Disease relevance of GINSENOSIDE

• On the other hand, ginsenoside Rh1 does not inhibit the growth of melanoma cells even at concentrations over 100 microM but stimulates the expression of the melanotic phenotype [1].
• Ginsenoside Rh2 inhibits the growth of B16 melanoma cells, causes morphological alterations, and stimulates melanogenesis at high cellular density [1].
• This antidiabetic effect of ginsenoside Re was not associated with body weight changes, suggesting that other constituents in the extract have distinct pharmacological mechanisms on energy metabolism [2].
• Thus, ginsenoside Re acts as a specific agonist for the nongenomic pathway of sex steroid receptors, and NO released from activated eNOS underlies cardiac K(+) channel activation and protection against ischemia-reperfusion injury [3].
• We have shown that ginsenoside Rf (Rf) regulates voltage-dependent Ca(2+) channels through pertussis toxin (PTX)-sensitive G proteins in rat sensory neurons [4].

Psychiatry related information on GINSENOSIDE

• In a mouse model of Alzheimer's disease (AD) by Abeta(25-35) i.c.v. injection, impaired spatial memory was recovered by p.o. administration of ginsenoside Rb1 or M1 [5].
• The ginsenoside Rb1 has previously been reported to improve memory deficits induced by anticholinergic drug treatment, and to facilitate acetylcholine (Ach) release from rat brain hippocampal slices [6].
• Ginsenoside Rb1 significantly prolonged the response latency of ischemic gerbils and rescued a significant number of ischemic CA1 pyramidal neurons, whereas ginsenosides Rg1 and Ro were ineffective [7].
• METHODS: The effect of ginsenoside on the developing embryo during the critical period of organogenesis was investigated using a whole rat embryo culture model [8].
• Ginsenoside Rg1 prevents histaminergic modulation of rat adaptive behavior from elevation of ambient temperature [9].

High impact information on GINSENOSIDE

• To assess the antimutagenic potentials of ginsenoside Rh2 (Rh2), its effects on the baseline and mitomycin C-induced sister chromatid exchange (SCE) were examined in human peripheral blood lymphocytes (PBLs) [10].
• Suppression of the formation of sister chromatid exchanges by low concentrations of ginsenoside Rh2 in human blood lymphocytes [10].
• Prevention of ginsenoside-induced desensitization of Ca2+-activated Cl- current by microinjection of inositol hexakisphosphate in Xenopus laevis oocytes: involvement of GRK2 and beta-arrestin I [11].
• We show that Cdc6, an essential initiation factor for DNA replication, undergoes caspase-3-mediated cleavage in the early stages of apoptosis in HeLa cells and SK-HEP-1 cells induced by etoposide, paclitaxel, ginsenoside Rh2, or tumor necrosis factor-related apoptosis-inducing ligand [12].
• Injection of the cRNA coding RGS2, which interacts most selectively with G alpha(q/11) among various identified RGS isoforms and stimulates the hydrolysis of GTP to GDP in active GTP-bound G alpha subunit, resulted in a severe attenuation of ginsenoside effect on the Cl(-) current [13].

Chemical compound and disease context of GINSENOSIDE

• The effects of ginsenoside Re and its metabolite, ginsenoside Rh1, on 12-O-tetradecanoylphorbol 13-acetate- and oxazolone-induced mouse dermatitis models [14].
• Saikosaponin a and ginsenoside Rb1 were found to reduce the mutagenicity of AF-2 significantly when applied post-AF-2-treatment in the Salmonella mutagenicity assay [15].
• PURPOSE: We previously observed that American ginseng berry and ginsenoside Re attenuated cisplatin-induced emesis in a rat model, suggesting that the herb may have a value in treating chemotherapy-induced nausea/vomiting [16].
• Ginsenoside Ro (10,50, and 200 mg/kg, P. O.) inhibited an increase in vascular permeability in mice induced by acetic acid and reduced an acute paw edema in rats induced by compound 48/80 or carrageenin [17].
• The activities of saikosaponin d were much stronger than those of typical saponins ginsenoside Rg1 and glycyrrhizin and almost comparable with or somewhat weaker than those of lipopolysaccharide, a streptococcal preparation OK-432 and formalin-killed Propionibacterium acnes, indicating that saikosaponin d is a potent macrophage activator [18].

