• Journal of Ginseng Research
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• 제21권3호
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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.

• Journal of Ginseng Research
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• 제37권4호
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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.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2002년도 학술대회지
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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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.

• Journal of Ginseng Research
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• 제37권2호
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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.

• Journal of Ginseng Research
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• 제45권2호
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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.

• 한국식품과학회지
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• 제41권1호
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• pp.77-81
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• 2009

Streptozotocin-유도 당뇨병 모델을 이용하여 흑삼의 혈당강하작용에 대한 효과를 연구하고 증포과정에 따른 ginsenoside의 조성 변화를 분석하였다. 증포별 ginsenoside의 정량분석 결과, 증포 횟수가 증가할수록 조사포닌의 총량과 대부분의 ginsenoside는 줄어든 반면 ginsenoside-$Rg_3$ 함량 및 PD/PT 비율은 증가하는 경향을 보였는데, 이러한 조성은 다른 인삼제품과는 차별성 있는 특징이다. 또한, streptozotocin-당뇨병 유발쥐를 이용한 모델실험에서 흑삼추출물의 투여는 고혈당 준위(300 mg/dL이상)를 정상 수준(102 mg/dL)으로 감소시켰으며, 혈당 수준의 감소는 glycolysis나 HMT shunt 및 지방산 합성에 관여하는 glucokinase, glucose-6-phosphate dehydrogenase, 6-phosphogluconate dehydrogenase, acetyl CoA carboxylase 등의 효소의 활성증대에 기인하는 것으로 판단되었다. 이러한 결과는 흑삼추출물의 유의적인 혈당강하 효과를 입증하며 이에 따라 신약이나 식이보조제의 항당뇨물질로서의 이용가능성을 시사한다.

• 한국약용작물학회지
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• 제21권5호
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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.

• 한국식품과학회지
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• 제14권3호
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• pp.197-202
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• 1982

인삼제품제조용(人蔘製品製造用)엑기스의 숙성중(熟成中)에 일어나는 ginsenosides의 분해(分解)에 미치는 온도(溫度)의 영향(影響)을 구명(究明)하기 위하여 숙성온도(熟成溫度) 및 시간(時間)에 따른 ginsenosides의 함량변화(含量變化)로써 분해속도상수(分解速度常數) 및 반감기(牛減期)를 구(求)하였고 분해속도상수(分解速度常數)와 온도(溫度)에 대(對)한 Arrhenius plot에 의하여 활성화(活性化)에너지 및 $Q_{10}$ value를 구(求)하여 ginsenosides의 분해속도상수(分解速度常數)의 온도의존성(溫度依存性)에 대(對)한 관계식(關係式)을 설정(設定)하였다. 가. ginsenosides의 분해반응(分解反應)은 1차반응(次反應)을 나타냈으며 분해시(分解時)의 반감기(半減期)가 $100^{\circ}C$에서 34시간(時間), $90^{\circ}C$에서 70시간(時間), $80^{\circ}C$에서는 131시간(時間)이므로 ginsenosides의 함량변화(含量變化)만을 고려(考慮)한다면 $80^{\circ}C$이하(以下)의$70^{\circ}C$ 부근에서 숙성(熟成)함이 바람직하다. 나. 숙성중(熟成中)에 ginsenoside-Re가 감소(減少)하는 대신 $ginsenoside-Rg_2$가 증가(增加)하고 $ginsenoside-Rg_1$이 감소(減少)하는 대신 $ginsenoside-Rh_1$이 증가(增加)하므로 ginsenosides의 상호변환관계(相互變換關係)가 인정(認定)되었다. 다. ginsenosides의 분해시(分解時)의 온도상화(速度常數)가 $80^{\circ}C$에서 $5.30{\times}10^{-3}\;hr^{-1}$, $90^{\circ}C$에서 $9.90{\times}10^{-3}\;hr^{-1}$, 100"C에서는 $20.50{\times}10^{-3}\;hr^{-1}$으로서 숙성온도(熟成溫度)가 $10^{\circ}C$높아질 때마다 분해속도상수(分解速度常數)가 약(約) 2배(培) 증가(增加)하였고 또 $Q_{10}$ value도 $2.01{\sim}3.49$로서 숙성온도(熟成溫度)가 높아질수록 ginsenosides는 상대적(相對的)으로 불안정(不安定)하였다. 라. ginsenosides분해시(分解時)의 활성화(活性化)에너지 ($E_a$)는 $16.8{\sim}30.1$ kcal/mole의 범위 안에 있으며 ginsenoside-Re 및 $-Rg_1$이 $ginsenoside-Rb_1,\;-Rb_2$, -Rc 및 -Rd 보다 훨씬 높으므로 troil saponin이 diol saponin보다 온도(溫度)의 영향(影響)을 더 많이 받고 있었다. 마. total ginsenosides의 분해반응시(分解反應時)의 활성화(活性化)에너지($E_a$)는 17.7kcal/mole이었고 분해속도상수(分解速度常數)의 온도의존성(溫度依存性)은 $k=4.574{\times}10^8{\exp}(-8898.8/T)$의 관계식(關係式)으로 표시(表示)할 수 있다

• Food Science and Biotechnology
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• 제18권2호
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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.