• BMB Reports
• /
• 제56권10호
• /
• pp.551-556
• /
• 2023

Ginsenosides, among the most active components of ginseng, exhibit several therapeutic effects against cancer, diabetes, and other metabolic diseases. However, the molecular mechanism underlying the anti-osteoporotic activity of ginsenoside Rg2, a major ginsenoside, has not been clearly elucidated. This study aimed to determine the effects of ginsenoside Rg2 on receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast formation. Results indicate that ginsenoside Rg2 inhibits RANKL-induced osteoclast differentiation of bone marrow macrophages (BMMs) without cytotoxicity. Pretreatment with ginsenoside Rg2 significantly reduced the RANKL-induced gene expression of c-fos and nuclear factor of activated T-cells (Nfatc1), as well as osteoclast-specific markers tartrate-resistant acid phosphatase (TRAP, Acp5) and osteoclast-associated receptor (Oscar). Moreover, RANKL-induced phosphorylation of mitogen-activated protein kinases (MAPKs) was decreased by ginsenoside Rg2 in BMM. Therefore, we suggest that ginsenoside Rg2 suppresses RANKL-induced osteoclast differentiation through the regulation of MAPK signaling-mediated osteoclast markers and could be developed as a therapeutic drug for the prevention and treatment of osteoporosis.

• Journal of Ginseng Research
• /
• 제40권3호
• /
• pp.300-303
• /
• 2016

The result of USRG-12 indicated that ultrasonication-processed ($100^{\circ}C$, 12 h) red ginseng extracts had the highest amount of ginsenosides Rg3 (0.803%), Rg5 (0.167%), and Rk1 (0.175%).

• Archives of Pharmacal Research
• /
• 제27권1호
• /
• pp.61-67
• /
• 2004

When ginseng water extract was incubated at $60^{\circ}C$ in acidic conditions, its protopanaxadiol ginsenosides were transformed to ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$. However, protopanaxadiol glycoside ginsenosides $Rb_1, Rb_2$ and Rc isolated from ginseng were mostly not transformed to ginsenoside $Rg_3$ by the incubation in neutral condition. The transformation of these ginsenosides to ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$ was increased by increasing incubation temperature and time in acidic condition: the optimal incubation time and temperature for this transformation was 5 h and $60^{\circ}C$ resepectively. The transformed ginsenoside $Rg_3$ and ${\Delta}^{20}$-ginsenoside $Rg_3$ were metabolized to ginsenoside $Rh_2$ and $\Delta^{20}$--ginsenoside $Rh_2$, respectively, by human fecal microflora. Among the bacteria isolated from human fecal microflora, Bacteroides sp., and Bifidobacterium sp. and Fusobacterium sp. potently transformed ginsenoside $Rg_3$ to ginsenoside $Rh_2$. Acid-treated ginseng (AG) extract, fermented AG extract, ginsenoside $Rh_2$ and protopanaxadiol showed potent cytotoxicity against tumor cell lines. AG extract, fermented AG extract and protopanaxadiol potently inhibited the growth of Helicobacter pylori.

• 생약학회지
• /
• 제45권2호
• /
• pp.107-112
• /
• 2014

The purpose of this study is to develop a new preparation process of American ginseng (Panax quinquefolium) extract featuring high concentration of ginsenoside $Rg_3$, $Rg_5$, and $Rk_1$, Red ginseng special components. Chemical transformation from ginseng saponin glycosides to prosapogenin was analyzed by the HPLC. Extracts of American ginseng were processed under several treatment conditions of microwave and vinegar (about 14% acidity). The results showed that the quantity of ginsenoside $Rg_3$ increased by over 0.9% at the 20 minutes of the pH 2~4 vinegar and microwave American ginseng ethanol extract compared with other process times. The result of MAG-20 indicates that the American ginseng microwave and vinegar-processed American ginseng extracts (about 14% acidity) treated for 20 minutes produced the highest amount of ginsenoside $Rg_3$ (0.969%), $Rg_5$ (1.071%), and $Rk_1$ (0.247%). Besides, MAG-15 indicates that the microwave - and vinegar-processed American ginseng extracts (about 14% acidity) treated for 15 minutes produced the highest amount of ginsenoside $Rg_3$ (0.772%), $Rg_5$ (1.330%), and $Rk_1$ (0.386%). This indicates that American ginseng treated with microwave and vinegar had the quantity of the ginsenoside $Rg_3$ over 32 times the amount of the ginsenoside $Rg_3$ (which was not found in raw and American ginsengs) in the average commercial Red ginseng.

