2-2--azino-di-(3-ethylbenzothiazoline)-6-sulfonic-acid and Stomach-Ulcer

The resin from the trunk wood of Virola oleifera (Schott) A. C. Smith (Myristicaceae) is used in folk medicine to hasten wound repair and to treat pain and inflammatory conditions, and our previous report indicated the anti-oxidative properties in other oxidative stress model.. To investigate the protective effects of resin from V. oleifera in two experimental models of gastric ulcer oxidative-stress dependent.. Plant material was collected and the resin was subjected to partitioning with organic solvents. The buthanol fraction was subjected to chromatographic and spectrometric methods for isolation and structural elucidation. The resin was quantified for polyphenols and flavonoids by colorimetric methods. Furthermore, the antioxidant activity of resin was determined by three different methods. The ulcers were induced acutely in Swiss male mice with ethanol/HCl and indomethacin using single-doses of 10 and 100 mg/kg. The gastroprotection of the experimental groups was comparable to reference control lansoprazole (3 mg/kg).. The gastroprotection might be related to tannins, phenolic acids and flavonoids present in the resin by antioxidant properties.. The results indicate that this resin has gastroprotective activity probably associated with the presence of phenolic antioxidant substances.

Topics: Animals; Anti-Ulcer Agents; Antioxidants; Benzothiazoles; Chromatography, Thin Layer; Disease Models, Animal; Ethanol; Flavonoids; Gastric Mucosa; Hydrochloric Acid; Indomethacin; Lethal Dose 50; Male; Mice; Myristicaceae; Phytotherapy; Plant Bark; Plant Extracts; Plants, Medicinal; Polyphenols; Resins, Plant; Solvents; Spectrometry, Mass, Electrospray Ionization; Stomach Ulcer; Sulfonic Acids; Tandem Mass Spectrometry

Lectins are proteins able to interact specifically and reversibly with carbohydrates. They are present in all living beings, particularly in legume seeds, which have many biological functions. The aim of this study was to isolate, characterize and verify antioxidant, anti-hemolytic, antitumor and gastroprotective activities in a lectin present in seeds of Phaseolus lunatus L. var. cascavel (PLUN). The isolation of lectin was performed by size exclusion chromatography on Sephadex G-100, which was isolated from a protein capable of agglutinating only human erythrocytes type A, being this the only inhibited haemagglutination n-acetyl-d-galactosamine. Its weight was estimated by PAGE is 128kDa. The lectin is thermostable up to 80°C and is active between pH 2-11. As 8M urea was able to denature the lectin. PLUN is a glycoprotein consisting of 2% carbohydrate and has antioxidant action with ascorbic acid equivalent antioxidant capacity (μMAA/g) of 418.20, 326 and 82.9 for total antioxidant activity, ABTS radical capture and capture of DPPH radical, respectively. The lectin has antitumor activity against melanoma derived cells at doses of 100 and 50mg/ml, reducing up to 83% tumor cells, and gastroprotective action, reducing up to 63% damaged area of ​​the stomach induced by ethanol.

Topics: Acetylgalactosamine; Animals; Antineoplastic Agents, Phytogenic; Antioxidants; Benzothiazoles; Biphenyl Compounds; Cell Line, Tumor; Erythrocytes; Ethanol; Gastrointestinal Agents; Hemagglutination Tests; Humans; Male; Mice; Molecular Weight; Phaseolus; Picrates; Plant Lectins; Protein Denaturation; Seeds; Solid Phase Extraction; Stomach; Stomach Ulcer; Sulfonic Acids; Urea

