• Asian Pacific Journal of Cancer Prevention
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• v.15 no.3
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• pp.1099-1104
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• 2014

Aims and Background: Ginsenoside Rh2, which exerts the potent anticancer action both in vitro and in vivo, is one of the most well characterized ginsenosides extracted from ginseng. Although its effects on cancer are significant, the underlying mechanisms remain unknown. In this study, we sought to elucidate possible links between ginsenoside Rh2 and phosphoglucose isomerase/autocrine motility factor (PGI/AMF). Methods: $KG1{\alpha}$, a leukemia cell line highly expressing PGI/AMF was assessed by western blot analysis and reverse transcription- PCR (RT-PCR) assay after transfection of a small interfering (si)-RNA to silence PGI/AMF. The effect of PGI/AMF on proliferation was measured by typan blue assay and antibody array. A cell counting kit (CCK)-8 and flow cytometry (FCM) were adopted to investigate the effects of Rh2 on PGI/AMF. The relationships between PGI/AMF and Rh2 associated with Akt, mTOR, Raptor, Rag were detected by western blot analysis. Results: KG1${\alpha}$ cells expressed PGI/AMF and its down-regulation significantly inhibited proliferation. The antibody array indicated that the probable mechanism was reduced expression of PARP, State1, SAPK/JNK and Erk1/2, while those of PRAS40 and p38 were up-regulated. Silencing of PGI/AMF enhanced the sensibility of $KG1{\alpha}$ to Rh2 by suppressing the expression of mTOR, Raptor and Akt. Conclusion: These results suggested that ginsenoside Rh2 suppressed the proliferation of $KG1{\alpha}$, the same as down-regulation of PGI/AMF. Down-regulation of PGI/AMF enhanced the pharmacological effects of ginsenoside Rh2 on KG1${\alpha}$ by reducing Akt/mTOR signaling.

• BMB Reports
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• v.44 no.10
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• pp.659-664
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• 2011

As part of the search for biologically active anti-osteoporotic agents that enhance differentiation and mineralization of osteoblastic MC3T3-E1 cells, we identified the ginsenoside Rh2(S), which is an active component in ginseng. Rh2(S) stimulates osteoblastic differentiation and mineralization, as manifested by the up-regulation of differentiation markers (alkaline phosphatase and osteogenic genes) and Alizarin Red staining, respectively. Rh2(S) activates p38 mitogen-activated protein kinase (MAPK) in time- and concentration-dependent manners, and Rh2(S)-induced differentiation and mineralization of osteoblastic cells were totally inhibited in the presence of the p38 MAPK inhibitor, SB203580. In addition, pretreatment with Go6976, a protein kinase D (PKD) inhibitor, significantly reversed the Rh2(S)-induced p38 MAPK activation, indicating that PKD might be an upstream kinase for p38 MAPK in MC3T3-E1 cells. Taken together, these results suggest that Rh2(S) induces the differentiation and mineralization of MC3T3-E1 cells through activation of PKD/p38 MAPK signaling pathways, and these findings provide a molecular basis for the osteogenic effect of Rh2(S).

• Preventive Nutrition and Food Science
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• v.14 no.3
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• pp.201-207
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• 2009

In an effort to improve ginsenoside bioavailability, the ginsenosides of fermented red ginseng were examined with respect to bioavailability and physiological activity. The results showed that the fermented red ginseng (FRG) had a high level of ginsenoside metabolites. The total ginsenoside contents in non-fermented red ginseng (NFRG) and FRG were 35715.2 ${\mu}g$/mL and 34822.9 ${\mu}g$/mL, respectively. However, RFG had a higher content (14914.3 ${\mu}g$/mL) of ginsenoside metabolites (Rg3, Rg5, Rk1, CK, Rh1, F2, and Rg2) compared to NFRG (5697.9 ${\mu}g$/mL). The skin permeability of RFG was higher than that of NFRG using Franz diffusion cells. Particularly, after 5 hr, the skin permeability of RFG was significantly (p<0.05) higher than that of NFRG. Using everted instestinal sacs of rats, RFG showed a high transport level (10.3 mg of polyphenols/g sac) compared to NFRG (6.67 of mg of polyphenols/g sac) after 1 hr. After oral administration of NFRG and FRG to rats, serum concentrations were determined by HPLC. Peak concentrations of Rk1, Rh1, Rc, and Rg5 were approximately 1.64, 2.35, 1.13, and 1.25-fold higher, respectively, for FRG than for NFRG. Furthermore, Rk1, Rh1, and Rg5 increased more rapidly in the blood by the oral administration of FRG versus NFRG. FRG had dramatically improved bioavailability compared to NFRG as indicated by skin permeation, intestinal permeability, and ginsenoside levels in the blood. The significantly greater bioavailability of FRG may have been due to the transformation of its ginsenosides by fermentation to more easily absorbable forms (ginsenoside metabolites).

