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1.
Carbohydr Polym ; 151: 957-964, 2016 Oct 20.
Article in English | MEDLINE | ID: mdl-27474644

ABSTRACT

Sulfated polysaccharides extracted from seaweed have important pharmacological properties. Thus, the aim of this study was to characterize the sulfated polysaccharide (PLS) from the algae Hypnea musciformis and evaluate its protective effect in colitis induced by trinitrobenzene sulfonic acid in rats. The sulfated polysaccharide possess a high molecular mass (1.24×10(5)gmol(-1)) and is composed of a κ-carrageenan, as depicted by FT-IR and NMR spectroscopic data. PLS was administered orally (10, 30, and 60mg/kg, p.o.) for three days, starting before TNBS (trinitrobenzene sulfonic acid) instillation (day 1). The rats were killed on day three, the portion of distal colon (5cm) was excised and evaluated macroscopic scores and wet weight. Then, samples of the intestinal were used for histological evaluation and quantification of glutathione, malonyldialdehyde acid, myeloperoxidase, nitrate/nitrite and cytokines. Our results demonstrate that PLS reduced the colitis and all analyzed biochemical parameters. Thus, we concluded that the PLS extracted from the marine algae H. musciformis reduced the colitis in animal model and may have an important promising application in the inflammatory bowel diseases.


Subject(s)
Galactans/chemistry , Galactans/pharmacology , Intestines/drug effects , Sulfates/chemistry , Trinitrobenzenesulfonic Acid/adverse effects , Animals , Cytokines/metabolism , Cytoprotection/drug effects , Galactans/isolation & purification , Intestinal Mucosa/metabolism , Intestines/cytology , Intestines/immunology , Male , Neutrophil Infiltration/drug effects , Oxidative Stress/drug effects , Rats , Rats, Wistar
2.
Basic Clin Pharmacol Toxicol ; 118(6): 440-8, 2016 Jun.
Article in English | MEDLINE | ID: mdl-26582552

ABSTRACT

Diarrhoea is a significant health problem for children in developing countries that causes more than 1 million deaths annually. This study aimed to evaluate the antidiarrhoeal effect of sulphated polysaccharide (PLS) from the alga Gracilaria caudata in rodents. For the evaluation, acute diarrhoea was induced in Wistar rats (150-200 g) by administration of castor oil (10 mg/kg). Then, different parameters, including enteropooling and gastrointestinal transit and its pharmacological modulation by opioid and cholinergic pathways, were assessed using activated charcoal in Swiss Mice (25-30 g). Secretory diarrhoea was examined using cholera toxin (CT) (1 mg/loop)-treated, isolated intestinal loops from Swiss mice (25-30 g), which were also used to examine fluid secretion, loss of chloride ions into the intestinal lumen and absorption. In addition, a GM1-dependent ELISA was used to evaluate the interaction between PLS, CT and the GM1 receptor. Pre-treatment with PLS (10, 30 and 90 mg/kg) reduced faecal mass, diarrhoeal faeces and enteropooling. However, 90 mg/kg more effectively reduced these symptoms; therefore, it was used as the standard dose in subsequent experiments. Gastrointestinal transit was also reduced by PLS treatment via a cholinergic mechanism. Regarding the diarrhoea caused by CT, PLS reduced all study parameters, and the ELISA showed that PLS can interact with both the GM1 receptor and CT. These results show that PLS from G. caudata effectively improved the parameters observed in acute and secretory diarrhoea, which affects millions of people, and may lead to the development of a new alternative therapy for this disease.


