• Journal of Ginseng Research
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• v.32 no.3
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• pp.264-269
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• 2008

Ginsenosides are major components in Panax ginseng and known to have numerous pharmacological activities such as anti-cancer, anti-diabetes, anti-viral and anti-atherosclerosis effects. In this study, the regulatory activities of G-Rg3 and its derivative 25-hydroxy Rg3 (G-Rg3-2H) on the production of nitric oxide (NO) in macrophages and the proliferation of lymphocytes prepared from spleen and bone marrow under treatment of lipopolysaccharide (LPS) or concanavalin (Con) A were examined. G-Rg3 and G-Rg3-2H dose-dependently inhibited NO production from LPS-activated RAW264.7 cells and in agreement, these compounds protected RAW264.7 cells from LPS-mediated cytotoxicity. In contrast, G-Rg3-2H dose-dependently inhibited lymphocyte proliferation induced by both LPS and Con A, while there was no inhibition by G-Rg3. Therefore, our data suggest that these compounds may be applied for NO-mediated or lymphocyte-mediated immunological diseases.

• Journal of Ginseng Research
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• v.33 no.4
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• pp.294-304
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• 2009

Ginsenosides are among the most well-known traditional herbal medicines frequently used for the treatment of various symptoms in South Korea. The neuroprotective effects of ginsenoside $Rg_3$ (G-$Rg_3$) on cholesterol-oxide-(CO)-induced neurotoxicity were investigated through the analyses of rat brains. The recently accumulated reports show that ginseng saponins (GTS), the major active ingredients of Panax ginseng, have protective effects against neurotoxin insults. In the present study, the neuroprotective effects of G-$Rg_3$ on CO-induced hippocampal excitotoxicity were examined in vivo. The in-vitro studies using rat cultured hippocampal neurons revealed that G-$Rg_3$ treatment significantly inhibited CO-induced hippocampal cell death. G-$Rg_3$ treatment not only significantly reduced CO-induced DNA damage but also attenuated CO-induced apoptosis. The in-vivo studies that were conducted revealed that the intracerebroventricular (i.c.v.) pre-administration of G-$Rg_3$ significantly reduced i.c.v. CO-induced hippocampal damage in rats. To examine the mechanisms underlying the in-vitro and in-vivo neuroprotective effects of G-$Rg_3$ against CO-induced hippocampal excitotoxicity, the effect of G-$Rg_3$ on the CO-induced elevations of the apoptotic cells in cultured hippocampal cells was examined, and it was found that G-$Rg_3$ treatment inhibited CO-induced apoptosis. The histopathological evaluation demonstrated that G-$Rg_3$ significantly diminished the apoptosis in the hippocampus and also spared the hippocampal CA1, CA3, and dentate gyrus neurons. G-$Rg_3$ also significantly improved the CO-caused behavioral impairment. G-$Rg_3$ itself had no effect, however, on the CO-induced inhibition of succinate dehydrogenase activity (data not shown). These results collectively indicate the G-$Rg_3$-induced neuroprotection against CO in rat hippocampus. With regard to the wide use of G-$Rg_3$, this agent is potentially beneficial in treating CO-induced brain injury.

• Natural Product Sciences
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• v.27 no.1
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• pp.10-17
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• 2021

The purpose of this study is to develop a new method of producing tienchi seng (notoginseng, Panax notoginseng) extracts featuring high concentrations of the ginsenoside Rg3, Rg5, and Rg6, special components of Korean red ginseng. The chemical transformation from ginseng saponin glycosides to prosapogenin was analyzed by HPLC. Tienchi seng was heat-processed at 100℃ and the optimum conditions were identified. The highest concentrations of total saponin (29.723%) and the ginsenoside Rg3 (1.769%), Rg5 (5.979%), and Rg6 (13.473%) were produced at 48 hours. Also, when tienchi seng was subjected to the ultrasonic thermal fusion (100℃) process, the concentrations of total saponin (30.578%), ginsenoside Rg3 (2.392%), Rg5 (6.614%), and Rg6 (13.017%) were highest at 36 hours. On the other hand, the 2-hour heat-processed extract and 2-hour ultrasonic thermal fusion-processed extract did not contain ginsenoside Rg3, Rg5, and Rg6. The ultrasonic thermal fusion process had an extraction yield that was approximately 1.26 times greater than that of the heat process. These results indicate that the highly functional tienchi seng extracts created through the ultrasonic thermal fusion process are more industrially useful than those produced using the heat process.

