OBJECTIVE: To examine the antiplatelet and antithrombotic activity of Rumex acetosella extract. METHODS: Standard light aggregometry was used for platelet aggregation, intracellular calcium mobilization assessed using Fura-2/AM, granule secretion (ATP release) by luminometer, and fibrinogen binding to integrin α_IIbβ₃ detected using flow cytometry. Western blotting is carried out to determine the phosphorylation of mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K)/Akt signaling. RESULTS: Rumex acetosella displayed the ability to inhibit platelet aggregation, calcium mobilization, granule secretion, and fibrinogen binding to integrin α_IIbβ₃. Rumex acetosella has also down-regulated MAPK and PI3K/Akt phosphorylation (all P<0.01). CONCLUSION Rumex acetosella extract exhibits antiplatelet activity via modulating GPVI signaling, and it may protect against the development of platelet-related cardiovascular diseases.
Blood Platelets/metabolism* ; Calcium/metabolism* ; Fibrinogen/metabolism* ; Mitogen-Activated Protein Kinases/metabolism* ; Phosphatidylinositol 3-Kinase/pharmacology* ; Phosphatidylinositol 3-Kinases/metabolism* ; Phosphorylation ; Plant Extracts/pharmacology* ; Platelet Aggregation ; Platelet Aggregation Inhibitors/pharmacology* ; Platelet Glycoprotein GPIIb-IIIa Complex/pharmacology* ; Proto-Oncogene Proteins c-akt/metabolism* ; Rumex/metabolism*

The present study was designed to investigate the anti-sepsis effects of physcion 8-O-β-glucopyranoside (POG) isolated from Rumex japonicas and explore its possible pharmacological mechanisms. POG was extracted from R. japonicas by bioactivity-guided isolation with the anti-sepsis agents. Survival analysis in septic mouse induced by LPS and heat-killed Escherichia coli were used to evaluate the protective effect of POG (40 mg·kg, i.p.) on sepsis. Cytokines including TNF-α, IL-1β and IL-6 in RAW 264.7 cells induced by LPS (100 ng·mL) were determined by ELISA. In addition, the proteins expressions of TLR2 and TLR4 were determined by Western blotting assay. Our results demonstrated that POG (40 mg·kg, i.p.) possessed significant protective activity on the endotoxemic mice. The POG treatment (20, 40, and 80 μg·mL) significantly decreased the TNF-α, IL-1β and IL-6 induced by LPS (P < 0.01) in a concentration-dependent manner. Furthermore, the TLR4 and TLR2 proteins were also down-regulated by POG at 20 (P < 0.01), 40 (P < 0.01), and 80 μg·mL (P < 0.01). The present study demonstrated that the POG extracted from R. japonicas possessed significant anti-sepsis effect on endotoxemic mice, and can be developed as a novel drug for treating sepsis in the future.
Animals ; Anti-Inflammatory Agents ; administration & dosage ; Drugs, Chinese Herbal ; administration & dosage ; Emodin ; administration & dosage ; analogs & derivatives ; Glucosides ; administration & dosage ; Humans ; Interleukin-1beta ; genetics ; immunology ; Interleukin-6 ; genetics ; immunology ; Interleukin-8 ; genetics ; immunology ; Macrophages ; drug effects ; immunology ; Male ; Mice ; Mice, Inbred ICR ; RAW 264.7 Cells ; Rumex ; chemistry ; Sepsis ; drug therapy ; genetics ; immunology ; Tumor Necrosis Factor-alpha ; genetics ; immunology

Quercetin-3-O-beta-D-glucuronopyranoside (QGC) is a flavonoid glucoside extracted from Rumex Aquaticus Herba. In the present study, anti-oxidative and anti-inflammatory effects of QGC were tested in vitro. Epithelial cells obtained from cat esophagus were cultured. When the cells were exposed to acid for 2 h, cell viability was decreased to 36%. Pretreatment with 50 microM QGC for 2 h prevented the reduction in cell viability. QGC also inhibited the productions of intracellular ROS by inflammatory inducers such as acid, lipopolysaccharide, indomethacin and ethanol. QGC significantly increased the activities of superoxide dismutase (SOD) and catalase, and also induced the expression of SOD2, while it restored the decrease of catalase expression in cells exposed to acid. QGC inhibited NF-kappaB translocation, cyclooxygenase-2 expression and PGE2 secretion in cells exposed to acid, which plays an important role in the pathogenesis of esophagitis. The data suggest that QGC may well be one of the promising substances to attenuate oxidative epithelial cell injury and inflammatory signaling in esophagus inflammation.
Animals ; Catalase ; Cats ; Cell Survival ; Cyclooxygenase 2 ; Dinoprostone ; Epithelial Cells ; Esophagitis ; Esophagus ; Ethanol ; Indomethacin ; Inflammation ; NF-kappa B ; Quercetin ; Rumex ; Superoxide Dismutase

