Ginsenoside Rb1 Preconditioning Enhances eNOS Expression and Attenuates Myocardial Ischemia/Reperfusion Injury in Diabetic Rats

Diabetes mellitus is associated with decreased NO bioavailability in the myocardium. Ginsenoside Rb1 has been shown to confer cardioprotection against ischemia reperfusion injury. The aim of this study was to investigate whether Ginsenoside Rb1 exerts cardioprotective effects during myocardial ischemia-reperfusion in diabetic rats and whether this effect is related to increase the production of NO via enhancing eNOS expression in the myocardium. The myocardial I/R injury were induced by occluding the left anterior descending artery for 30 min followed by 120 min reperfusion. An eNOS inhibitor L-NAME or Rb1 were respectively administered 25 min or 10 min before inducing ischemia. Ginsenoside Rb1 preconditioning reduced myocardial infarct size when compared with I/R group. Ginsenoside Rb1 induced myocardial protection was accompanied with increased eNOS expression and NO concentration and reduced plasma CK and LDH (P < 0.05). Moreover, the myocardial oxidative stress and tissue histological damage was attenuated by Ginsenoside Rb1 (P < 0.05). L-NAME abolished the protective effects of Ginsenoside Rb1. It is concluded that Ginsenoside Rb1 protects against myocardium ischemia/reperfusion injury in diabetic rat by enhancing the expression of eNOS and increasing the content of NO as well as inhibiting oxidative stress

Kinetic study for the optimization of ginsenoside Rg3 production by heat treatment of ginsenoside Rb1

AbstractBackgroundGinsenoside Rg3 is a promising anticancer agent. It is usually produced by heat treatment of ginseng, in which ginsenoside Rb1 is the major ginsenoside. A kinetic study was conducted to optimize ginsenoside Rg3 production by the heat treatment of ginsenoside Rb1.MethodsGinsenoside Rb1 was heated using an isothermal machine at 80°C and 100°C and analyzed using HPLC. The kinetic parameters were calculated from the experimental results. The activation energy was estimated and used to simulate the process. The optimized parameters of ginsenoside Rg3 production are suggested based on the simulation.ResultsThe rate constants were 0.013 h−1 and 0.073 h−1 for the degradation of ginsenosides Rb1 and Rg3 at 80°C, respectively. The corresponding rate constants at 100°C were 0.045 h−1 and 0.155 h−1. The estimated activation energies of degradation of ginsenosides Rb1 and Rg3 were 69.2 kJ/mol and 40.9 kJ/mol, respectively. The rate constants at different temperatures were evaluated using the estimated activation energies, and the kinetic profiles of ginsenosides Rb1 and Rg3 at each temperature were simulated based on the proposed kinetic model of consecutive reaction. The optimum strategies for producing ginsenoside Rg3 from ginsenoside Rb1 are suggested based on the simulation. With increased temperature, a high concentration of ginsenoside Rg3 is formed rapidly. However, the concentration decreases quickly after the reaching the maximal concentration value.ConclusionThe optimum temperature for producing ginsenoside Rg3 should be the highest temperature technically feasible below 180°C, in consideration of the cooling time. The optimum reaction time for heat treatment is 30 min

Microbial conversion of major ginsenoside Rb1 to minor ginsenoside Rd by Indian fermented food bacteria

Ginsenoside Rb1 is the predominant secondary metabolite (saponin) in Panax ginseng. Hydrolysis of the sugar residues in Rb1 yields more pharmaceutically active ginsenosides like Rd, Rg3, F2, Rh2 andC-K. Among them, the minor ginsenoside Rd enhances the differentiation of neural stem cells, protects neurons from neurotoxic chemicals, decreases urea nitrogen and creatinine in kidney. It also protects the kidney from apoptosis and DNA fragmentation caused by cancer and chemical drugs and is more useful therapeutically than the major ginsenoside Rb1. Bacteria showing b-glucosidase activity were isolated from fermented Indian food using esculin-MRS agar. Bacteria from Amla in sugar syrup and Boiled Amla in jaggery syrup converted ginsenoside Rb1 to minor ginsenoside Rd. TLC and HPLC analysis showed that with increase in incubation time the conversion of Rb1 to Rd also increased. The 16s rDNA sequence was determined and the bacteria showed 93% sequence similarity to Brumimicrobium mesophilum

Preparation and Characterization of a Standardized Anticonvulsant Ginseng Rb Extract from Panax quinquefolius L.

