• Title/Summary/Keyword: Ginsenoside Rh2(S)

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Identification of Nuclear Receptors by RT-PCR in F9 Cells Induced by Ginsenosides

  • Youl-Nam Lee;Shi
    • Journal of Ginseng Research
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    • v.21 no.3
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    • pp.147-152
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    • 1997
  • Ginsenosides $Rh_1$ and $Rh_2$ Induced the differentiation of F9 teratocarcinoma stem cells. These agents are structurally similar to the steroid hormones, therefore, we speculated that the steroid receptor (s) or novel nuclear receptor (s) could be involved in the differentiation process induces by them. Based on this speculation, we tried to alone new nuclear receptors with reverse transcription-polymerase chain reaction (RT-PCR) method by isolating RNA from F9 teratocarcinoma cells induced by ginsenosides. By using RT-PCR with degenerated primers from highly conserved DNA binding domain of nuclear receptors, we identified several nuclear receptors. In northern blot analysis we found that these clones are transcriptionally regulated by ginsenoside Rhl or Rh2 treatment. Further characterizations of these clones are needed to identify the mechanism of gene expression, which has an important role in the differentiation of F9 cells induced by ginsenosides.

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A new validated analytical method for the quality control of red ginseng products

  • Kim, Il-Woung;Cha, Kyu-Min;Wee, Jae Joon;Ye, Michael B.;Kim, Si-Kwan
    • Journal of Ginseng Research
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    • v.37 no.4
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    • pp.475-482
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    • 2013
  • The main active components of Panax ginseng are ginsenosides. Ginsenoside Rb1 and Rg1 are accepted as marker substances for quality control worldwide. The analytical methods currently used to detect these two compounds unfairly penalize steamed and dried (red) P. ginseng preparations, because it has a lower content of those ginsenosides than white ginseng. To manufacture red ginseng products from fresh ginseng, the ginseng roots are exposed to high temperatures for many hours. This heating process converts the naturally occurring ginsenoside Rb1 and Rg1 into artifact ginsenosides such as ginsenoside Rg3, Rg5, Rh1, and Rh2, among others. This study highlights the absurdity of the current analytical practice by investigating the time-dependent changes in the crude saponin and the major natural and artifact ginsenosides contents during simmering. The results lead us to recommend (20S)- and (20R)-ginsenoside Rg3 as new reference materials to complement the current P. ginseng preparation reference materials ginsenoside Rb1 and Rg1. An attempt has also been made to establish validated qualitative and quantitative analytical procedures for these four compounds that meet International Conference of Harmonization (ICH) guidelines for specificity, linearity, range, accuracy, precision, detection limit, quantitation limit, robustness and system suitability. Based on these results, we suggest a validated analytical procedure which conforms to ICH guidelines and equally values the contents of ginsenosides in white and red ginseng preparations.

A Structure-Function Relationship Exists for Ginsenosides in Reducing Cell Proliferation and Inducing Apoptosis in THP-1 Cells

  • Popovich David G.;Kitts David D.
    • Proceedings of the Ginseng society Conference
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    • 2002.10a
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    • pp.545-555
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    • 2002
  • Ginsenosides of 20(S)-protopanaxadiol and 20(S)-protopanaxatriol classification including the aglycones, PD, PI and ginsenosides Rh2, Rhl were shown to posses characteristic effects on proliferation of THP-l human leukaemia cells. A similar result was not apparent for ginsenoside Rg3 or dexamathasone. The concentration to inhibit $50\%$ of cells $(LC_{50})$ for PD, Rh2, PI and Rhl were 13 ${\mu}g/mL,\;15{\mu}g/mL,\;19{\mu}g/mL\;and\;210\;{\mu}g/mL$ respectively. Cell cycle analysis showed apoptosis with PD and PI treatment of THP-1 cells resulting in a build up of sub-G1 cells after 24, 48 and 72 hours of treatment. Rh2, and dexamathasone treatments also increased apoptotic cells after 24 hours, where as Rhl did not. After 48 and 72 hours Rh2, Rhl and dexamathasone similarly increased apoptosis, but these effects were significantly (P<0.05) lower than observed for both PD and PI treatments. Furthermore, treatments that produced the largest build up of apoptotic cells were also found to have the largest release of lactate dehydrogenase (LDH). It can be concluded from these studies that the presence of sugars to PD and PI aglycone structure reduces the potency to induce apoptosis, and alternately alter membrane integrity. These cytotoxic effects to THP-l cells were different from dexamethasone.

