• 고려인삼학회:학술대회논문집
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• 고려인삼학회 2004년도 추계 학술대회 및 정기총회
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• pp.7-11
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• 2004

We previously reported that ginseng inhibited NMDA receptors in cultured hippocampal neurons. Here, we further examined the detailed mechanism of ginseng-mediated inhibition using its main active ingredient, ginsenoside Rg$_3$. Co-application of ginsenoside Rg$_3$ with increasing concentrations of NMDA did not change the EC$_{50}$ of NMDA to the receptor, suggesting ginsenoside Rg$_3$ inhibits NMDA receptors without competing with the NMDA-binding site. Ginsenoside Rg$_3$-mediated inhibition also occurred in a distinctive manner from the well-characterized NMDA receptor open channel blocker, MK-801, However, ginsenoside Rg$_3$ produced its effect in a glycine concentration-dependent manner and shifted the glycine concentration-response curve to the right without changing the maximal response, suggesting the role of ginsenoside Rg$_3$ as a competitive NMDA receptor antagonist. We also demonstrated that ginsenoside Rg$_3$ significantly protected neurons against NMDA insults. Therefore, these results suggest that ginsenoside Rg$_3$ protects NMDA-induced neuronal death via a competitive interaction with the glycine-binding site of NMDA receptors in cultured hippocampal neurons.

• 대한화장품학회지
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• 제49권4호
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• pp.375-383
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• 2023

최근 다양한 피부 기능 개선 효과로 기능성 소재로서 활용도가 높은 홍삼 사포닌의 한 종류인 진세노사이드 Rg3를 위한 사과산(malic acid)활용 전환 방법을 확인하였다. 실험 계획법인 반응 표면 분석법(RSM)을 활용하여 진세노사이드 Rg3로의 전환에 영향을 주는 요인을 최적화하기 위한 실험 조건을 설계 및 검증하였다. 주요 독립변수는 사과산 농도, 반응 온도와 반응 시간이었고 Box-Behnken design (BBD)법에 따라 설계된 실험 조건으로 진세노사이드 Rg3로 전환을 수행하고 최적화 조건을 분석하였다. 전환된 진세노사이드 Rg3의 농도는 1.548 mg/L에서 최대 4.558 mg/L까지 확인되었고 사과산 1%, 50℃, 9 h에서 가장 높은 양의 진세노사이드 Rg3생성량을 보였다. 결론적으로, 진세노사이드 Rg3의 생성에 가장 영향을 미치는 요인은 사과산의 농도, 반응 시간, 온도 순이었다. 또한, 사과산의 농도와 반응 시간의 교호작용이 반응 온도 요인보다 영향도가 큰 것을 확인하였다.

• 생명과학회지
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• 제24권9호
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• pp.1001-1005
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• 2014

Ginsenoside Rg3는 홍삼으로부터 추출한 활성 성분들 중 하나로 한방 의학에선 원기를 회복시키는 약제로 잘 알려져 있는 인체에 유효한 화학 성분이다. Rg3는 지금까지 많은 연구들에 의하여 다양한 암세포로부터 강력한 항암효과를 가진다고 알려져 있다. 그러나 Rg3가 악성 흑색종 세포에서 어떻게 세포사멸을 유도하는지에 대한 작용 기작은 명백하게 밝혀지지 않았다. 따라서, 본 연구에서는 ginsenoside Rg3가 B16F10 흑색종 세포에서 세포 사멸 유도 활성 및 기전에 관한 영향을 조사하였다. 세포 생존력을 MTT assay 법으로 수행한 결과, B16F10 세포에선 농도 의존적으로 세포증식 저해 효과가 나타났고 정상세포인 EA.hy.926 과 NIH3T3 에서는 나타나지 않았다. B1610 세포에 Rg3를 농도 별로 처리 후, TUNEL 염색을 한 결과 세포사멸이 농도 의존적으로 증가 하는 것을 확인 할 수 있었다. Western blot 분석을 실시한 결과, Rg3를 처리한 B16F10 세포에서 p-FAK, Bcl-2, pro-caspase3 단백질들의 발현이 감소 되었고 이와 반대로 Bax, p-p38의 발현은 증가되었다. 따라서, 본 연구에서는 Rg3가 B16F10 흑색종 세포에서 항암제의 agent로써 사용 될 수 있다는 것을 입증하였다.

