• Asian Pacific Journal of Cancer Prevention
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• 제15권3호
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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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• 제44권10호
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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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• 제14권3호
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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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• 제44권2호
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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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• 제23권5호
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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.

• 한국식품영양과학회지
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• 제39권11호
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• pp.1660-1665
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• 2010

홍삼 파우치 제품의 성분 및 제조방법의 표준화를 위한 일환으로 국내 유통 중인 홍삼 파우치의 사포닌 함량 및 이화학적 특성을 분석하였다. 총 ginsenoside 함량은 5.5~185.7 mg/100 mL의 함량을 나타내었고 항암효과로 알려진 ginsenoside $Rg_3$, $Rg_2$, $Rh_1$과 $Rh_2$의 함량 분포는 $Rg_3$는 1.6~46.3 mg/100 mL, $Rg_2$는 미검출~22.0 mg/100 mL, $Rh_1$은 미검출~4.3 mg/100 mL, $Rh_2$는 미검출~20.4 mg/100 mL의 분포를 나타내었다. 항 당뇨 효과가 있는 ginsenoside $Rb_2$와 Re의 함량분포는 $Rb_2$는 미검출~10.8 mg/100 mL, Re는 미검출~7.0 mg/100 mL의 함량을 나타내었으며 그 밖의 사포닌 중 ginsenoside $Rb_1$는 미검출~25.2 mg/100 mL, Rc는 미검출~12.5 mg/100 mL, Rd는 미검출~11.3 mg/100 mL, Rf는 미검출~5.9 mg/100 mL, $Rg_1$는 미검출~4.4 mg/100 mL까지의 함량 분포를 보였다. 이화학적 특성 분석결과 총당함량은 226.6~3,102.9 mg/100 mL, 당도는 $1.4\sim9.5^{\circ}Bx$, 탁도는 82.2~100.0%, pH는 4.1~5.0의 범위를 나타내었다. 국내에서 수집한 홍삼 파우치 제품의 약 50%(21~24개 제품)가 ginsenoside $Rb_1$, $Rb_2$, Rc, Rd, Re, $Rg_1$이 미검출 되었으며, 각 제품별 사포닌 함량 차이가 매우 크게 나타나, 국내유통 중인 홍삼 제품에 대한 기준 설정 및 생산방법의 표준화가 필요할 것으로 사료된다.

• 농업생명과학연구
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• 제44권3호
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• pp.61-67
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• 2010

국산 재배삼 4년근의 뿌리, 장뇌삼 4년근과 8년근의 잎과 뿌리에 대한 물 및 80% 에탄올 추출물에 대한 구성사포닌 및 항산화 활성을 분석하였다. 재배삼 80% 에탄올 추출물에 대한 조사포닌 함량은 3.85% (d.b) 이었으며, 4년근 장뇌삼 뿌리와 잎의 조사포닌 함량은 각각 6.75 및 8.57% (d.b)이었으며, 8년근 장뇌삼은 각각 6.53 및 7.54% (d.b)이었다. 재배삼의 구성사포닌은 ginsenoside-$Rh_1$의 함량이 6.07 mg/g으로 가장 높았고, 4년근 장뇌삼뿌리는 $-Rb_1$이 11.63 mg/g, 잎은 -Re가 24.35 mg/g으로 가장 높았고 8년근 장뇌삼 뿌리는 $-Rh_1$ 이 19.77 mg/g, 잎은 -Re가 20.43 mg/g으로 가장 높았다. 항산화활성 ($IC_{50}$값)은 삼의 종류 및 연근별로 1.84~21.88 mg/mL의 범위이었고 8년근 장뇌삼 잎 80% 에탄올 추출물에서 가장 높았다. 총 항산화력은 5.56~20.67 mg AA eq/g의 범위를 나타내었으며, 8년근 장뇌삼 잎 증류수 추출물에서 가장 높은 값을 나타내었다.

• 한국식품과학회지
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• 제44권4호
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• pp.411-416
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• 2012

본 연구에서는 인삼의 수용성 물질의 추출 수율을 높이고 압출 온도가 ginsenoside 및 당의 변화에 미치는 영향을 조사하기 위하여 압출온도를 달리하여 제조한 압출성형 백삼의 추출수율과 성분의 변화를 조사하였다. 인삼의 증류수 추출 수율은 압출성형 백삼이 가장 높았으며 백삼이 가장 낮았다. 압출 성형백삼의 경우는 압출 온도가 높을수록 추출 수율이 증가하였다. 또한 증류수 추출시 80% 에탄올 추출시보다 추출수율이 증가하였다. 조사포닌 함량은 압출 성형 백삼이 가장 높았으며 이는 압출 온도가 증가함에 따라 조사포닌 함량도 증가하였다. 11종의 총 ginsenoside함량은 홍삼이 가장 높았다. 백삼에서는 Re의 함량이 가장 높았고, 홍삼에서는 Rg1, Rg3, Rb2가 가장 높았다. 압출성형 백삼에서는 Rg2, Rh1 및 Rh2의 함량이 증가되었다. 인삼의 유리당 함량은 홍삼이 가장 높았으며 압출 성형 인삼이 가장 낮았다. 인삼의 명도(L)값은 백삼이 가장 높았으며 압출 성형백삼이 가장 낮았다. 적색도(a)와 황색도(b) 값은 압출성형 백삼이 가장 높았다. 이상의 실험에서 압출 성형 백삼은 정수로 추출 시 추출 수율이 백삼에 비해 25%이상 높았고, 조사포닌 함량도 약 20% 높았다. 또한 Rg2, Rh1, Rh2, Rg3의 ginsenoside 함량이 백삼에 비해 월등히 높았다. 이는 압출 성형 백삼을 이용하여 제품 개발 시 높은 추출 수율, 사포닌 함량이 높은 제품을 만들 수 있을 가능성을 보여 주는 결과라 생각된다.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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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.

• 약학회지
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• 제60권2호
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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.