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1.  Physico-chemical characterization and pharmacological evaluation of sulfated polysaccharides from three species of Mediterranean brown algae of the genus Cystoseira 
Background
Seaweed polysaccharides are highly active natural substances having valuable applications. The present study was conducted to characterize the physico-chemical properties of sulphated polysaccharides from three Mediterranean brown seaweeds (Cystoseira sedoides, Cystoseira compressa and Cystoseira crinita) and to evaluate their anti-radical, anti-inflammatory and gastroprotective activities.
Methods
The different rates of neutral sugars, uronic acids, L-fucose and sulphate content were determined by colorimetric techniques. The different macromolecular characteristics of isolated fucoidans were identified by size exclusion chromatography equipped with a triple detection: multiangle light scattering, viscometer and differential refractive index detectors, (SEC/MALS/VD/DRI). Anti-inflammatory activity was evaluated, using the carrageenan-induced rat paw edema test in comparison to the references drugs Acetylsalicylate of Lysine and Diclofenac. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats and to examine the antioxidant effect of fucoidans in the three species, the free radical scavenging activity was determined using 1,1-diphenyl-2-picrylhydrazyl.
Results
The pharmacological evaluation of the isolated fucoidans for their anti-inflammatory, and their gastroprotective effect established that these products from C. sedoides, C. compressa and C. crinita exhibited a significant anti-inflammatory activity at a dose of 50 mg/kg, i.p; the percentages of inhibition of the oedema were 51%, 57% and 58% respectively. And, at the same dose, these fucoidans from C. sedoides and C. compressa showed a significant decrease of the intensity of gastric mucosal damages compared to a control group by 68%, whereas, the fucoidan from C. crinita produced a less gastroprotective effect. Furthermore, the isolated fucoidans exhibited a radical scavenging activity.
Conclusion
The comparative study of fucoidans isolated from three species of the genus Cystoseira showed that they have similar chemicals properties and relatives anti-radical, anti-inflammatory and gastroprotective activities which are found to be promising.
doi:10.1186/s40199-015-0089-6
PMCID: PMC4298055  PMID: 25582169
Fucoidans; Cystoseiraceae; Cystoseira; SEC/MALS/VS/DRI; Anti-inflammatory activity; Gastroprotective activity
2.  Pharmacological evaluation of the semi-purified fractions from the soft coral Eunicella singularis and isolation of pure compounds 
Background
Gorgonians of the genus Eunicella are known for possessing a wide range of pharmacological activities such as antiproliferative and antibacterial effect. The aim of this study was to evaluate the anti-inflammatory and gastroprotective effect of the organic extract and its semi-purified fractions from the white gorgonian Eunicella singularis and the isolation and identification of pure compound(s) from the more effective fraction.
Methods
Anti-inflammatory activity was evaluated, using the carrageenan-induced rat paw edema test and in comparison to the reference drug Acetylsalicylate of Lysine. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification of compound(s) from the more effective fraction was done by two chromatographic methods (HPLC and MPLC). The structure elucidation was determined by extensive spectroscopic analysis (1H and 13C NMR, COSY, HMBC, HMQC and NOESY) and by comparison with data reported in the literature.
Results
The evaluation of the anti-inflammatory activity of different fractions from Eunicella singularis showed in a dependent dose manner an important anti-inflammatory activity of the ethanol fraction, the percentage of inhibition of edema, 3 h after carrageenan injection was 66.12%, more effective than the reference drug (56.32%). In addition, this ethanolic fraction showed an interesting gastroprotective effect compared to the reference drugs, ranitidine and omeprazol. The percentage of inhibition of gastric ulcer induced by HCl/ethanol in rats was 70.27%. The percentage of the reference drugs (ranitidine and omeprazol) were 65 and 87.53%, respectively. The purification and structure elucidation of compound(s) from this ethanolic fraction were leading to the isolation of five sterols: cholesterol (5α-cholest-5-en-3β-ol) (1); ergosterol (ergosta-5,22-dien-3β-ol) (2); stigmasterol (24-ethylcholesta-5,22-dien-3b-ol) (3); 5α,8α-epidioxyergosta 6,22-dien-3β-ol (4) and 3β-hydroxy-5α,8α-epidioxyergosta-6-ene (5); and one diterpenoid: palmonine D (6).