Subject(s)
Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Gracilaria/chemistry , Phytotherapy/methods , Polysaccharides/pharmacology , Seaweed/chemistry , Animals , Brazil , Castor Oil/pharmacology , Cathartics/pharmacology , Cholera Toxin/pharmacology , Diarrhea/chemically induced , Disease Models, Animal , Enzyme-Linked Immunosorbent Assay , Gastrointestinal Transit/drug effects , Mice , Rats , Rats, Wistar , Receptors, Cell Surface/metabolism
3.
J Pharm Pharmacol ; 66(8): 1161-70, 2014 Aug.
Article in English | MEDLINE | ID: mdl-24579929

ABSTRACT

OBJECTIVES: The aim of this study was to evaluate the protective effect of the sulfated-polysaccharide (PLS) fraction extracted from the seaweed Gracilaria birdiae in rats with trinitrobenzenesulfonic acid (TNBS)-induced colitis. METHODS: In the experiments involving TNBS-induced colitis, rats were pretreated with polysaccharide extracted from G. birdiae (PLS: 30, 60 and 90 mg/kg, 500 µL p.o.) or dexamethasone (control group: 1 mg/kg) once daily for 3 days starting before TNBS instillation (day 1). The rats were killed on the third day, the portion of distal colon was excised and washed with 0.9% saline and pinned onto a wax block for the evaluation of macroscopic scores. Samples of the intestinal tissue were used for histological evaluation and assays for glutathione (GSH) levels, malonyldialdehyde (MDA) concentration, myeloperoxidase (MPO) activity, nitrate and nitrite (NO3 /NO2 ) concentration and cytokines levels. KEY FINDINGS: PLS treatment reduced the macroscopic and microscopic TNBS-induced intestinal damage. Additionally, it avoided the consumption of GSH, decreased pro-inflammatory cytokine levels, MDA and NO3 /NO2 concentrations and diminished the MPO activity. CONCLUSIONS: Our results suggest that the PLS fraction has a protective effect against intestinal damage through mechanisms that involve the inhibition of inflammatory cell infiltration, cytokine releasing and lipid peroxidation.


Subject(s)
Colitis/chemically induced , Colitis/drug therapy , Colon/drug effects , Gracilaria/chemistry , Polysaccharides/pharmacology , Rhodophyta/chemistry , Trinitrobenzenesulfonic Acid/pharmacology , Animals , Cytokines/metabolism , Dexamethasone/pharmacology , Glutathione/metabolism , Inflammation/drug therapy , Inflammation/metabolism , Lipid Peroxidation/drug effects , Male , Malondialdehyde/metabolism , Nitrates/metabolism , Nitrites/metabolism , Peroxidase/metabolism , Polysaccharides/chemistry , Rats , Rats, Wistar
4.
Carbohydr Polym ; 99: 59-67, 2014 Jan.
Article in English | MEDLINE | ID: mdl-24274479

ABSTRACT

The sulfated polysaccharide (PLS) fraction of Agardhiella ramosissima was characterized by microanalysis, infrared spectroscopy, NMR and gas-liquid-chromatography-mass-spectrometry. The main constituent of PLS was the ι carrageenan. The monosaccharide composition of the PLS showed galactose, 3,6-anhydrogalactose and 6-O-methylgalactose. The PLS (30 mg kg(-1)) significantly reduced the paw oedema induced by carrageenan, dextran, histamine and serotonin and also was able to significantly inhibit leucocyte migration into the peritoneal cavity and decrease the concentration of myeloperoxidase (MPO) in paw tissue. In the antinociceptive tests, the pre-treatment with PLS reduced the number of writhes, the licking time but did not increase the latency time of response. This study demonstrates for the first time the anti-inflammatory and anti-nociceptive effects of PLS from A. ramosissima. Thus, we concluded that PLS could be a new natural tool in pain and acute inflammatory conditions.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Edema/drug therapy , Inflammation/drug therapy , Pain/drug therapy , Plant Extracts/chemistry , Polysaccharides/pharmacology , Rhodophyta/chemistry , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Carrageenan , Cell Movement/drug effects , Dextrans , Edema/chemically induced , Edema/physiopathology , Galactose/analogs & derivatives , Galactose/chemistry , Hindlimb , Histamine , Inflammation/chemically induced , Inflammation/physiopathology , Male , Methylgalactosides/chemistry , Mice , Nociception/drug effects , Nociception/physiology , Pain/chemically induced , Pain/physiopathology , Peroxidase/antagonists & inhibitors , Peroxidase/metabolism , Polysaccharides/chemistry , Polysaccharides/isolation & purification , Serotonin , Spectroscopy, Fourier Transform Infrared
5.
Rev. bras. farmacogn ; 23(2): 320-328, Mar.-Apr. 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-669527