• 생약학회지
• /
• 제45권1호
• /
• pp.77-83
• /
• 2014

The purpose of this study is to develop a new preparation process of ginseng extracts having high concentrations of ginsenoside $Rg_3$, $Rg_5$ and $Rk_1$, a special component of Red ginseng. Chemical transformation from ginseng saponin glycosides to prosapogenin was analyzed by the HPLC. Extracts of White ginseng (Panax ginseng) and Fine White ginseng were processed under several treatment conditions including microwave and vinegar (about 14% acidity) treatments. Results of those treatments showed that the quantity of ginsenoside $Rg_3$ increased by over 0.6% at 4 minutes of pH 2~4 vinegar and microwave treatments. The results of processing with MWG-4 indicate that the Microwave and vinegar processed white ginseng extracts (about 14% acidity) that had gone through 4-minute treatments were found to contain the largest amount of ginsenoside $Rg_3$ (0.626%), $Rg_5$ (0.514%) and $Rk_1$ (0.220%). Results of treatments with MFWG-5 showed that the Fine White ginseng extracts that had been processed with microwave and vinegar (about 14% acidity) for 5 minutes were found to contain the largest amount of ginsenoside $Rg_3$ (4.484%), $Rg_5$ (3.192%) and $Rk_1$ (1.684%). It is thought that such results provide basic information in preparing White ginseng and Fine White ginseng extracts with functionality enhanced.

• 산업식품공학
• /
• 제14권2호
• /
• pp.159-165
• /
• 2010

팽화홍삼으로부터 용매추출, 용매분획 및 silica gel column chromatography를 반복하여 두 개의 화합물을 분리하였다. 이들 두 화합물의 결정특성, 녹는점, 비선광도, Infrared spectrum 분석 결과, TLC에서의 Rf값, HPLC에서의 retention time 및 NMR 데이터를 측정하여 고찰한 결과 두 개의 화합물은 20(S)-ginsenoside Rg3와 ginsenoside Rg5임을 확인할 수 있었다. 특히 $^{1}H$- 및 $^{13}C$-NMR 데이터를 HSQC 및 HMBC와 같은 2D-NMR 실험을 통하여 더욱 정확하게 동정하였다.

• Journal of Ginseng Research
• /
• 제44권3호
• /
• pp.490-495
• /
• 2020

Background: Ginsenoside Rk1, a saponin component isolated from heat-processed Panax ginseng Meyer, has been implicated in the regulation of antitumor and anti-inflammatory activities. Although our previous studies have demonstrated that ginsenoside Rg3 significantly attenuated the activation of NMDA receptors (NMDARs) in hippocampal neurons, the effects of ginsenosides Rg5 and Rk1, which are derived from heat-mediated dehydration of ginsenoside Rg3, on neuronal NMDARs have not yet been elucidated. Methods: We examined the regulation of NMDARs by ginsenosides Rg5 and Rk1 in cultured rat hippocampal neurons using fura-2-based calcium imaging and whole-cell patch-clamp recordings. Results: The results from our investigation showed that ginsenosides Rg3 and Rg5 inhibited NMDARs with similar potencies. However, ginsenoside Rk1 inhibited NMDARs most effectively among the five compounds (Rg3, Rg5, Rk1, Rg5/Rk1 mixture, and protopanaxadiol) tested in cultured hippocampal neurons. Its inhibition is independent of the NMDA- and glycine-binding sites, and its action seems to involve in an interaction with the polyamine-binding site of the NMDAR channel complex. Conclusion: Taken together, our results suggest that ginsenoside Rk1 might be a novel component contributable to the development of ginseng-based therapeutic treatments for neurodegenerative diseases.

