ}C$ for 2 hours, the content of ginsenoside-$Rg_3$ was increased 2 times than in control. When the extracts were subject to $120^{\circ}C$ and acidic conditions adjusted with citric acid, the ginsenoside-$Rg_3$, was detected 2.8 times, but other ginsenoside were decreased heavily to 65%. When the extract were treated with for 12 hours at $80^{\circ}C$, the content of ginsenoside-$Rg_3$ was increased to 3.3 times, Also, when the red ginseng extracts were treated with apricot extract, the ginsenoside-$Rg_3$ was detected to 4 times than in control, but other ginsenoside were decreased lightly to 35%, not same as at the $120^{\circ}C$ treatment.

• Journal of the Korean Society of Food Science and Nutrition
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• v.39 no.8
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• pp.1194-1200
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• 2010

This study was carried out to investigate the compositional changes of ginsenosides and phenolic acids of ginseng leaf by fermentation in order to promote the utilization of ginseng leaf. The chief ginsenosides in non-fermented ginseng leaf (NFGL) were ginsenoside-Rg1 (26.0 mg/g), -Re (47.3 mg/g) and -Rd (23.9 mg/g). By fermentation, ginsenoside-Rg1, -Rb1, -Rb2, -Rb3, -Rc and -Re were decreased tremendously and new ginsenoside-Rh2, -Rh1, -Rg2 and -Rg3 appeared. Especially, ginsenoside-Rg3 (3.7 mg/g) on FGL was increased 15-fold compared to that of NFGL (0.2 mg/g). Total phenolic compound content of NFGL and FGL measured by colorimetric analysis was 350.4 and 312.5 mg%, respectively. There were 8 free and 6 ester forms of phenolic acids in NFGL. Among them, content of ferulic acid was the highest, comprised of 12.6 and 50.7 mg%, respectively. In FGL, total content of protocatechuic acid, p-hydroxybenzoic acid, and vanillic acid were increased by 28, 5 and 7.8 fold and ferulic acid was decreased greatly. Tyrosinase inhibitory activity of FGL was stronger than NFGL, while electron donating abilities of FGL were similar to NFGL.

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.6
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• pp.1557-1561
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• 2008

Red ginseng possibly has new ingredients converted during steaming and dry process from fresh ginseng. Kujeungkupo method which means 9 repetitive steamings and dryings process was used for the production of red ginseng from 6-year old ginseng roots. Saponin was extracted from each red ginseng produced at the 1st, 3rd, 5th, 7th, and 9th during the steaming and drying treatment, and we analyzed saponin content with TLC. Minor saponins, such as ginsenoside-Rg3, -Rh2, compound K, and F2, increased as the process time of steaming and drying, but major saponins (ginsenoside-Rb1, -Rb2, -Rc, -Rd, -Re, -Rf, -Rg1) were decreased. Major saponins were yet observed almost at the 1st process, then degraded as the increasing time of steaming and drying process. Especially, ginsenoside-Re and -Rg were observed as considerable amount after the 1st treatment, but there were no trace of them after the 9th treatment. Ginsenoside-Rg1, -Rb2, and -Rb1 were also reduced remarkedly by 96.6%, 96%, and 92.3%, respectively. Minor saponins were increased significantly, especially for ginsenoside-Rg3 and ginsenoside-F2. These results suggest that Kujeungkupo method is the very useful method for the production of minor ginsenoside-Rg3 and -Rh2.

• Journal of Ginseng Research
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• v.40 no.4
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• pp.366-374
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• 2016

Background: In this study, we screened and identified an endophyte JG09 having strong biocatalytic activity for ginsenosides from Platycodon grandiflorum, converted ginseng total saponins and ginsenoside monomers, determined the source of minor ginsenosides and the transformation pathways, and calculated the maximum production of minor ginsenosides for the conversion of ginsenoside Rb1 to assess the transformation activity of endophyte JG09. Methods: The transformation of ginseng total saponins and ginsenoside monomers Rb1, Rb2, Rc, Rd, Rg1 into minor ginsenosides F2, C-K and Rh1 using endophyte JG09 isolated by an organizational separation method and Esculin-R2A agar assay, as well as the identification of transformed products via TLC and HPLC, were evaluated. Endophyte JG09 was identified through DNA sequencing and phylogenetic analysis. Results: A total of 32 ${\beta}$-glucosidase-producing endophytes were screened out among the isolated 69 endophytes from P. grandiflorum. An endophyte bacteria JG09 identified as Luteibacter sp. effectively converted protopanaxadiol-type ginsenosides Rb1, Rb2, Rc, Rd into minor ginsenosides F2 and C-K, and converted protopanaxatriol-type ginsenoside Rg1 into minor ginsenoside Rh1. The transformation pathways of major ginsenosides by endophyte JG09 were as follows: $Rb1{\rightarrow}Rd{\rightarrow}F2{\rightarrow}C-K$; $Rb2{\rightarrow}C-O{\rightarrow}C-Y{\rightarrow}C-K$; $Rc{\rightarrow}C-Mc1{\rightarrow}C-Mc{\rightarrow}C-K$; $Rg1{\rightarrow}Rh1$. The maximum production rate of ginsenosides F2 and C-K reached 94.53% and 66.34%, respectively. Conclusion: This is the first report about conversion of major ginsenosides into minor ginsenosides by fermentation with P. grandiflorum endophytes. The results of the study indicate endophyte JG09 would be a potential microbial source for obtaining minor ginsenosides.