Inhibition of prostaglandin biosynthesis by sulphasalazine and its metabolites

Collier, H. O. J.; Francis, A.A.; McDonald-Gibson, Wendy J.; Saeed, Sheikh A.

doi:10.1016/0090-6980(76)90145-3

Cited by 52 publications

(16 citation statements)

References 9 publications

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“…5-Aminosalicylic acid (5-ASA; mesalamine) has long been a mainstay for the treatment of mild to moderate active ulcerative colitis and is used regularly in patients with Crohn's disease. Early evidence indicated that 5-ASA was a potent in vitro inhibitor of cyclooxygenase (COX) enzymatic activity and inhibited prostaglandin E 2 (PGE 2 ) production in colonic tissue from patients with ulcerative colitis [4,5]. Furthermore, 5-ASA is a powerful free-radical scavenger and antioxidant [6,7].…”

Section: Introductionmentioning

confidence: 99%

Effects of N-Acetylcysteine Plus Mesalamine on Prostaglandin Synthesis and Nitric Oxide Generation in TNBS-Induced Colitis in Rats

et al. 2008

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The aim of the present studies was to examine mechanisms by which the rectally administered combination of N-acetylcysteine (NAC) plus mesalamine (5-ASA) affects inducers of inflammation to promote mucosal healing and reduce tissue inflammation in chemically (trinitrobenzene sulfonic acid, TNBS) induced colitis in rats. Experimental findings demonstrate that dual therapy with NAC plus 5-ASA was superior to individual agents in reducing histological measures of colitis. NAC alone and in combination with 5-ASA suppressed COX2 gene expression and prostaglandin E(2) (PGE(2)) levels to control values. Furthermore, NAC plus 5-ASA reduced nitrate generation, an expression of inducible nitric oxide synthase (iNOS) activity, to basal levels and these results were significantly lower than those observed with either NAC or 5-ASA alone. In conclusion, these results indicate that NAC plus 5-ASA exerts therapeutic benefit, in part by countering the actions of PGE(2) and the deleterious effects of oxidative and nitrosative stress induced by TNBS colitis.

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Section: Introductionmentioning

confidence: 99%

Effects of N-Acetylcysteine Plus Mesalamine on Prostaglandin Synthesis and Nitric Oxide Generation in TNBS-Induced Colitis in Rats

et al. 2008

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“…If high concentrations of prostaglandins are detrimental, then inhibitors of their synthesis would be beneficial; yet the prostaglandin synthesis inhibitors, sodium salicylate (delivered as an enema) and flurbiprofen, were not useful; indeed, the latter resulted in a worsening of the disease (Campieri, Lanfranchi, Bazzocchi, Brignola, Corazza, Cortini, Michelini & Labo, 1978;). It appears that inhibitionof prostaglandin E2 and F2a synthesis is not an important property of drugs useful in the treatment of ulcerative colitis, particularly as sulphasalazine and 5-ASA only weakly inhibit the synthetase enzymes (Collier et al, 1976;Sharon et al, 1978).…”

Section: Discussionmentioning

confidence: 99%

“…High doses can cause accumulation of fluid in the bowel with resulting effects on diarrhoea (Robert, 1976); in some circumstances prostaglandins can exhibit proinflammatory actions (Weissmann, 1980) and sulphasalazine and 5-ASA, which benefit patients with ulcerative colitis, clearly, but relatively weakly, inhibit prostaglandin synthetase activity (Collier, Francis, McDonald-Gibson & Saeed, 1976;Sharon et al, 1978). If prostaglandins are mediators of the inflammatory processes of ulcerative colitis, more powerful inhibitors of their synthesis would be of benefit.…”

Section: Introductionmentioning

confidence: 99%

ULCERATIVE COLITIS: EFFECT OF SULPHASALAZINE, ITS METABOLITES AND INDOMETHACIN ON THE ABILITY OF HUMAN COLONIC MUCOSA TO METABOLIZE PROSTAGLANDINS in vitro

Hillier

Mason

Pacheco

et al. 1982

British J Pharmacology

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“…Its effectiveness as an antiinflammatory agent is probably due to its effect on the metabolism of leukotrienes. 3,4 Different drug formulations have been developed in order to enhance the drug effectiveness and to attain the drug controlling and targeting, these formulations especially employ a pH-dependent release mechanism. 5,6 Polymeric microspheres received more attention in recent years and have emerged as the most promising carriers able to improve the site specific release characteristic of drugs.…”

Section: Introductionmentioning

confidence: 99%

Optimization and in-vitro Evaluation of Poly (lactic acid) /Mesalazine Microspheres as Drug Carriers

Banabid¹,

Ferhat²,

Maiza³

et al. 2017

IJPER

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Purpose: The present study is intended to the preparation and optimization of controlled drug release microparticles based on polylactic acid and Mesalazine. This active ingredient is usually used in the therapy of intestine inflammatory diseases, particularly the Crohn's disease and hemorrhagic recto colitis. Methods: Microencapsulation by simple O/W emulsion solvent evaporation method was used to prepare these formulations. Some of the process variables such as the emulsifier concentration, the polymer concentration, the drug: polymer ratio and stirring speed were varied and the obtained biodegradable microparticles were characterized by FTIR spectroscopy, X-ray diffraction, DSC method and optical microscopy. The drug release was established both in simulated intestinal fluid and distilled water and the data analysis and the release mechanism were investigated on the basis of Higuchi and Korsmeyer-Peppas models. Results: The microparticles' size i.e. the number mean diameter (d10) ranged from 127 to 744 µm and the drug content varied from 12 to 27%. The effect of the selected variables on the microparticles' characteristics (size, morphology and drug release) were exhaustively discussed for the PLA/mesalazine microparticles' optimization. Conclusion: This study showed that the microparticles' morphology depended strongly on the emulsifier concentration and the drug entrapment is related to the initial drug:polymer ratio and polymer concentration.

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Inhibition of prostaglandin biosynthesis by sulphasalazine and its metabolites

Cited by 52 publications

References 9 publications

Effects of N-Acetylcysteine Plus Mesalamine on Prostaglandin Synthesis and Nitric Oxide Generation in TNBS-Induced Colitis in Rats

Effects of N-Acetylcysteine Plus Mesalamine on Prostaglandin Synthesis and Nitric Oxide Generation in TNBS-Induced Colitis in Rats

ULCERATIVE COLITIS: EFFECT OF SULPHASALAZINE, ITS METABOLITES AND INDOMETHACIN ON THE ABILITY OF HUMAN COLONIC MUCOSA TO METABOLIZE PROSTAGLANDINS in vitro

Optimization and in-vitro Evaluation of Poly (lactic acid) /Mesalazine Microspheres as Drug Carriers

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