• Journal of Ginseng Research
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• 제41권3호
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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.

• 대한한의학방제학회지
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• 제30권3호
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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.

• 대한약침학회지
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• 제13권2호
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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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.

• 대한약침학회지
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• 제11권2호
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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.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 1999년도 The 6th International Symposium on the Development of Anti-Cancer Resource from Plants
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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.

• 한국자원식물학회지
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• 제19권1호
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• pp.139-143
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• 2006

고기능성 홍삼사포닌성분의 함량을 증대시키기 위한 목적으로 홍삼엑스에 열처리, 산(acid)처리하여 그 가능성을 조사하였다. 산도를 조정하지 않은 무처리구(control, pH 4.4)에 $120^{\circ}C$ 열처리한 경우 ginsenoside-$Rg_3$의 함량이 약 2배 정도 증가였다. 구연산으로 pH 2.0으로 조정하고 온도처리한 처리구에서는 2.8배나 많은 ginsenoside-$Rg_3$ 성분이 증가하였으나 다른 유효한 사포닌의 파괴가 두드러져 처음 홍삼엑스에 함유되어 있던 총사포닌의 65% 정도가 소실되었다. $80^{\circ}C$에서 12시간 처리를 한 경우에는 pH를 2.5와 2.0로 조정한 처리구에서는 11.20 mg과 12.50 mg으로 홍삼엑스의 3.3 mg보다 3.3배 이상 ginsenoside-$Rg_3$ 성분이 변환되었다. Ginsenoside-$Rb_1,\;Rb_2$, Rc, Re, $Rg_1$의 함량이 산도가 높아짐에 따라서 급격히 소실되었고 홍삼 특이성분(ginsenoside-$Rg_3,\;Rh_2,\;Rh_1$)의 함량은 현저히 증가되었다. 매실엑스로 pH를 2.5로 조정한 처리구에서는 13.34 mg으로 홍삼엑스의 3.3 mg보다 4배 이상 변환된 것으로 분석되었다. 비록 31%정도의 total saponin의 감소가 있었으나 $120^{\circ}C$의 고온처리에서 처럼 다른 유효한 사포닌의 큰 손실 없이 $60^{\circ}C$에 12시간 처리하는 것만으로도 다량의 ginsenoside-$Rg_3$를 생산하는 것을 확인하였다.

• 한국식품영양과학회지
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• 제39권8호
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• pp.1194-1200
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• 2010

본 연구에서는 인삼잎이 인삼뿌리보다 사포닌 함량이 높은 부위로서 식품 소재로 이용가치가 있을 것으로 생각되어 인삼잎을 이용하여 차 제품을 개발하기 위한 방안으로 인삼잎을 발효시켜 진세노사이드 조성 및 형태별 페놀산 조성의 변화를 분석하고 인삼잎을 침출시켜 침출액에 대한 전자공여능과 tyrosinase 저해활성을 측정하였다. 인삼잎에서 진세노사이드는 10종이 검출되었고 주된 진세노사이드는 ginsenoside-Rg1(26.0 mg/g), -Re(47.3 mg/g) 및 -Rd(23.9mg/g)이었고 발효에 의하여 ginsenoside-Rh2, -Rh1, -Rg2 및 -Rg3는 증가하였으며 특히 Rg3는 15배가 증가하였다. 인삼잎의 총 폴리페놀성 함량은 350.4 mg%이었고 발효인삼잎은 312.5 mg%으로 발효에 의해서는 약간 감소하였다. 인삼잎의 페놀산은 결합형은 검출되지 않았고, 유리형과 에스테르형이 각각 8 및 6종이 검출되었으며 그중에서 ferulic acid가 각각 12.6 및 50.7 mg%로 가장 많은 함량을 차지하고 있었다. 발효인삼잎에서는 ferulic acid는 상당량이 감소하였으나 protocatechuic acid, p-hydroxybenzoic acid, vanillic acid의 3종의 페놀산이 유리형, 에스테르형 및 결합형 모두에서 상당량 증가하여 총 함량이 각각 28배, 5배 및 7.8배 증가하였다. 인삼잎을 침출시킨 액을 이용하여 전자공여능과 tyrosinase 저해활성을 측정한 결과 전자공여능은 발효에 의하여 활성이 증가하지는 않았으나, tyrosinase 저해활성은 증가하여 $500\;{\mu}L/mL$ 농도로 첨가 시 46.5%를 나타내어 무발효인삼잎에 비하여 2배 이상 증가하여 시판녹차와 비슷한 결과를 보여주었다.

• 동의생리병리학회지
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• 제22권6호
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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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• 제40권4호
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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.