• Journal of Ginseng Research
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• v.44 no.2
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• pp.215-221
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• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.518-524
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• 2000

We examined the modulation of protein kinase C (PKC) subtypes during apoptosis induced by ginsenoside Rh2 (G-Rh2) in human neuroblastoma SK-N-Bl(2) and rat glioma C6Bu-1 cells. Apoptosis induced by C-Rh2 in both cell lines was confirmed, as indicated by DNA fragmentation and in situ strand breaks, and characteristic morphological changes. During apoptosis induced by G-Rh2 in SK-N-BE(2) cells, PKC subtypes $\alpha$, $\beta$ and $\gamma$ were progressively increased with prolonged treatment, whereas PKC $\delta$ increased transiently at 3 and 6 h and PKC $\varepsilon$ was gradually down-regulated after 6 h following the treatment. On the other hand, PKC subtype $\beta$ markedly increased at 24 h when maximal apoptosis was achieved. In C6Bu-l cells, no significant changes in PKC subtypes $\alpha$, $\gamma$, $\delta$, $\varepsilon$ and $\beta$ were observed during apoptosis induced by G-Rh2. These results suggest the evidence for a possible role of PKC subtype in apoptosis induced by G-Rh2 in SK-N-BE(2) cells but not in C6Bu-1 cells, and raise the possibility that G-Rh2 may induce apoptosis via different pathways interacting with or without PKC in different cell types.

• Journal of the Korean Society of Food Science and Nutrition
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• v.39 no.11
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• pp.1660-1665
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• 2010

To obtain data for the standardization of manufacturing method of red ginseng extract pouch products, saponin and physico-chemical properties of 44 Korean red ginseng extract pouch products were analyzed. The concentration of total ginsenoside contents were 5.5~185.7 mg/100 mL. Distribution of the contents of ginsenoside $Rg_3$, $Rg_2$, $Rh_1$, and $Rh_2$ known to have anticancer effect are as follows: $Rg_3$ is 1.6~46.3 mg/100 mL, $Rg_2$ is 0~22.0 mg/100 mL, $Rh_1$ is 0~4.3 mg/100 mL and that of $Rh_2$ is 0~20.4 mg/100 mL, respectively. The anti-diabetic effect of ginsenoside $Rb_2$ and Re distribution of contents were 0~10.8 mg/100 mL and 0~7.0 mg/100 mL, respectively. Among the other saponins, exhibited content to distribution of ginsenoside $Rb_1$ was 0~25.2 mg/100 mL, Rc was 0~12.5 mg/100 mL, Rd was 0~11.3 mg/100 mL, Rf was 0~5.9 mg/100 mL and $Rg_1$ was 0~4.4 mg/100 mL. Results of physicochemical characterization showed total sugar content of 226.6~3,102.9 mg/100 mL, total soluble solids content $1.4\sim9.5^{\circ}Bx$, turbidity 82.2~100.0%, pH in the range of 4.1 to 5.0, respectively. In approximately 50% of collected domestic ginseng extract pouch products (21~24 items), ginsenoside $Rb_1$, $Rb_2$, Rc, Rd, Re and $Rg_1$ were not detected, and saponin content of each product appears to differ greatly. Results indicated that standardization of production methods and standards set for red ginseng extract pouch products in Korea is needed.

