• Journal of Ginseng Research
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• 제42권2호
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• pp.199-207
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• 2018

Background: Ginseng is a well-known traditional Chinese medicine that has been widely used in a range of therapeutic and healthcare applications in East Asian countries. Microbial transformation is regarded as an effective and useful technology in modification of nature products for finding new chemical derivatives with potent bioactivities. In this study, three minor derivatives of ginsenoside compound K were isolated and the inducing effects in the Wingless-type MMTV integration site (Wnt) signaling pathway were also investigated. Methods: New compounds were purified from scale-up fermentation of ginsenoside Rb1 by Paecilomyces bainier sp. 229 through repeated silica gel column chromatography and high pressure liquid chromatography. Their structures were determined based on spectral data and X-ray diffraction. The inductive activities of these compounds on the Wnt signaling pathway were conducted on MC3T3-E1 cells by quantitative real-time polymerase chain reaction analysis. Results: The structures of a known 3-keto derivative and two new dehydrogenated metabolites were elucidated. The crystal structure of the 3-keto derivative was reported for the first time and its conformation was compared with that of ginsenoside compound K. The inductive effects of these compounds on osteogenic differentiation by activating the Wnt/b-catenin signaling pathway were explained for the first time. Conclusion: This study may provide a new insight into the metabolic pathway of ginsenoside by microbial transformation. In addition, the results might provide a reasonable explanation for the activity of ginseng in treating osteoporosis and supply good monomer ginsenoside resources for nutraceutical or pharmaceutical development.

• Journal of Ginseng Research
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• 제30권2호
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• pp.70-77
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• 2006

Ginseng has an anti-cancer effect in several cancer models. As a mechanism study of ginsenoside-induced growth inhibition in cancer cells, we measured change of membrane potential in prostate cancer and glioma cells by ginsenosides, active constituents of ginseng. Membrane potential was estimated by measuring fluorescence change of DiBAC-Ioaded cells. Among 11 ginsenosides tested, ginsenosides $Rb_2$, $Rg_3$, and $Rh_2$ increased significantly and robustly the membrane potential in a concentration-dependent manner in prostate cancer and glioma cells. Ginsenosides Rc, Ro, and $Rb_1$ slightly increased membrane potential. The ginsenoside-induced membrane potential increase was not affected by treatment with pertussis toxin or U73122. The ginsenoside-induced membrane potential increase was not diminished in $Na^+$-free or $HCO_3^-$-free media. Furthermore, the ginsenoside-induced increase of membrane potential was not changed by EIPA (5-(N-ethyl-N-isopropyl)-amiloride), SITS (4-acetoamido-4'-isothiocyanostilbene-2,2'-disulfonic acid), and omeprazole. In summary, ginsenosides $Rb_2$, $Rg_3$, and $Rh_2$ increased membrane potential in prostate cancer and glioma cells in a GPCR-independent and $Na^+$ independent manner.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1980년도 학술대회지
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• pp.181-185
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• 1980

• 한국약용작물학회지
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• 제26권2호
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• pp.148-156
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• 2018

Background: Hot steaming is known to be effective in improving the biological activities of plant extracts by breaking down useful compounds to low molecular weight ones. Methods and Results: This study aimed to develop an optimal extraction and steam processing method for enhancing the low molecular ginsenoside contents of the adventitious roots culture of wild mountain ginseng. The total ginsenoside was optimally extracted when 70% EtOH was used at $50^{\circ}C$, whereas low molecule ginsenoside such as Rg2, Rh1, Rh4 and Rk1 could be extracted using 70% EtOH at $70^{\circ}C$. The adventitious roots culture of wild mountain ginseng is known to contain four major ginsenosides, i.e., Rb2, Rb1, Rg1 and Rd, however new ginsenosides Rg6, Rh4, Rg3, Rk1 and Rg5 were new abundantly obtaind after steam processing method was applied. The contents of total ginsenosides were the highest when thermal steam processing was conducted at $120^{\circ}C$ for 120 min. Unlike ginsenosides such as Rg1, Re, Rb1, Rc, Rb2, and Rh1, which decreased after steam processing, Rg3, Rk1, and Rg5 increased after thermal processing. Steam processing significanltly reduced the content of Rb1, increased that of Rg6 by about ten times than that in the adventitious roots culture of wild mountain ginseng. Conclusions: Our study showed that the optimal extraction and steam processing method increased the content of total ginsenosides and allowed the extraction of minor ginsenosides from major ones.