This study investigated effect of extract containing quercetin-3-O-beta-D-glucuronopyranoside from Rumex Aquaticus Herba (ECQ) against chronic gastritis in rats. To produce chronic gastritis, the animals received a daily intra-gastric administration of 0.1 ml of 0.15% iodoacetamide (IA) solution for 7 days. Daily exposure of the gastric mucosa to IA induced both gastric lesions and significant reductions of body weight and food and water intake. These reductions recovered with treatment with ECQ for 7 days. ECQ significantly inhibited the elevation of the malondialdehyde levels and myeloperoxidase activity, which were used as indices of lipid peroxidation and neutrophil infiltration. ECQ recovered the level of glutathione, activity of superoxide dismutase (SOD), and expression of SOD-2. The increased levels of total NO concentration and iNOS expression in the IA-induced chronic gastritis were significantly reduced by treatment with ECQ. These results suggest that the ECQ has a therapeutic effect on chronic gastritis in rats by inhibitory actions on neutrophil infiltration, lipid peroxidation and various steps of reactive oxygen species (ROS) generation.
Animals ; Body Weight ; Drinking ; Gastric Mucosa ; Gastritis* ; Glutathione ; Iodoacetamide* ; Lipid Peroxidation ; Malondialdehyde ; Neutrophil Infiltration ; Peroxidase ; Quercetin* ; Rats* ; Reactive Oxygen Species ; Rumex ; Superoxide Dismutase

The study elucidated carbohydrase inhibition, anti-cancerous, free radical scavenging properties and also investigated the DNA and protein protection abilities of methanolic root extract of Rumex crispus (RERC). For this purpose, pulverized roots of Rumex crispus was extracted in methanol (80% and absolute conc.) for 3 hrs for 60degrees C and filtered and evaporated with vacuum rotary evaporator. RERC showed high phenolic content (211 microg/GAE equivalent) and strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging (IC50 = 42.86 (absolute methanol) and 36.91 microg/mL (80% methanolic extract)) and reduced power ability. Furthermore, RERC exhibited significant protective ability in H2O2/Fe3+/ascorbic acid-induced protein or DNA damage and percentage inhibition of the HT-29 cell growth rate following 80% methanolic RERC exposure at 400 microg/mL was observed to be highest (10.2% +/- 1.03). Moreover, methanolic RERC inhibited alpha-glucosidase and amylase effectively and significantly (P < 0.05). Conclusively, RERC could be considered as potent carbohydrase inhibitor, anti-cancerous and anti-oxidant.
alpha-Glucosidases ; Amylases ; Biphenyl Compounds ; DNA ; DNA Damage ; Glycoside Hydrolases ; HT29 Cells ; Humans ; Methanol ; Phenol ; Picrates ; Power (Psychology) ; Rumex ; Vacuum

This study was designed to determine the protective effect of Rumex Aquaticus Herba extracts containing quercetin-3-beta-D-glucuronopyranoside (ECQ) on experimental reflux esophagitis. Reflux esophagitis was induced by surgical procedure. The rats were divided into seven groups, namely normal group, control group, ECQ (1, 3, 10, 30 mg/kg) group and omeprazole (30 mg/kg) group. ECQ and omeprazole groups received intraduodenal administration. The Rats were starved for 24 hours before the experiments, but were freely allowed to drink water. ECQ group attenuated the gross esophagitis significantly compared to that treated with omeprazole in a dose-dependent manner. ECQ decreased the volume of gastric juice and increased the gastric pH, which are similar to those of omeprazole group. In addition, ECQ inhibited the acid output effectively in reflux esophagitis. Significantly increased amounts of malondialdehyde (MDA), myeloperoxidase (MPO) activity and the mucosal depletion of reduced glutathione (GSH) were observed in the reflux esophagitis. ECQ administration attenuated the decrement of the GSH levels and affected the MDA levels and MPO activity. These results suggest that the ECQ has a protective effect which may be attributed to its multiple effects including anti-secretory, anti-oxidative and anti-inflammatory actions on reflux esophagitis in rats.
Animals ; Control Groups ; Esophagitis ; Esophagitis, Peptic ; Gastric Juice ; Glutathione ; Hydrogen-Ion Concentration ; Malondialdehyde ; Omeprazole ; Peroxidase ; Rats ; Rumex ; Water