• Journal of Applied Biological Chemistry
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• 제61권3호
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• pp.257-265
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• 2018

The Panax ginseng Mayer is used in conventional medicine in Asia owing to its preventing effects on thrombosis, hypertension, atherosclerosis, vasorelaxation and myocardial infarction. Because platelets are crucial mediators of cardiovascular diseases, many studies have investigated its functions. The previous study showed the antiplatelet effects of crude ginseng fraction and two of its components, ginsenoside Rg3 (20S and 20R). In addition, ginsenoside Rg3-enriched fraction shows an inhibitory effect on collagen-activated rat platelets. However, the mechanism underlying this effect remains unclear. Thus, I investigated the inhibitory action of ginsenoside Rg3 (20S, G-Rg3) on the regulation of signaling molecules involved in ${\alpha}IIb/{\beta}_3$ activation. I found that G-Rg3, in a cyclic AMP dependent manner, inhibited thrombin-induced activation of human platelets and affinity of fibrinogen and fibronectin with ${\alpha}IIb/{\beta}_3$. Thus, in the present study, G-Rg3 showed an inhibitory effect on glycoprotein IIb/IIIa (${\alpha}IIb/{\beta}_3$) activation, suggesting its potential use for preventing platelet-mediated thrombotic disease.

• 생약학회지
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• 제42권4호
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• pp.361-365
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• 2011

The objective of this study is to provide basic information for developing a high-value ginseng product using ginseng saponin and prosapogenin. In order to achieve the proposed objective ginsenoside compositions of Black (BG) and Red (RG) ginseng extract with 95% ethyl alcohol were examined by means of HPLC. The crude saponin and ginsenoside composition of processed ginseng products were analyzed and compared, with BG topping the list with a crude saponin content of 7.53%, followed by RG (5.29%). Ginseng prosapogenin (ginsenosides $Rg_2$, $Rg_3$, $Rg_5$, $Rg_6$, $Rh_1$, $Rh_4$, $Rk_1$, $Rk_3$, $F_1$ and $F_4$) in BG was found to be contained almost 2.6 times as much as that in RG. Ginsenosides $Rg_3$, $Rg_5$, $Rk_1$, $Rh_4$ and $F_4$ in BG in particular were found to be almost 3 times as much as those in RG. $Rg_6$ and $Rk_3$ in BG were also found to be almost 4 times as much as those in RG.

• Journal of Ginseng Research
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• 제45권5호
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• pp.610-616
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• 2021

Background: Thymic stromal lymphopoietin (TSLP) acts as a master switch for inflammatory responses. Ginsenoside Rg3 (Rg3) which is an active ingredient of Panax ginseng Meyer (Araliaceae) is known to possess various therapeutic effects. However, a modulatory effect of Rg3 on TSLP expression in the inflammatory responses remains poorly understood. Methods: We investigated antiinflammatory effects of Rg3 on an in vitro model using HMC-1 cells stimulated by PMA plus calcium ionophore (PMACI), as well as an in vivo model using PMA-induced mouse ear edema. TSLP and vascular endothelial growth factor (VEGF) levels were detected using enzyme-linked immunosorbent assay or real-time PCR analysis. Murine double minute 2 (MDM2) and hypoxia-inducible factor 1α (HIF1α) expression levels were detected using Western blot analysis. Results: Rg3 treatment restrained the production and mRNA expression levels of TSLP and VEGF in activated HMC-1 cells. Rg3 down-regulated the MDM2 expression level increased by PMACI stimulation. The HIF1α expression level was also reduced by Rg3 in activated HMC-1 cells. In addition, Rg3-administered mice showed the decreased redness and ear thickness in PMA-irritated ear edema. Rg3 inhibited the TSLP and VEGF levels in the serum and ear tissue homogenate. Moreover, the MDM2 and HIF1α expression levels in the ear tissue homogenate were suppressed by Rg3. Conclusion: Taken together, the current study identifies new mechanistic evidence about MDM2/HIF1α pathway in the antiinflammatory effect of Rg3, providing a new effective therapeutic strategy for the treatment of skin inflammatory diseases.