• 한국작물학회지
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• 제31권3호
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• pp.286-292
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• 1986

Saponin생합성의 개체발생학적 정보를 얻기 위하여 인삼종자의 개갑과정과 묘삼생육초기에 saponin및 유리당의 변화를 HPLC로 조사하있다. 개갑처리 40일 후에 약 80%의 saponin이 없어졌으며 Rc, Rb$_2$, Rb$_1$이 없어지고 PD가 더 많이 없어졌다. 70일 후에는 40일 후보다 증가하였으며 Rg$_2$와 Rg$_3$(추정), 20-gluco Rf(추정)의 증가는 분해용탈 외에 생합성 가능성을 배제하지 아니하였다. F$_3$(추정)는 과육에 없고 미숙배유와 배에 있고 개갑과정에서 적어졌다. Rg$_3$는 과육에 없고 배유와 배에 흔적으로 있으나 개갑에서 증가되었다. 20-gluco Rf는 개갑 중 배유와 배에서만 나타났다. 4월 20일의 묘삼근에서 saponin은 없었으나 줄기에서는 개갑시 보다 많았다. 근의 saponin 생성은 5월 29일에 나타났으나 6월 30일에야 Rc, Rb$_2$, Rb$_1$이 처음 생기며 본 궤도에 이르는 것 같다. 6월 중 단위 생중당 saponin 생합성 속도는 뿌리보다 잎에서 배가 높았다. 잎사포닌 F$_3$와 F$_{6}$가 뿌리에서 발견되고, 근 saponin Rg$_3$와 20-gluco-Rf가 엽에서 나타났으나 점점 감소하였다. Saponin함량의 변화에는 PD가 주역이여서 PT/PD는 saponin 함량과 부상관을 보였다. 재갑처리 70일에도 sucrose의 함량이 높았으나 glucose는 흔적, fructose는 없었다. 묘삼의 잎은 sucrose보다 glucose와 fructose가 초기에는 많았으나 후에는 상당히 적어졌다. 줄기는 glu-cose가 많고 기타는 흔적 정도 였으며 뿌리는 초기에 sucrose가 종자에서 보다 높았으나 그 후 모든 당이 거의 흔적뿐이었다.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1978년도 학술대회지
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• pp.55-66
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• 1978

Five ginsenosides $(A_1,\;A_2,\;B_1,\;B_2,\;C)$ and a yellow pigment were isolated from American ginseng stems and leaves. Ginsenoside $A_2,\;B_1,\;B_2$ and C were proven to be identical with Korean ginseng root ginsenoside $Rg_1,$ Rd, Re and $Rb_2,$ respectively. The yellow pigment proved identical with panasenoside isolated from Korean ginseng leaves. Ginsenoside $A_1$, which was also present in American ginseng roots, was not identical to any of the known root (ginsenoside $R_{0}-Rg_{2}$) and leaf (ginsenoside $F_{1}-F_{3}$) Korean ginseng saponins. A gas-liquid chromatographic method was developed to analyze ginsenosides and sapogenins in rabbit plasma and urine samples. Panasenoside and stigmasterol were found to be the best internal standards for ginsenosides and sapogenihs, respectively. Ginsenoside C had a significantly longer half-life, higher plasma protein binding, lower metabolic and renal clearance than ginsenoside $A_1,\;A_2\;and\;B_2$. Ginsenosides were not found in rabbit plasma and urine samples after oral administration. Ginsenoside C had a higher toxicity than ginsenoside $A_2$ after intraperitoneal administration to mice. Toxicity was not observed after oral administration of the ginsenosides.

• BMB Reports
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• 제28권4호
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• pp.301-305
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• 1995

Considering the stimulatory effects of ginsenosides from Panax ginseng C. A. Meyer on the release of nitric oxide from bovine aortic endothelial cells in vitro and vasodilatation of rabbit pulmonary artery in vivo, the present study is designed to investigate the mechanism of nitric oxide release by ginsenosides in calf pulmonary artery endothelial cells, Nitric oxide release was determined in endothelial cells treated with ginsenosides and compared with those of the receptor-dependent agonists, bradykinin and ADP and the receptor-independent calcium ionophore $A_{23187}$. The results showed that total saponin and ginsenoside $Rg_1$, not $Rb_1$, stimulated nitric oxide release measured as conversion to L-citrulline. The nitric oxide releasing properties of total saponin and ginsenoside $Rg_1$ were different; total saponin stimulated only conversion to L-citrulline, like $A_{23187}$, while ginsenoside $Rg_1$ stimulated both L-arginine transport and conversion to L-citrulline, as bradykinin or ADP did.