• Journal of agriculture & life science
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• v.44 no.3
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• pp.61-67
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• 2010

This study was conducted to investigate the antioxidant activities and ginsenoside compositions of 4-year-old cultured ginseng roots (4CGR), 4-year-old mountain ginseng roots (4MGR) and leaves (4MGL), and 8-year-old mountain ginseng roots (MGR) and leaves (8MGL). Ginseng root and leaves were extracted with water and 80% ethanol. Crude saponin content of 4CGR was 3.85% (d.b.) and the contents of 4MGR, 4MGL, 8MGR and 8MGL were 6.75, 8.57, 6.53 and 7.54% (d.b.), respectively. 4CGR showed the highest content of ginsenoside-$Rh_1$ (6.07 mg/g), 4MGR showed the highest content of ginsenoside-$Rb_1$ (11.63 mg/g), 4MGL showed the highest content of ginsenoside-Re (24.35 mg/g), 8MGR showed the highest content of ginsenoside-$Rh_1$ (19.77 mg/g), and 8MGL showed the highest content of ginsenoside-Re (20.43 mg/g). Total antioxidant activity (AEAC) was ranged from 5.56 at 4MGR to 20.67 mg AA eq/g at 8MGL.

• Korean Journal of Food Science and Technology
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• v.44 no.4
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• pp.411-416
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• 2012

This study was carried out to investigate the effects of the extrusion process on the change of components in ginseng. The extraction yields from ginseng by distilled water extraction were highest in the extruded ginsengs, whereas it was lowest in the white ginseng. The contents of crude saponin were highest in the extruded ginseng, and they increased as the extrusion temperature was raised. The total contents of 11 kinds of ginsenosides increased in the order of red, white and extruded ginsengs. In particular, red ginseng showed higher contents of Rg1, Rg3 and Rb2, whereas Re was highest in white ginseng. In addition, the contents of Rg2, Rh1, Rh2 and Rg3 in the extruded white ginseng became higher. Free sugar contents were greatest in red ginseng. However, they were lowest in the extruded ginseng. White ginseng had a greater L value, whereas extruded ginseng demonstrated higher a and b values. In conclusion, the extraction yields, the contents of saponin, and ginsenoside-Rg2, Rh1, Rh2 and Rg3 were increased through the extrusion process.

• Proceedings of the Ginseng society Conference
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• 1998.06a
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• pp.244-252
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• 1998

Ginsenoside Rh, (G-Rh,) from Panax ginseng induced morphological features of apoptosis and DNA fragmentation as a biochemical marker of apoptosis confirmed by TUNEL reaction and agarose gel electrophoresis in human neuroblastoma SK-N-BE(2) and rat glioma C6Bu-1 cells During apoptosis by G-Rh2, protein kinase C (PKC) isoforms were analysed by immunoblotting. In SK-N-BE(2) cells, the levels of a, p and ${\gamma}$ subtypes were increased by undergoing apoptosis, while PKC e isoform increased early in treatment (3 h and 6 h). In addition, PKC s isoform gradually decreased during apoptosis by G-Rh2 and PKC $\theta$ isoform was detected in neither untreated- nor G-Rh1-treated SK-N-BE(2) cells (data not shown). However, no significant changes in the level of S and s isoforms were observed in C6Bu-1 cells undergoing apoptosis by G-Rh2. These results suggest that PKC subtypes may play differential roles in apoptotic signal pathways and their roles can be cell type-specific in apoptosis induced by G-Rh2.

• YAKHAK HOEJI
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• v.60 no.2
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• pp.58-63
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• 2016

The purpose of this study is to develop a new preparation process of ginseng berry extracts having high concentrations of ginsenoside Rh1, Rg2, Rg5, F4, a special component of red and black ginseng. Chemical transformation from ginseng saponin glycosides to prosapogenin was analyzed by the HPLC. Extracts of ginseng (Panax ginseng) berry was processed under several treatment conditions including ultrasonication treatments. The content of total saponin reached their heights at 6 hr (UGB-6, 61.760%) of ultrasonication treatment, followed by 10 hr (UGB-10, 53.009%) and 9 hr (UGB-9, 50.652%) of ultrasonication treatment at $100^{\circ}C$. Results of those treatments showed that the quantity of ginsenoside Rh1 increased by over 15% at 10 hr of ultrasonication treatment at $100^{\circ}C$. The results of processing with UGB-10 indicate that the ultrasonication processed ginseng berry extracts that had gone through 10 hr treatments were found to contain the largest amount of ginsenoside Rh1 (15.358%), Rg2 (6.301%), Re (4.567%) and F4 (2.658%). In addition, UGB-6 contained ginsenoside Rg3 (13.632%) at high concentrations. It is thought that such results provide basic information in preparing ginseng berry extracts with functionality enhanced.