• Journal of Ginseng Research
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• 제34권3호
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• pp.246-253
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• 2010

Ginsenoside $Rg_3$ ($Rg_3$), one of the active ingredients in Panax ginseng, attenuates NMDA receptor-mediated currents in vitro and antagonizes NMDA receptors through a glycine modulatory site in rat cultured hippocampal neurons. In the present study, we examined the neuroprotective effects of $Rg_3$ on 24-hydroxycholesterol (24-OH-chol)-induced cytotoxicity in vitro. The results showed that $Rg_3$ treatment significantly and dose-dependently inhibited 24-OH-chol-induced cell death in rat cultured cortical neurons, with an $IC_{50}$ value of $28.7{\pm}7.5\;{\mu}m$. Furthermore, the $Rg_3$ treatment not only significantly reduced DNA damage, but also dose-dependently attenuated 24-OH-chol-induced caspase-3 activity. To study the mechanisms underlying the in vitro neuroprotective effects of $Rg_3$ against 25-OH-chol-induced cytotoxicity, we also examined the effect of $Rg_3$ on intracellular $Ca^{2+}$ elevations in cultured neurons and found that $Rg_3$ treatment dose-dependently inhibited increases in intracellular $Ca^{2+}$, with an $IC_{50}$ value of $40.37{\pm}12.88\;{\mu}m$. Additionally, $Rg_3$ treatment dose-dependently inhibited apoptosis with an $IC_{50}$ of $47.3{\pm}14.2\;{\mu}m$. Finally, after confirming the protective effect of $Rg_3$ using a terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling assay, we found that $Rg_3$ is an active component in ginseng-mediated neuroprotection. These results collectively indicate that $Rg_3$-induced neuroprotection against 24-OH-chol in rat cortical neurons might be achieved via inhibition of a 24-OH-chol-mediated $Ca^{2+}$ channel. This is the first report to employ cortical neurons to study the neuroprotective effects of $Rg_3$ against 24-OH-chol. In conclusion, $Rg_3$ was effective for protecting cells against 24-OH-chol-induced cytotoxicity in rat cortical neurons. This protective ability makes $Rg_3$ a promising agent in pathologies implicating neurodegeneration such as apoptosis or neuronal cell death.

• Journal of Ginseng Research
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• 제21권2호
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• pp.132-140
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• 1997

The effects of ginsenosides purified from red ginseng on platelet aggregation were investigated. Preincubation of washed platelets from rats with either ginsenoside Rg3, ginsenosides non-polar fraction (G-NPF), ginsenoside Rg1(Rg1) or ginsenosides polar fraction(G-PF) reduced the plytelet aggrelation induced by collagen in a dose-dependent manner, whereas ginsenoside Rg2 failed to inhibit the aggregation. Their IC50 values of Rg3, G-NPF, Rgl, and G-PF were 8.7$\pm$1.0, 150.3$\pm$0.1, 369.9$\pm$ 1.0, 606.211.3 $\mu\textrm{g}$/ml, respectively. Aggrelation induced by thrombin was also inhibited by Rg3 and G-NPF with IC50 being 5.2$\pm$ 1.1 and 66.5$\pm$0.8 $\mu\textrm{g}$/ml, respectively. The alterations of Intracellular Ca2+ concentration in platelets were monitored using fura-2 as a fluorescent Ca2+ indicator. Both Ca2+ release from internal stores and Ca2+ influx into cytosol were suppressed by Rg3. Rg3 also inhibited granular release of ATP and TXA2 formation induced by thrombin in a dose-dependent manner in the washed platelets. Rg3 also inhibited Aggregation and ATP release from human platelets induced by collagen to a similar extent as were observed in rat platelets. In conclusion, Rg3 is a Potent anti-aggregating component in ginsenosides and may exert its anti-aggrega1ing activity by decreasing TXAa formation and granular secretion in platelets, most likely by inhibiting Ca2+ influx and Ca2+ mobilization from intracellular stores. Thus ginseng may contribute to the prevention and treatment of thrombosis.