• 한국식품과학회지
• /
• 제50권3호
• /
• pp.349-355
• /
• 2018

본 연구에서는 상처치유(wound healing)와 같은 허혈성 심뇌혈관 질환의 잠재적 치료제로서 산양삼 추출물과 진세노사이드 Rg5의 가능성을 인간 제대정맥 내피세포인 HUVEC에서 확인하고자 하였다. 그 결과, 산양삼 추출물과 Rg5는 10-100 nM의 저농도에서 혈관신생 과정에서 발생하는 세포의 증식이나 이동, 관 형성과정을 유의적으로 증진시켰으며, 그 증가현상은 산양삼 추출물과 Rg5가 유사한 수준으로 발생하였다. 따라서 Rg5를 이용하여 혈관신생 과정에 관여하는 신호전달 메커니즘을 확인한 결과, Akt/eNOS와 ERK1/2의 인산화는 양성대조군으로 사용한 VEGF와 유사한 수준으로 증가되는 것을 확인하였다. 마지막으로 혈관 신생 유도인자이며 양성대조군인 VEGF의 혈관염증 관련 부작용이 Rg5의 혈관신생 효과에도 작용하는지 확인하기 위하여 혈관염증 관련 단백질인 ICAM-1과 VCAM-1의 발현량을 확인한 결과, ICAM-1과VCAM-1의 발현이 양성대조군인 VEGF에서는 유의적으로 증가하였으나 Rg5를 처리한 경우에는 일반 대조군과 유사한 수준으로 낮게 나타났다. 따라서 본 연구는 산양삼 추출물과 Rg5가 혈관신생 유도효과가 있으며, 이러한 현상은 Akt/eNOS와 ERK 관련 신호전달 메커니즘을 통해 진행되고 이러한 효과가 혈관염증은 유도하지 않는다는 것을 입증하였으며, 잠재적 치료제로서의 가능성을 확인하는 계기가 되었다.

• 한국자원식물학회지
• /
• 제19권1호
• /
• pp.139-143
• /
• 2006

고기능성 홍삼사포닌성분의 함량을 증대시키기 위한 목적으로 홍삼엑스에 열처리, 산(acid)처리하여 그 가능성을 조사하였다. 산도를 조정하지 않은 무처리구(control, pH 4.4)에 $120^{\circ}C$ 열처리한 경우 ginsenoside-$Rg_3$의 함량이 약 2배 정도 증가였다. 구연산으로 pH 2.0으로 조정하고 온도처리한 처리구에서는 2.8배나 많은 ginsenoside-$Rg_3$ 성분이 증가하였으나 다른 유효한 사포닌의 파괴가 두드러져 처음 홍삼엑스에 함유되어 있던 총사포닌의 65% 정도가 소실되었다. $80^{\circ}C$에서 12시간 처리를 한 경우에는 pH를 2.5와 2.0로 조정한 처리구에서는 11.20 mg과 12.50 mg으로 홍삼엑스의 3.3 mg보다 3.3배 이상 ginsenoside-$Rg_3$ 성분이 변환되었다. Ginsenoside-$Rb_1,\;Rb_2$, Rc, Re, $Rg_1$의 함량이 산도가 높아짐에 따라서 급격히 소실되었고 홍삼 특이성분(ginsenoside-$Rg_3,\;Rh_2,\;Rh_1$)의 함량은 현저히 증가되었다. 매실엑스로 pH를 2.5로 조정한 처리구에서는 13.34 mg으로 홍삼엑스의 3.3 mg보다 4배 이상 변환된 것으로 분석되었다. 비록 31%정도의 total saponin의 감소가 있었으나 $120^{\circ}C$의 고온처리에서 처럼 다른 유효한 사포닌의 큰 손실 없이 $60^{\circ}C$에 12시간 처리하는 것만으로도 다량의 ginsenoside-$Rg_3$를 생산하는 것을 확인하였다.

• 한국약용작물학회지
• /
• 제21권5호
• /
• pp.401-414
• /
• 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.