We investigated inhibitory effects of extract containing quercetin-3-O-beta-D-glucuronopyranoside (ECQ) extracted from Rumex Aquaticus Herba on indomethacin-induced gastric damage in Rats. Gastritis was induced in male Sprague-Dawley rats (200~220 g) by oral administration of indomethacin at a dose of 40 mg/kg. One hour before administration of indomethacin, animals were orally pretreated with ECQ at doses of 0.3, 1, 3 or 10 mg/kg. Six hours after indomethacin administration, the rats were sacrificed and the stomach was excised and opened along the greater curvature, and the surface area of gastric lesion was measured using optical microscope. Superoxide dismutase (SOD), catalase (CAT), myeloperoxidase (MPO) activities and malondialdehyde (MDA) levels were measured by ELISA. Western blot analysis was performed to detect protein expression of SOD-2. Linear hemorrhagic mucosal lesions were observed in the stomach 6 hours after oral administration of indomethacin. Pretreatment with ECQ significantly reduced the severity of the lesions in a dose-dependent manner. It also inhibited the reductions in SOD and CAT activities and SOD expression by the indomethacin-induced gastric damage. In addition, the pretreatment with ECQ significantly suppressed the elevation of the MPO activity and the MDA levels induced by indomethacin. These results suggest that ECQ has the inhibitory effects via antioxidative action against indomethacin-induced gastritis in rats.
Administration, Oral ; Animals ; Blotting, Western ; Catalase ; Cats ; Enzyme-Linked Immunosorbent Assay ; Gastritis ; Humans ; Indomethacin ; Male ; Malondialdehyde ; Peroxidase ; Quercetin ; Rats ; Rats, Sprague-Dawley ; Rumex ; Stomach ; Superoxide Dismutase

Quercetin-3-O-beta-D-glucuronopyranoside (QGC) is a flavonoid glucoside extracted from Rumex Aquaticus Herba. We aimed to explore its protective effect against ethanol-induced cell damage and the mechanism involved in the effect in feline esophageal epithelial cells (EEC). Cell viability was tested and 2',7'-dichlorofluorescin diacetate assay was used to detect intracellular H2O2 production. Western blotting analysis was performed to investigate MAPK activation and interleukin 6 (IL-6) expression. Exposure of cells to 10% ethanol time-dependently decreased cell viability. Notably, exposure to ethanol for 30 min decreased cell viability to 43.4%. When cells were incubated with 50 microM QGC for 12 h prior to and during ethanol treatment, cell viability was increased to 65%. QGC also inhibited the H2O2 production and activation of ERK 1/2 induced by ethanol. Pretreatment of cells with the NADPH oxidase inhibitor, diphenylene iodonium, also inhibited the ethanol-induced ERK 1/2 activation. Treatment of cells with ethanol for 30 or 60 min in the absence or presence of QGC exhibited no changes in the IL-6 expression or release compared to control. Taken together, the data indicate that the cytoprotective effect of QGC against ethanol-induced cell damage may involve inhibition of ROS generation and downstream activation of the ERK 1/2 in feline EEC.
Blotting, Western ; Cell Survival ; Epithelial Cells ; Ethanol ; European Union ; Fluoresceins ; Hydrogen Peroxide ; Interleukin-6 ; NADPH Oxidase ; Onium Compounds ; Quercetin ; Rumex

A new anthraquinone, (1)-hydroxymethyl-3,6-dimethoxyl-2,8-dihydroxylanthraquinone 1, was isolated from the root of Rumex japonicus along with six known compounds 2-7. Their structures were elucidated by various spectroscopic methods including 2D-NMR techniques or comparison with authentic samples.
Anthraquinones ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Plant Extracts ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Rumex ; chemistry

It was evaluated the inhibitory action of quercetin-3-O-beta-D-glucuronopyranoside (QGC) on reflux esophagitis and gastritis in rats. QGC was isolated from the herba of Rumex Aquaticus. Reflux esophagitis or gastritis was induced surgically or by administering indomethacin, respectively. Oral QGC decreased ulcer index, injury area, gastric volume, and acid output and increased gastric pH as compared with quercetin. Furthermore, QGC significantly decreased gastric lesion sizes induced by exposing the gastric mucosa to indomethacin. Malondialdehyde levels were found to increase significantly after inducing reflux esophagitis, and were reduced by QGC, but not by quercetin or omeprazole. These results show that QGC can inhibit reflux esophagitis and gastritis in rats.
Animals ; Esophagitis, Peptic ; Gastric Mucosa ; Gastritis ; Hydrogen-Ion Concentration ; Indomethacin ; Lipid Peroxidation ; Malondialdehyde ; Omeprazole ; Quercetin ; Rats ; Rumex ; Ulcer