Conclusion
Based on data presented here, we concluded that diterpenoids and sterols detected in the ethanolic fraction can be responsible for its pharmacological activity.
Electronic supplementary material
The online version of this article (doi:10.1186/s40199-014-0064-7) contains supplementary material, which is available to authorized users.
doi:10.1186/s40199-014-0064-7
PMCID: PMC4172910  PMID: 25199994
Eunicella singularis; Anti-inflammatory activity; Gastroprotective effect; Marine natural product; Diterpenoid; Sterols
3.  Antioxidant, Anti-inflammatory and Antiproliferative Effects of Aqueous Extracts of Three Mediterranean Brown Seaweeds of the Genus Cystoseira 
Seaweeds have caused an emerging interest in the biomedical area, mainly due to their contents of bioactive substances which show great potential as anti-inflammatory, anti-microbial, anti-viral and anti-tumoral drugs. Despite the diversity in quality and quantity of the Mediterranean Tunisian coast flora, with its large contains of marine organisms and seaweeds, most of them have not yet been investigated for pharmacological and biological activities. Antioxidant, anti-inflammatory and antiproliferative effects of the aqueous extracts (AQ) of three brown seaweed respectively, Cystoseira crinita (AQ-Ccri), Cystoseira sedoides (AQ-Csed) and Cystoseira compressa (AQ-Ccom) were investigated. Antioxidant activity was evaluated using the DPPH assay. Total phenolic contents were measured using Folin–Ciocalteu method. The anti-inflammatory activity of these extracts was determined in-vivo, using carrageenan induced rat paw oedema assay. The antiproliferative activity was studied on normal cells (MDCK and rat fibroblast) and cancer (A549, MCF7 and HCT15) cell lines by the ability of the cells to metabolically reduce MTT formazan dyes, in comparison to a reference drug the Cisplatin. Results demonstrated that AQ-Ccri, AQ-Csed and AQ-Ccom extracts exhibited significant radical scavenging activity. AQ-Ccom extract had the highest total phenolic content. AQ-Ccri, AQ-Csed and AQ-Ccom extracts exhibited significant anti-inflammatory activity in a dose dependent manner by comparison to reference drugs. Moreover, AQ-Ccri, AQ-Csed and AQ-Ccom extracts showed an important antiproliferative activity against both Human tumor cell lines HCT15 and MCF7. These pharmacological efficacies of these AQ- extracts of Cystoseira were positively correlated with their total phenol content and their good antioxidant activity. The purification and the determination of chemical structures of compounds of these active aqueous extracts are under investigation. It could have a promising role in the future medicine and nutrition when used as drug or food additive.
PMCID: PMC3985253  PMID: 24734073
Antioxidant activity; Antiproliferative activity; Anti-inflammatory activity;  Cystoseira
4.  Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: anti-inflammatory agents with gastroprotective effect in rats 
Medicinal Chemistry Research  2013;23(3):1591-1598.
We report the synthesis of new anti-inflammatory 1,7-dihydropyrazolo[3′,4′:4,5]pyrimido[1,6-a]pyrimidine 5 from aminocyanopyrazole. All compounds were characterized by physical, chemical and spectral studies. Preliminary pharmacological evaluation of the resulting products showed that compounds 5a, b, f (50–100 mg/kg, i.p) are active anti-inflammatory agents in carrageenan-induced rat paw oedema assay, and their effects are comparable to that of acetylsalicylic–lysine (300 mg/kg, i.p.), used as a reference drug. The nature of substituent (Y, R3) had a pronounced effect on the anti-inflammatory activity. Studies of structure–activity relationships have led to selection of compound ethyl-3,5-dimethyl-7-imino-N1-phenyl-1,7-dihydropyrazolo[3′,4′:4,5]pyrimido[1,6-a]pyrimidine-6-carboxylate, 5f which exhibited the most potent anti-inflammatory activity. In addition, the compounds 5a, b, f showed a significant gastroprotective effect against HCl/EtOH-induced gastric ulcer.