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항균성 및 항암성 배당체의 합성연구

  • 임광식
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.115-115
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    • 1993
  • i) total ginsenoside의 분리 시판백삼(900g)을 상법에 따라 처리, 조 saponin을 얻었으며 (24g) 이를 20(S)-protopanaxadiol을 얻는 원료로 사용하였다. ii) 20(S)-protopanaxadiol의 분리연구 본 연구에서 가장 중요한 단계는 20(S)-protopanaxadiol을 다량 얻는 것이다. 그러나 인삼 saponin을 산으로 가수분해하면 진성 aglycone 인 20(S)-protopanaxadiol이 얻어지지 않고 artifact sapogenol인 panaxadiol이 얻어진다. 이를 해결하기 위하여 sodium ethoxide의 ethanol 용액, sodium butoxide의 butanol 용액, sodium methoxide의 pyridine 용액, sodium methoxide의 DMSO 용액등의 조건에서의 가수분해를 검토한 결과 aprotic polar splvent인 DMSO용매중에서의 분해가 가장 좋음을 알았다. iii) ginsenoside Rh$_2$의 합성연구 Koenigs-Knorr 법에 의하여 bromosugar와 20(S)-protopanaxadiol의 glycosidation 반응결과 약 40%의 수득률로 합성됨을 확인하였다.

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The effect of extrusion conditions on the acidic polysaccharide, ginsenoside contents and antioxidant properties of extruded Korean red ginseng

  • Gui, Ying;Ryu, Gi Hyung
    • Journal of Ginseng Research
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    • v.37 no.2
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    • pp.219-226
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    • 2013
  • This study was conducted to investigate the effect of extrusion conditions (moisture content 20% and 30%, screw speed 200 and 250 rpm, barrel temperature $115^{\circ}C$ and $130^{\circ}C$) on the acidic polysaccharide, ginsenoside contents and antioxidant properties of extruded Korean red ginseng (KRG). Extruded KRGs showed relatively higher amounts of acidic polysaccharide (6.80% to 9.34%) than non-extruded KRG (4.34%). Increased barrel temperature and screw speed significantly increased the content of acidic polysaccharide. The major ginsenosides (Rb1, Rb2, Rc, Rd, Re, Rf, Rg2s, Rg3s, Rh1, and Rg3r) of KRG increased through extrusion, while the ginsenoside (Rg1) decreased. The EX8 (moisture 30%, screw speed 250 rpm, and temperature $130^{\circ}C$) had more total phenolics and had a better scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals than those of extruded KRG samples. The extrusion cooking showed a significant increase (6.8% to 20.9%) in reducing power. Increased barrel temperature significantly increased the values of reducing power, the highest value was 1.152 obtained from EX4 (feed moisture 20%, screw speed 250 rpm, and temperature $130^{\circ}C$). These results suggest that extrusion conditions can be optimized to retain the health promoting compounds in KRG products.