• 생약학회지
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• 제48권1호
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• pp.82-87
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• 2017

Malonyl ginsenoside content of the Panax ginseng C.A. Meyer is known to account for 35% to 60% of total ginsenosides content. However, its distribution by ginseng part has not been studied. In this study, four kinds of malonyl ginsenosides were compared in Korean white ginseng part using the purified malonyl ginsenoside standards in our laboratory. White ginseng was prepared by the freeze drying ($-70^{\circ}C$, 48 h) or air drying ($50^{\circ}C$, 48 h) methods form 4-year-old ginseng. Malonyl ginsenoside content of main, lateral, and fine root, and of the main root without skin and its skin was compared. Malonyl ginsenosides (m-Rb1, m-Rb2, m-Rc and m-Rd) content (58%, 19.17 mg/g) in total ginsenosides of air dried white ginseng was decreased about 4% compared to its content of freeze dried white ginseng (62%, 20.40 mg/g). Malonyl ginsenoside content was the highest in fine root, compared to the main or lateral root. Malonyl ginsenosides content in skin of main root was 20.08 mg/g, while its content of the main root without skin was 2.58 mg/g. These results are expected to help establishment of quality specification and processing process in Korean white ginseng.

• Journal of Ginseng Research
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• 제40권4호
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• pp.344-350
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• 2016

Background: Mountain-cultivated ginseng (MCG) and cultivated ginseng (CG) both belong to Panax ginseng and have similar ingredients. However, their pharmacological activities are different due to their significantly different growth environments. Methods: An ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS)-based approach was developed to distinguish MCG and CG. Multivariate statistical methods, such as principal component analysis and supervised orthogonal partial-least-squares discrimination analysis were used to select the influential components. Results: Under optimized UPLC-QTOF-MS/MS conditions, 40 ginsenosides in both MCG and CG were unambiguously identified and tentatively assigned. The results showed that the characteristic components of CG and MCG included ginsenoside Ra3/isomer, gypenoside XVII, quinquenoside R1, ginsenoside Ra7, notoginsenoside Fe, ginsenoside Ra2, ginsenoside Rs6/Rs7, malonyl ginsenoside Rc, malonyl ginsenoside Rb1, malonyl ginsenoside Rb2, palmitoleic acid, and ethyl linoleate. The malony ginsenosides are abundant in CG, but higher levels of the minor ginsenosides were detected in MCG. Conclusion: This is the first time that the differences between CG and MCG have been observed systematically at the chemical level. Our results suggested that using the identified characteristic components as chemical markers to identify different ginseng products is effective and viable.

• Journal of Ginseng Research
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• 제38권1호
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• pp.22-27
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• 2014

Background: Research has been conducted with regard to the development of methods for improving the pharmaceutical effect of ginseng by conversion of ginsenosides, which are the major active components of ginseng, via high temperature or high-pressure processing. Methods: The present study sought to investigate the anticancer effect of heat-processed American ginseng (HAG) in human gastric cancer AGS cells with a focus on assessing the role of apoptosis as an important mechanistic element in its anticancer actions. Results and Conclusion: HAG significantly reduced the cancer cell proliferation, and the contents of ginsenosides Rb1 and Re were markedly decreased, whereas the peaks of less-polar ginsenosides [20(S,R)-Rg3, Rk1, and Rg5] were newly detected. Based on the activity-guided fractionation of HAG, ginsenoside 20(S)-Rg3 played a key role in inducing apoptosis in human gastric cancer AGS cells, and it was generated mainly from ginsenoside Rb1. Ginsenoside 20(S)-Rg3 induced apoptosis through activation of caspase-3, caspase-8, and caspase-9, as well as regulation of Bcl-2 and Bax expression. Taken together, these findings suggest that heat-processing serves as an increase in the antitumor activity of American ginseng in AGS cells, and ginsenoside 20(S)-Rg3, the active component produced by heat-processing, induces the activation of caspase-3, caspase-8, and caspase-9, which contributes to the apoptotic cell death.