Biological context of GINSENOSIDE

• Mutations of the AP2 binding sites in the heterologous promoter and natural context systems abolished the transcriptional activation by ginsenoside Rb2 [19].
• Transcriptional activation of the Cu,Zn-superoxide dismutase gene through the AP2 site by ginsenoside Rb2 extracted from a medicinal plant, Panax ginseng [19].
• Mobility shift assays with cis-elements in the proximal promoter region showed that specific binding of the AP2 transcription factor was significantly increased by treatment with ginsenoside Rb2 [19].
• Ginsenoside Rb(1) appears to be a promising agent not only for the treatment of cerebral stroke, but also for the treatment of other diseases involving activation of mitochondrial cell death signaling.Journal of Cerebral Blood Flow & Metabolism (2006) 26, 708-721. doi:10.1038/sj.jcbfm.9600225; published online 14 September 2005 [20].
• Functional expression of a novel ginsenoside Rf binding protein from rat brain mRNA in Xenopus laevis oocytes [4].

Anatomical context of GINSENOSIDE

• G alpha(q/11) coupled to mammalian phospholipase C beta 3-like enzyme mediates the ginsenoside effect on Ca(2+)-activated Cl(-) current in the Xenopus oocyte [13].
• Although the expression levels of phosphorylated NF-H and synaptophysin were reduced in the cerebral cortex and the hippocampus of Abeta(25-35)-injected mice, their levels in ginsenoside Rb1- and M1-treated mice were almost completely recovered up to control levels [5].
• Ginsenoside F1 protects human HaCaT keratinocytes from ultraviolet-B-induced apoptosis by maintaining constant levels of Bcl-2 [21].
• Ginsenoside-induced relaxation of human bronchial smooth muscle via release of nitric oxide [22].
• This study investigates the effects of ginsenoside Rb1, a major constituent of ginseng, on Hcy-induced endothelial dysfunction and molecular changes in porcine coronary arteries [23].

Associations of GINSENOSIDE with other chemical compounds

• Among the panaxadiol fractions, ginsenoside Rb2 was a more specific and more remarkable inducer of the SOD1 gene than ginsenoside Rb1 [19].
• Estrogen-like activity of ginsenoside Rg1 derived from Panax notoginseng [24].
• Ginsenoside Re, a Main Phytosterol of Panax ginseng, Activates Cardiac Potassium Channels via a Nongenomic Pathway of Sex Hormones [3].
• To elucidate whether ginsenoside affects airway smooth muscle tone and, if so, what the mechanism of action is, we studied relaxant responses of human bronchial strips under isometric condition in vitro, and directly measured the release of nitric oxide (NO) by an amperometric sensor for this molecule [22].
• It is concluded that ginsenoside induces relaxation of human bronchial smooth muscle via stimulation of NO generation predominantly from airway epithelium and cyclic GMP synthesis [22].

Gene context of GINSENOSIDE

• 3. In human keratinocyte cultures (HaCaT cells), ginsenoside Rb1 (100 fg ml(-1) to 1 ng ml(-1)) enhanced VEGF production induced by IL-1beta and expression of hypoxia-inducible factor (HIF)-1alpha [25].
• The aim of this study was to determine the effects of ginsenoside Rg1 on the proliferation and molecular mechanism in cultured human arterial vascular smooth muscle cell (HASMC) induced by tumor necrosis factor-alpha (TNF-alpha) [26].
• Taken together, these results show that ginsenoside Rh2 and staurosporine increase caspase-3 activity, which in turn directly cleaves p21WAF1/CIP1 during the early stages of apoptosis [27].
• Treatment with ginsenoside Rg1, which blocked the cell cycle in the G1-phase, induced a downregulation of cyclin D1 and an upregulation in the expression of p53, p21(WAF/CIP1), and p27(KIP1) [26].
• Electrophoretic mobility shift assays revealed that ginsenoside Rh2 significantly inhibited the LPS/IFN-gamma-induced AP-1 DNA binding activity, while it enhanced the protein binding to CRE sequences [28].

Analytical, diagnostic and therapeutic context of GINSENOSIDE

• Prevention of ischemic neuronal death by intravenous infusion of a ginseng saponin, ginsenoside Rb(1), that upregulates Bcl-x(L) expression [20].
• It is important to stress that ginsenoside Rf and 24(R)-pseudoginsenoside F11, which possess the same molecular weight and were found to have similar retention times under most LC conditions, can be unambiguously distinguished in the present HPLC/MS method [29].
• 2 We used perforated configuration of patch-clamp technique to define the mechanism of enhancement of IKs and suppression of I(Ca,L) by ginsenoside Re in guinea-pig ventricular myocytes [30].
• Liquid chromatography/mass spectrometric analysis of rat samples for in vivo metabolism and pharmacokinetic studies of ginsenoside Rh2 [31].
• It is noteworthy that this ginsenoside production exceeded by almost 3-fold that obtained during the shake flask culture of our hairy root line, although it often happens that the scale-up from shake flask to a bioreactor culture results in reduced productivities [32].

References