naphthoquinones and Stomach-Ulcer

evaluate the antiulcer healing effect of echinochrome pigment (Ech 5 and 10 mg/kg) extracted from sea urchin (Paracentrotus lividus).. Severe gastric ulceration induced in rats by administration of indomethacin in combination with cold stress (IND + CS) for 2 h. The antiulcer effect of Ech was indicated by determination of gastric juice volume, gastric juice acidity, and ulcer index as well as determination of gastric malondialdhyde (MDA), glutathione (GSH), catalase (CAT), glutathione-S-transferase (GST), superoxide dismutase (SOD), nitric oxide (NO) activities. Moreover, macroscopic and microscopic evaluations of the stomachs were determined.. The anti-ulcer healing effect of Ech against IND + CS induced oxidative tissue injury was investigated by a significant decrease in MDA level, GST and CAT activities and a significant increase of GSH content, NO level and SOD activity. In addition, Ech treatments (5 mg/kg and 10 mg/kg) reduce gastric lesion area to (73.51% and 75.50%, respectively) with great amelioration of the gastric juice volume and acidity. Also, affirmed by maintaining macroscopic and microscopic gastric mucosal integrity.. Ech pigments had an insightful effect against peptic ulcer-induced oxidative stress in rats, as it alleviates the alterations in gastric acidity and ulcer index as well as the oxidative stress markers.

Topics: Animals; Antioxidants; Gastric Juice; Gastric Mucosa; Indomethacin; Lipid Peroxidation; Male; Naphthoquinones; Rats, Wistar; Stomach Ulcer

The possibility of using different types of carrageenans (CRG) as matrixes for incorporating of echinochrome A (Ech) was investigated. Ech interacts with carrageenans and is incorporated into the macromolecular structure of the polysaccharide. The inclusion of Ech in carrageenan matrices decreased its oxidative degradation and improved its solubility. The changing in the charge and morphology of CRGs during binding with Ech was observed. The rate of Ech release from CRG matrices depended on the structure of the used polysaccharide and the presence of specific ions. The gastroprotective effect of CRG/Ech complexes was investigated on the model of stomach ulcers induced by indomethacin in rats. Complexes of CRG/Ech exhibited significant gastroprotective activity that exceeded the activity of the reference drug Phosphalugel. The gastroprotective effect of the complexes can be associated with their protective layer on the surface of the mucous membrane of a stomach.

Topics: Animals; Carrageenan; Cytoprotection; Female; Indomethacin; Naphthoquinones; Polysaccharides; Rats, Wistar; Seaweed; Stomach; Stomach Ulcer; Sulfates

The stem bark of Tabebuia species and the rhizomes of Jatropha isabelii are used in Paraguayan traditional medicine to treat gastric lesions and as anti-inflammatory agents. The sesquiterpene cyperenoic acid obtained from J. isabelii has been shown to display a gastroprotective effect in animal models of induced gastric ulcers while the quinone lapachol shows several biological effects associated with the use of the crude drug. The aim of this work was to prepare hybrid molecules presenting a terpene and a quinone moiety and to obtain an assessment of the gastroprotective activity of the new compounds using human cell cultures (MRC-5 fibroblasts and AGS epithelial gastric cells). Eight compounds, including the natural products and semisynthetic derivatives were assessed for proliferation of MRC-5 fibroblasts, protection against sodium taurocholate-induced damage, prostaglandin E2 content, and stimulation of cellular-reduced glutathione synthesis in AGS cells. The following antioxidant assays were performed: DPPH discoloration, scavenging of the superoxide anion, and inhibition of induced lipoperoxidation in erythrocyte membranes. 3-Hydroxy-β-lapachone (3) and cyperenoic acid (4) stimulated fibroblast proliferation. Lapachol (1), dihydroprenyl lapachol (2), 3-hydroxy-β-lapachone (3), and lapachoyl cyperenate (6) protected against sodium taurocholate-induced damage in AGS cells. Lapachol (1) and dihydroprenyl lapachoyl cyperenate (7) significantly stimulated prostaglandin E2 synthesis in AGS cells. Compounds 3, 4, and 7 raised reduced glutathione levels in AGS cells. The hybrid compounds presented activities different than those of the starting sesquiterpene or quinones.

Topics: Anti-Ulcer Agents; Cells, Cultured; Epithelial Cells; Fibroblasts; Gastric Mucosa; Humans; Jatropha; Naphthoquinones; Paraguay; Plant Bark; Plant Extracts; Plant Stems; Protective Agents; Rhizome; Sesquiterpenes; Stomach Ulcer; Tabebuia

New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.

Topics: Animals; Anti-Ulcer Agents; Cell Line, Tumor; Diterpene Alkaloids; Diterpenes; Gastric Mucosa; Humans; Liver; Lung; Male; Mice; Naphthoquinones; Stomach; Stomach Ulcer; Tabebuia