• Archives of Pharmacal Research
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• v.28 no.10
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• pp.1164-1169
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• 2005

Brain microglia are phagocytic cells that are the major inflammatory response cells of the central nervous system and widely held to play important pathophysiologic roles in Alzheimer's disease (AD) in both potentially neurotoxic responses and potentially beneficial phagocytic responses. In the study, we examined whether ginsonoside Rg3, a by-product of red ginseng, enhances the microglial phagocytosis of $A{\beta}$. We found that Rg3 promoted $A{\beta}$ uptake, internalization, and digestion. Increased maximal $A{\beta}$ uptake was observed at 4 and 8 h after Rg3 pretreatment (25 ${\mu}g/mL$), and the internalized $A{\beta}$ was almost completely digested from cells within 36 h when pretreated with Rg3 comparing with single non-Rg3-treated groups. The expression of MSRA (type A MSR) was also up-regulated by Rg3 treatment in a dose- and time-dependent manner which was coincidently identified in western blots for MSRA proteins in cytosol. These results indicate that microglial phagocytosis of $A{\beta}$ may be enhanced by Rg3 and the effect of Rg3 on promoting clearance of $A{\beta}$ may be related to the MSRA-associated action of Rg3. Thus, stimulation of the MSRA might contribute to the therapeutic potentials of Rg3 in microglial phagocytosis and digestion in the treatment of AD.

• Korean Journal of Medicinal Crop Science
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• v.21 no.5
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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.

• Journal of Ginseng Research
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• v.46 no.1
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• pp.138-146
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• 2022

Background: Red Ginseng has been used for many years to treat diseases. Ginsenoside Rg3 has documented therapeutic effects, including anticancer and anti-inflammatory activities. However, the anticancer effect of Rg3-enriched red ginseng extract (Rg3-RGE) and its underlying mechanisms have not been fully explored. We investigated whether Rg3-RGE plays an anti-tumor role in lung cancer cells. Methods: To examine the effect of Rg3-RGE on lung cancer cells, we performed cell viability assays, flow cytometry, western blotting analysis, and immunofluorescence to monitor specific markers. Results: Rg3-RGE significantly inhibited cell proliferation and induced mitochondria-dependent apoptosis. Furthermore, Rg3-RGE also increased expression of mitophagy-related proteins such as PINK1 and Parkin. In addition, treatment with Rg3-RGE and mitophagy inhibitors stimulated cell death by inducing mitochondria dysfunction. Conclusions: Rg3-RGE could be used as a therapeutic agent against lung cancer.

• Journal of Microbiology and Biotechnology
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• v.33 no.1
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• pp.135-141
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• 2023

Protection of skin cells from chronic infrared-A (IRA) irradiation is crucial for anti-photoaging of the skin. In this study, we investigated the protective activity of Rg3(S) and Rg3(S)-incorporated anionic soybean lecithin liposomes (Rg3/Lipo) with a size of approximately 150 nm against IRA-induced photodamage in human fibroblasts. The formulated Rg3/Lipo showed increased solubility in aqueous solution up to a concentration of 200 ㎍/ml, compared to free Rg3(S). In addition, Rg3/Lipo exhibited superior colloidal stability in aqueous solutions and biocompatibility for normal human dermal fibroblasts (NHDFs). After repeated IRA irradiation on NHDFs, elevated levels of cellular and mitochondrial reactive oxygen species (ROS) were greatly reduced by Rg3(S) and Rg3/Lipo. In addition, cells treated with Rg3/Lipo exhibited noticeably reduced apoptotic signals following IRA irradiation compared to untreated cells. Thus, considering aqueous solubility and cellular responses, Rg3/Lipo could serve as a promising infrared protector for healthy aging of skin cells.