20(S)-ginsenoside Rh2 induces caspase-dependent promyelocytic leukemia-retinoic acid receptor A degradation in NB4 cells via Akt/Bax/caspase9 and TNF-α/caspase8 signaling cascades

  • Zhu, Sirui;Liu, Xiaoli;Xue, Mei;Li, Yu;Cai, Danhong;Wang, Shijun;Zhang, Liang
    • Journal of Ginseng Research
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    • v.45 no.2
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    • pp.295-304
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    • 2021
  • Background: Acute promyelocytic leukemia (APL) is a hematopoietic malignancy driven by promyelocytic leukemia-retinoic acid receptor A (PML-RARA) fusion gene. The therapeutic drugs currently used to treat APL have adverse effects. 20(S)-ginsenoside Rh2 (GRh2) is an anticancer medicine with high effectiveness and low toxicity. However, the underlying anticancer mechanisms of GRh2-induced PML-RARA degradation and apoptosis in human APL cell line (NB4 cells) remain unclear. Methods: Apoptosis-related indicators and PML-RARA expression were determined to investigate the effect of GRh2 on NB4 cells. Z-VAD-FMK, LY294002, and C 87, as inhibitors of caspase, and the phosphatidylinositol 3-kinase (PI3K) and tumor necrosis factor-α (TNF-α) pathways were used to clarify the relationship between GRh2-induced apoptosis and PML-RARA degradation. Results: GRh2 dose- and time-dependently decreased NB4 cell viability. GRh2-induced apoptosis, cell cycle arrest, and caspase3, caspase8, and caspase9 activation in NB4 cells after a 12-hour treatment. GRh2-induced apoptosis in NB4 cells was accompanied by massive production of reactive oxygen species, mitochondrial damage and upregulated Bax/Bcl-2 expression. GRh2 also induced PML/PML-RARA degradation, PML nuclear bodies formation, and activation of the downstream p53 pathway in NB4 cells. Z-VAD-FMK inhibited caspase activation and significantly reversed GRh2-induced apoptosis and PML-RARA degradation. GRh2 also upregulated TNF-α expression and inhibited Akt phosphorylation. LY294002, an inhibitor of the PI3K pathway, enhanced the antitumor effects of GRh2, and C 87, an inhibitor of the TNF-α pathway, reversed NB4 cell viability, and GRh2-mediated apoptosis in a caspase-8-dependent manner. Conclusion: GRh2 induced caspase-dependent PML-RARA degradation and apoptosis in NB4 cells via the Akt/Bax/caspase9 and TNF-α/caspase8 pathways.

Effects of Black Ginseng (9 Times-Steaming Ginseng) on Hypoglycemic Action and Changes in the Composition of Ginsenosides on the Steaming Process (흑삼(구증구포인삼)이 혈당 강하에 미치는 영향 및 증포별 ginsenoside 조성 변화)

  • Kim, Suong-Nuen;Kang, Shin-Jyung
    • Korean Journal of Food Science and Technology
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    • v.41 no.1
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    • pp.77-81
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    • 2009
  • This study examined the effects of black ginseng (9 times-steamed ginseng) on hypoglycemic action in streptozotocininduced diabetic rats as well as changes in ginsenoside composition by the steaming process. As the number of steaming cycles increased, the amounts of crude saponin and most ginsenoside contents decreased, while the amount of ginsenoside- Rg3 and the ratio of PD/PT (=[$Rb_1+Rb_2+Rc+Rd+Rg_3]/[Re+Rb_1+Rh_1]$) increased. This ginsenoside composition is a unique characteristic compared to other types of ginseng products. In order to investigate the hypoglycemic effect of the black ginseng extract, in vivo studies were performed in rats with streptozotocin-induced diabetes. The studies showed that the administration of the black ginseng extract decreased high blood glucose levels (more than 300 mg/dL) to a normal level (102 mg/dL). These results suggest that this black ginseng extract has a significant hypoglycemic effect and can be used as an anti-diabetic substance for dietary supplements or new drugs.