doi:10.1007/s00044-013-0742-x
PMCID: PMC3905175  PMID: 24489456
Aminocyanopyrazole; Anti-inflammatory; Gastroprotective; Pyrazolo[3,4-d]pyrimidine; Dihydropyrazolo[3′,4′:4,5]pyrimido[1,6-a]pyrimidine
5.  Evaluation of antiproliferative and anti-inflammatory activities of methanol extract and its fractions from the Mediterranean sponge 
Background
Without doubt, natural products have been, and still are, the cornerstone of the health care armamentarium. Of all natural sources, the marine environment is clearly the last great frontier for pharmaceutical and medical research.
Methods
This work progresses in the direction of identifying component(s) from the Mediterranean sponge, Spongia officinalis with pharmacological activities. In the present study we investigated the efficacy of methanol extract and its semi-purified fractions (F2, F3) from Spongia officinalis for their in vivo anti-inflammatory activity using the carrageenan-induced paw edema in rats and their in vitro antiproliferative effects by their potential cytotoxic activity using the MTT colorimetric method and clonogenic inhibition against three human cancer cell lines (A549, lung cell carcinoma, HCT15, colon cell carcinoma and MCF7, breast adenocarcinoma).
Results
The fractions F2 and F3 showed interesting anti-inflammatory and antiproliferative activities in a dose dependent manner.
Conclusions
The present study indicates that the methanolic extrac and its fractions from Spongia officinalis are a significant source of compounds with the antiproliferative and anti-inflammatory activities, and this may be useful for developing potential chemopreventive substances.
doi:10.1186/1475-2867-12-18
PMCID: PMC3441879  PMID: 22587650
Spongia officinalis; Anti-inflammatory activity; Antiproliferative activity
6.  Anticonvulsant and analgesic activities of crude extract and its fractions of the defensive secretion from the Mediterranean sponge, Spongia officinalis 
This study progresses in the direction of identifying component(s) from the Mediterranean sponge, Spongia officinalis with anticonvulsant and analgesic activities. We investigated the efficacy of crude extract and its semi-purified fractions (F1-F3) of the defensive secretion from Spongia officinalis for their in vivo anticonvulsant activity using the pentylenetetrazole (PTZ) seizure model and analgesic activity using the writhing test in mice. Among the series the crude extract exhibited interesting analgesic activity in a dose dependent manner. Similarly the fraction F2 showed a partial protection of mice from PTZ-induced seizure and interesting analgesic activity in a dose dependent manner. The purification and the determination of chemical structure(s) of compound(s) of this active fraction are under investigation.
doi:10.1186/1475-2867-12-15
PMCID: PMC3407508  PMID: 22494441
Spongia officinalis; Anticonvulsant activity; Analgesic activity
7.  Parallel synthesis and anti-inflammatory activity of cyclic peptides cyclosquamosin D and Met-cherimolacyclopeptide B and their analogs 
We report the parallel synthesis of two natural cyclopeptides, isolated from the seeds of Annona squamosa, cyclosquamosin D (A1) and Met-cherimolacyclopeptide B (B) and their analogs. All of the compounds were screened for anti-inflammatory activity by evaluating their inhibitory effects on the production of pro-inflammatory cytokines using the lipopolysaccharide stimulated macrophage J774A.1 cell line. Compounds having significant anti-inflammatory activity in suppressing the secretion of IL-6 and TNF-α have been identified, some of which exhibit activity superior to that observed with the natural products.
doi:10.1016/j.bmcl.2010.08.033
PMCID: PMC2940269  PMID: 20801649
Parallel synthesis; Solid phase synthesis; natural cyclopeptides; antiinflammatory activity

Results 1-7 (7)