A ginseng Rb extract (GRbE) containing three major ingredients of ginsenoside Rb1 (G-Rb1), ginsenoside Rb3 (G-Rb3) and ginsenoside Rd (G-Rd) has been shown to have anticonvulsant and neuroprotective activity. As such, sufficient characterization and standardization of this active GRbE are demanded to facilitate an ongoing preclinical investigation on its potential for the treatment of epilepsy. In the investigation, the methods for generating the active GRbE and isolating G-Rb1, G-Rb3, and G-Rd in large scale from Panax quinquefolius are described. The chemical profile of GRbE was characterized by identifying the structure of the individual ingredients using NMR, and the concentration of individual ingredients was determined using HPLC. This study demonstrates the application of the established methods for reproducibly generating anticonvulsant GRbE, which is enriched in five panaxadiol glycosides of G-Rb1, ginsenoside Rb2 (G-Rb2), G-Rb3, ginsenoside Rc (G-Rc), and G-Rd with total ginsenosides over 90%, and for purifying G-Rb1, G-Gb3 and G-Rd with purity of 97.9%, 96.6% and 98.6%, respectively

生薬ニンジンの健康食品中のジンセノサイド含有量

We investigated the contents of ginsenoside Rb1 and Rg1 in 8 products of ginseng health foods by HPLC. Ginsenosides were detected from all the products. The ginsenoside Rb1 was at the level of 0.82 ～ 43.5 mg/ g, and the ginsenoside Rg1 was at the level of 0.05 ～ 10.7 mg/g. In some ginseng health foods, ginsenosides contents were higher than that of the ginseng crude drug (Rb1 : 6.57 mg/g, Rg1 : 4.71 mg/g). Therefore, the possibility of excessive intake of ginsenosides from ginseng health foods should be considere

Ginsenoside Rb1 Reduces Nitric Oxide Production via Inhibition of Nuclear Factor-κB Activation in Interleukin-1β- Stimulated SW1353 Chondrosarcoma Cells

Purpose: To investigate the effect and the potential mechanisms of ginsenoside Rb1 on nitric oxide (NO) production in chondrocytes.Methods: SW1353 chondrosarcoma cells were stimulated with interleukin-1β (IL-1β) in the presence of 20, 40, 80 μM ginsenoside Rb1. NO concentration was assessed by the Griess reaction. Expression of inducible nitric oxide synthase (iNOS), content of inhibitor of NF-κB (IκB)α and nuclear level of nuclear factor (NF)-κB p65 were determined by Western blot. DNA binding activity of NF-κB was evaluated with Trans AM™ kit for NF-κB p65.Results: Ginsenoside Rb1 (40 and 80 μM) significantly decreased NO level by 24 (p &lt; 0.05) and 46 % (p &lt; 0.01), as well as iNOS protein expression by 40 and 55 % (p &lt; 0.01), respectively, in IL-1β- stimulated SW1353 cells. Ginsenoside Rb1 (40 and 80 μM) also markedly elevated IκBα protein content by 200 and 260 % (p &lt; 0.01), reduced the nuclear level of p65 protein by 30 and 40 % (p &lt; 0.01), as well as decreased the DNA binding activity of NF-κB by 40 and 50 % (both p &lt; 0.01), respectively, in IL- 1β-stimulated SW1353 cells.Conclusion: These results suggest that ginsenoside Rb1 inhibits IL-1β-induced NO production through downregulation of NF-κB-dependent iNOS expression in chondrocytes, and also underlines the potential mechanisms of ginseng activity in OA treatment of TCM. Keywords: Ginsenoside Rb1, Nitric oxide, Nuclear factor-κB, Chondrocytes, Osteoarthriti

Ginsenosides are novel naturally-occurring aryl hydrocarbon receptor ligands.

The aryl hydrocarbon receptor (AHR) is a ligand-dependent transcription factor that mediates many of the biological and toxicological actions of structurally diverse chemicals. In this study, we examined the ability of a series of ginsenosides extracted from ginseng, a traditional Chinese medicine, to bind to and activate/inhibit the AHR and AHR signal transduction. Utilizing a combination of ligand and DNA binding assays, molecular docking and reporter gene analysis, we demonstrated the ability of selected ginsenosides to directly bind to and activate the guinea pig cytosolic AHR, and to stimulate/inhibit AHR-dependent luciferase gene expression in a recombinant guinea pig cell line. Comparative studies revealed significant species differences in the ability of ginsenosides to stimulate AHR-dependent gene expression in guinea pig, rat, mouse and human cell lines. Not only did selected ginsenosides preferentially activate the AHR from one species and not others, mouse cell line was also significantly less responsive to these chemicals than rat and guinea pig cell lines, but the endogenous gene CYP1A1 could still be inducted in mouse cell line. Overall, the ability of these compounds to stimulate AHR signal transduction demonstrated that these ginsenosides are a new class of naturally occurring AHR agonists

Biotransformation of major ginsenosides into compound K by a new Penicillium dipodomyicola strain isolated from the soil of wild ginseng

A new strain, GH9, having ß-glucosidase activity was isolated from the soil of wild ginseng using Esculin-R2A agar. It shows the strongest activities to convert ginsenoside Rb1 to minor ginsenosides compound K. The transformation products were identified by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC), and strain GH9 was found to transform major ginsenoside to minor ginsenoside compound K as the key sole product. The optimal biotransformation conditions of GH9 with C-K were obtained as follows: media, yeast broth (YB); transforming temperature, 40°C; pH of the medium, 4 - 6; transforming time, 7 days. At these optimum conditions, the maximum yield was 86.1%. Strain GH9 was identified as a Penicillium dipodomyicola species based on the internal transcribed spacers (ITS) ITS1-5.8S-ITS2 rRNA gene sequences constructed phylogenetic trees.Key words: Biotransformation, Panax ginseng, ginsenoside Rb1, ginsenoside compound K, minor ginsenoside