• Biomolecules & Therapeutics
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• v.16 no.4
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• pp.364-369
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• 2008

Anti-hyperlipidemic effect of red ginseng (RG; the steamed root of Panax ginseng C.A. Meyer) and Crataegii fructus (CF, the fruit of Crataegus pinnatifida BGE), which are used frequently in China and Korea as herbal medicines to treat arteriosclerosis, were investigated. Treatments of RG and CF significantly reduced blood triglyceride (TG) and total cholesterol (TC) levels in Triton WR-1339-induced hyperlipidemic mice and serum TG levels in corn oil-induced hypertriglyceridemic mice. Ginsenoside Rg3 and ursolic acid, the main constituents of RG and CF, respectively, also reduced TG and TC levels in hyperlipidemic mice. RG and CF significantly lowered the high blood TG and TC levels and body and epididymal mass weights induced by long-term feeding of a high-fat diet and increased the high-fat diet-induced decrease in blood HDL cholesterol levels. RG and Rg3 reduced the blood TC levels more than CF and ursolic acid. However, blood TG level were reduced by CF and ursolic acid more than RG and Rg3. RG, CF, and their constituents also inhibited pancreatic lipase and HMG-CoA reductase activities. The most potent inhibitor was Rg3. These findings suggest that RG and CF may be suitable for the therapies of hypercholesterolemia and triglyceridemia, respectively.

• Journal of Ginseng Research
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• v.43 no.2
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• pp.282-290
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• 2019

Background: Ginsenoside Rg3 (G-Rg3) is the major bioactive ingredient of Panax ginseng and has many pharmacological effects, including antiadipogenic, antiviral, and anticancer effects. However, the effect of G-Rg3 on mast cell-mediated allergic inflammation has not been investigated. Method: The antiallergic effects of G-Rg3 on allergic inflammation were evaluated using the human and rat mast cell lines HMC-1 and RBL-2H3. Antiallergic effects of G-Rg3 were detected by measuring cyclic adenosine monophosphate (cAMP), detecting calcium influx, and using real-time reverse transcription polymerase chain reaction, enzyme-linked immunosorbent assay, Western blotting, and in vivo experiments. Results: G-Rg3 decreased histamine release from activated mast cells by enhancing cAMP levels and calcium influx. Proinflammatory cytokine production was suppressed by G-Rg3 treatment via regulation of the mitogen-activated protein kinases/nuclear factor-kappa B and receptor-interacting protein kinase 2 (RIP2)/caspase-1 signaling pathway in mast cells. Moreover, G-Rg3 protected mice against the IgE-mediated passive cutaneous anaphylaxis reaction and compound 48/80-induced anaphylactic shock. Conclusion: G-Rg3 may serve as an alternative therapeutic agent for improving allergic inflammatory disorders.

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.286-290
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• 2011

Ginsenoside Rg3 was reported to have important biological activities. We demonstrate conjugation and quantification procedures of ginsenoside Rg3 to gold nanoparticles for future biological and medical applications. Ginsenoside Rg3 was conjugated to spherical gold nanoparticles using a bifunctional heptaethylene glycol linker. The sulfhydryl group of heptaethylene glycol was adsorbed onto gold nanoparticles, and carboxylic acid end of heptaethylene glycol was bonded through a hydroxyl group of Rg3 via ester bond formation. The conjugation of Rg3 was characterized with various spectroscopic techniques, high resolution-transmission electron microscopy, and using Rg3 monoclonal antibody. The Rg3- functionalized gold nanoparticles were $4.7{\pm}1.0$ nm in diameter with a surface charge of -4.12 mV. The total number of Rg3 molecules conjugated to a 3.6 mL solution of gold nanoparticle was determined to be $9.5{\times}10^{14}$ corresponding to ~6 molecules of Rg3/gold nanoparticle. These results suggest that ginsenoside Rg3 is successfully conjugated to gold nanoparticles via heptaethylene glycol linker. The quantification was performed by using Rg3 monoclonal antibody without interference of gold's intrinsic color.