Euphorbia umbellata (leitosinha) is used in southern Brazilian folk medicine to treat gastric problems, as well as for its analgesic and anti-inflammatory properties.. To evaluate the anti-ulcer effects of methanolic bark fraction (MF) against in vivo and in vitro assays, as well as an antioxidant, antibacterial and chromatographic study of this fraction.. In vivo anti-ulcer activity was performed using ethanol and indomethacin models with different MF concentrations (50, 100 or 200mg/Kg). The stomachs of the animals were applied to histological evaluation, and the serum to evaluate the ABTS(•+) radical capture. The 200mg/Kg dose was used to analyze the mechanisms involved in antiulcerogenic properties of methanolic fraction. The in vitro activity was performed using several different antioxidant assays, in addition to anti-Helicobacter pylori and anti-urease experiments. The chromatographic study was carried out by LC-MS analysis.. Pharmacological investigation of the MF showed an anti-ulcer potential in ethanol and indomethacin in vivo assays. The material presented a high antioxidant activity for several oxidant in vitro systems (DPPH(•), ABTS(•+), O2(•-), HOCl, TauCl and HRP), as well as an ABTS(•+) capture increasing (7.5%) by the treated animals serum (when compared to the negative control). Prostaglandins, nitric oxide/ cyclic guanosine monophosphate pathway and involvement of the protein components of the glutathione complex are some of the mechanisms related with this potential anti-ulcer action. The histological examination of the stomachs of the animals showed that the MF also prevents local action of offensive agents. Chemical analysis using LC-QTOF-MS revealed the presence of ellagic and gallic acid derivatives and flavonols.. The findings provide scientific basis to the ethnopharmacological purpose of the studied plant and the biological activities of MF of E. umbellata stem bark may be due to the presence of phenolic compounds.

Topics: Animals; Anti-Bacterial Agents; Anti-Ulcer Agents; Antioxidants; Benzothiazoles; Chromatography, High Pressure Liquid; Disease Models, Animal; Dose-Response Relationship, Drug; Ellagic Acid; Ethanol; Ethnopharmacology; Euphorbia; Female; Flavonols; Gallic Acid; Gastric Mucosa; Helicobacter pylori; Indomethacin; Methanol; Phytotherapy; Plant Bark; Plant Extracts; Plants, Medicinal; Polyphenols; Rats, Wistar; Signal Transduction; Solvents; Spectrometry, Mass, Electrospray Ionization; Stomach; Stomach Ulcer; Sulfonic Acids

Cuphea aequipetala (Lythraceae) is a medicinal plant highly appreciated in Mexico to treat stomach ailments such as pain and burning sensation, stomach infections, ulcers, diarrhea, dysentery, and different types of tumors and bruises. In this work, the infusion of aerial parts of this plant (CAI) was investigated for its polypharmacological potential.. In vitro anti-Helicobacter pylori activity was assessed by broth dilution method. Pharmacological studies included acute toxicity in mice using Lorke´s model, anti-inflammatory activity by xylene and TPA induced ear edema assay, as well as gastroprotection with ethanol-induced gastric ulcer model. DPPH and ABTS assays were used to determine antioxidant capacity. Polyphenols and flavonoid contents were determined by Folin-Ciocalteu method and AlCl3 reaction, respectively.. CAI showed good anti-Helicobacter pylori activity with a MIC of 125μg/mL. The infusion was not toxic according to Lorke's model with a LD50 greater than 5g/kg. CAI exhibited low anti-edematogenic action in the models assayed. Oral administration of 300mg/kg CAI significantly reduced gastric lesions by 87.9%. The effect was reversed only by indomethacin and N-ethylmaleimide demonstrating the role of endogenous prostaglandins and sulfhydryl compounds in gastroprotection. Total phenolic and flavonoid contents of CAI were 109.9mg GAE/g DW and 28.1mg QE/g DW, respectively, and the infusion exhibited a good antioxidant activity that is thought to play a role in its biological activity. The analysis of a preliminary fractionation of the infusion indicates that the complete extract conserves all its pharmacological activities in contrast to fractionated extracts.. Cuphea aequipetala is a promising native herb in an integral therapy for the treatment of bacterial or non-bacterial gastric ulcer because it possesses some anti-inflammatory properties, as well as exhibits good gastroprotective and antibacterial effects. It represents an important source for the isolation of anti-Helicobacter pylori compounds. This work provides ethnopharmacological evidence that supports the traditional use of this species.

Topics: Animals; Anti-Inflammatory Agents; Anti-Ulcer Agents; Antioxidants; Benzothiazoles; Cuphea; Edema; Ethanol; Flavonoids; Helicobacter pylori; Male; Mice; Plant Components, Aerial; Plant Extracts; Polyphenols; Stomach Ulcer; Sulfonic Acids; Tetradecanoylphorbol Acetate; Toxicity Tests, Acute; Xylenes