• Journal of Ginseng Research
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• 제48권1호
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• pp.31-39
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• 2024

Background: Ginsenoside Rg3, a primary bioactive component of red ginseng, has anti-cancer effects. However, the effects of Rg3-enriched ginseng extract (Rg3RGE) on apoptosis and autophagy in breast cancer have not yet been investigated. In the present study, we explored the anti-tumor effects of Rg3RGE on breast cancer cells stimulated CoCl₂, a mimetic of the chronic hypoxic response, and determined the operative mechanisms of action. Methods: The inhibitory mechanisms of Rg3RGE on breast cancer cells, such as apoptosis, autophagy and ROS levels, were detected both in vitro. To determine the anti-cancer effects of Rg3RGE in vivo, the cancer xenograft model was used. Results: Rg3RGE suppressed CoCl₂-induced spheroid formation and cell viability in 3D culture of breast cancer cells. Rg3RGE promoted apoptosis by increasing cleaved caspase 3 and cleaved PARP and decreasing Bcl2 under the hypoxia mimetic conditions. Further, we identified that Rg3RGE promoted apoptosis by inhibiting lysosomal degradation of autophagosome contents in CoCl₂-induced autophagy. We further identified that Rg3RGE-induced apoptotic cell death and autophagy inhibition was mediated by increased intracellular ROS levels. Similarly, in the in vivo xenograft model, Rg3RGE induced apoptosis and inhibited cell proliferation and autophagy. Conclusion: Rg3RGE-stimulated ROS production promotes apoptosis and inhibits protective autophagy under hypoxic conditions. Autophagosome accumulation is critical to the apoptotic effects of Rg3RGE. The in vivo findings also demonstrate that Rg3RGE inhibits breast cancer cell growth, suggesting that Rg3RGE has potential as potential as a putative breast cancer therapeutic.

• Journal of Ginseng Research
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• 제40권3호
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• pp.237-244
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• 2016

Background: Ginsenoside Rg3 and arginine-fructose (Arg-Fru) are known as the hypotensive compounds of Panax ginseng; however, their efficacy on antihypertension has not been reported yet to our best knowledge. Thus, hypotensive components-enriched fraction of red ginseng (HCEF-RG) was prepared from fine root concentrate (FR) and their antihypertensive effects were investigated in spontaneously hypertensive rats (SHR). Methods: Male SHRs were divided into six groups: control (Wistar Kyoto, SHR); FR 500; FR 1,000; HCEF-RG 500; and HCEF-RG 1,000; samples (mg/kg body weight) were orally administered every day for 8 wk. Blood pressure was monitored at 1 wk, 2 wk, 3 wk, 4 wk, 6 wk, and 8 wk by tail cuff method. At 8 wk after samples administration, mice were killed for the measurement of renin activity (RA), angiotensin-I converting enzyme inhibition, angiotensin II, and nitric oxide (NO) levels in plasma. Results: HCEF-RG with four-fold more Rg3 and 24-fold more Arg-Fru contents was successfully prepared from reacted mixtures of FR and persimmon vinegar (12 times against FR, v/v) at $80^{\circ}C$ for 18 h. Both FR 1,000 and HCEF-RG 1,000 showed lowered systolic blood pressure than SHR control group and HCEF-RG 1,000 group exhibited a significant decrease in diastolic blood pressure. RA was significantly lowered in all treated groups, while angiotensin II did not affect by FR and HCEF-RG treatment. However, angiotensin-I converting enzyme inhibition and NO in FR 1,000 and HCEF-RG 1,000 were significantly increased compared with SHR control group. Conclusion: HCEF-RG is more effective and useful for alleviating hypertension than FR, implying the health benefit of Rg3 and Arg-Fru.