ABSTRACT

Seaweeds are the most abundant source of polysaccharides such as alginates and agar, as well as carrageenans. This study aimed to investigate the gastroprotective activity and the mechanism underlying this activity of a sulfated-polysaccharide fraction extracted from the algae Hypnea musciformis (Wulfen) J.V. Lamour. (Gigartinales-Rhodophyta). Mice were treated with sulfated-polysaccharide fraction (3, 10, 30, and 90 mg/kg, p.o.) and, after 30 min, they were administered 50% ethanol (0.5 mL/25 g, p.o.). After 1 h, gastric damage was measured using a planimeter. In addition, samples of the stomach tissue were obtained for histopathological examination and for assays to determine the glutathione and malondialdehyde levels. Other groups of mice were pretreated with N G-nitro-L-arginine methyl ester (L-NAME, 10 mg/kg, i.p.), aminoguanidine (100 mg/kg, i.p.), or glibenclamide (10 mg/kg, i.p.). After 30 min to the aminoguanidine group and 1 h to the other groups, sulfated-polysaccharide fraction (30 mg/kg, p.o.) was administered and gastric damage was induced as described above. Sulfated-polysaccharide fraction prevented ethanol-induced gastric injury in a dose-dependent manner. However, treatment with L-NAME or glibenclamide reversed this gastroprotective effect. Administration of aminoguanidine did not influence the effect of sulfated-polysaccharide fraction. Our results suggest that sulfated-polysaccharide fraction exerts a protective effect against ethanol-induced gastric damage via activation of the NO/K ATP pathway.

6.
Mar Drugs ; 10(12): 2618-33, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23342384

ABSTRACT

Red seaweeds synthesize a great variety of sulfated galactans. Sulfated polysaccharides (PLSs) from seaweed are comprised of substances with pharmaceutical and biomedical potential. The aim of the present study was to evaluate the protective effect of the PLS fraction extracted from the seaweed Gracilaria birdiae in rats with naproxen-induced gastrointestinal damage. Male Wistar rats were pretreated with 0.5% carboxymethylcellulose (control group-vehicle) or PLS (10, 30, and 90 mg/kg, p.o.) twice daily (at 09:00 and 21:00) for 2 days. After 1 h, naproxen (80 mg/kg, p.o.) was administered. The rats were killed on day two, 4 h after naproxen treatment. The stomachs were promptly excised, opened along the greater curvature, and measured using digital calipers. Furthermore, the guts of the animals were removed, and a 5-cm portion of the small intestine (jejunum and ileum) was used for the evaluation of macroscopic scores. Samples of the stomach and the small intestine were used for histological evaluation, morphometric analysis and in assays for glutathione (GSH) levels, malonyldialdehyde (MDA) concentration, and myeloperoxidase (MPO) activity. PLS treatment reduced the macroscopic and microscopic naproxen-induced gastrointestinal damage in a dose-dependent manner. Our results suggest that the PLS fraction has a protective effect against gastrointestinal damage through mechanisms that involve the inhibition of inflammatory cell infiltration and lipid peroxidation.


Subject(s)
Gastrointestinal Diseases/prevention & control , Gracilaria/chemistry , Polysaccharides/pharmacology , Animals , Dose-Response Relationship, Drug , Gastrointestinal Diseases/chemically induced , Glutathione/metabolism , Inflammation/chemically induced , Inflammation/prevention & control , Lipid Peroxidation/drug effects , Male , Malondialdehyde/metabolism , Naproxen/toxicity , Peroxidase/metabolism , Polysaccharides/administration & dosage , Polysaccharides/isolation & purification , Rats , Rats, Wistar
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