Transformation Techniques for the Large Scale Production of Ginsenoside Rg3 (Ginsenoside Rg3의 함량증가를 위한 변환 기술)

  • Nam, Ki Yeul;Choi, Jae Eul;Park, Jong Dae
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.5
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    • pp.401-414
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    • 2013
  • Ginsenoside Rg3 (G-Rg3) contained only in red ginseng has been found to show various pharmacological effects such as an anticancer, antiangiogenetic, antimetastastic, liver protective, neuroprotective immunomodulating, vasorelaxative, antidiabetic, insulin secretion promoting and antioxidant activities. It is well known that G-Rg3 could be divided into 20(R)-Rg3 and 20(S)-Rg3 according to the hydroxyl group attached to C-20 of aglycone, whose structural characteristics show different pharmacological activities. It has been reported that G-Rg3 is metabolized to G-Rh2 and protopanaxadiol by the conditions of the gastric acid or intestinal bacteria, thereby these metabolites could be absorbed, suggesting its absolute bioavailability (2.63%) to be very low. Therefore, we reviewed the chemical, physical and biological transformation methods for the production on a large scale of G-Rg3 with various pharmacological effects. We also examined the influence of acid and heat treatment-induced potentials on for the preparation method of higher G-Rg3 content in ginseng and ginseng products. Futhermore, the microbial and enzymatic bio-conversion technologies could be more efficient in terms of high selectivity, efficiency and productivity. The present review discusses the available technologies for G-Rg3 production on a large scale using chemical and biological transformation.

Kinetic Studies on the Thermal Degradation of Ginsenosides in Ginseng Extract (Ginsenosides의 처리온도(處理溫度) 및 시간(時閭)에 따른 반응속도론적(反應速度論的) 연구(硏究))

  • Choi, Jin-Ho;Kim, Doo-Ha;Sung, Hyun-Soon;Kim, Woo-Jung;Oh, Sung-Ki
    • Korean Journal of Food Science and Technology
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    • v.14 no.3
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    • pp.197-202
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    • 1982
  • Kinetic study for the thermal degradation of ginsenosides in ginseng extract was conducted. The results indicate that the thermal degradation followed first order kinetics and rate constants varied substantially depending on the types of ginsenosides and heat treatment temperatures. Activation energy calculated by Arrhenius plots ranged from 16.80 kcal/mole to 30.10 kcal/mole and $Q_{10}$ values ranged from 2.01 to 3.49. Correlation coefficients between the change of ginsenoside contents by thermal degradation and heat treatment temperature were $0.995{\sim}0.999$. The dependence on temperatures of the decomposition rate constant of total ginsenoside can be expressed as $k=4.574{\times}10^8$ exp(8898.8/T).

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Antioxidant and Antimicrobial Activities of Various Solvent Fractions of Fine Ginseng Root

  • Lim, Jae-Kag;Kang, Ho-Jin;Kang, Suk-Nam;Lee, Boo-Yong
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.513-518
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    • 2009
  • This study was carried out to investigate the changes of yield, total phenolics, saponin content and composition, antimicrobial, and antioxidant activities of various fractions of fine ginseng root (Panax ginseng C.A. Mayer) by maceration method in the order of increasing polarity (hexane, chloroform, ethyl acetate, butanol, and water). Butanol fraction showed the highest total saponin content compare to other fractions. Hexane fraction could harvest significantly high ginsenoside Rg2, Rg1, and Rf (p<0.05). And the contents of ginsenoside Rh1, Rg3, and Rg1 showed relatively higher in the fraction of ethyl acetate than other fractions. The system of hexane-chloroform-ethyl aceate-butanol showed relatively high content of ginsenoside Re, Rd, Rc, Rb3, and Rb1. However, the last fraction of water still remained lots of Rb2 content. The fraction of water was the highest phenolics. The 1,1-diphenyl-2-picryhydrazil, superoxide, and hydroxyl radical scavenging activity of water fraction was higher than the other fractions. In antimicrobial activity, the fraction of hexane showed relatively high antimicrobial activity against Pseudomonas aeruginosa, Salmonella typhimurium, Staphylococcus aureus, Bacillus cereus, and Escherichia coli. And the fractions of the chloroform and ethyl acetate showed higher antimicrobial activities than the other samples in against P. aeruginosa and S. typhimurium.