S-diclofenac (2-[(2,6-dichlorophenyl)amino]benzeneacetic acid 4-(3H-1,2-dithiole-3-thione-5-yl)-phenyl ester) is a novel derivative of diclofenac which, in vivo, undergoes enzymatic cleavage of its ester linkage to release hydrogen sulfide (H(2)S) along with the parent moiety, diclofenac. In this study the anti-inflammatory activity of S-diclofenac and diclofenac was studied in a carrageenan-evoked hindpaw oedema model in the rat. Drugs or vehicle were administered 3 h before carrageenan. Both drugs produced a dose-dependent anti-inflammatory effect in this model. However, S-diclofenac (ED(30), 14.2+/-0.6 micromol/kg) was more potent (P<0.05) than diclofenac (ED(30), 39.3+/-1.4 micromol/kg) as an inhibitor both of hindpaw swelling and in reducing the carrageenan-evoked rise in hindpaw myeloperoxidase activity reflecting tissue neutrophil infiltration (ED(50)s of 12.0+/-2.1 micromol/kg and 21.9+/-2.0 micromol/kg). Intraplantar carrageenan injection also significantly (P<0.05) increased hindpaw concentrations of prostaglandin E(2) (PGE(2)), nitrite/nitrate and H(2)S synthesizing activity measured at 6 h. Both S-diclofenac and diclofenac pretreatment reduced the carrageenan-induced rise in hindpaw PGE(2), nitrite/nitrate and H(2)S synthesizing activity. Whilst treatment with either drug produced similar inhibition of hindpaw PGE(2) and H(2)S synthesizing activity--S-diclofenac more effectively reduced hindpaw nitrite/nitrate concentration than did diclofenac. It is proposed that the enhanced anti-inflammatory effect of S-diclofenac relates to its ability to release H(2)S at the inflamed site. These data provide evidence for an anti-inflammatory effect of H(2)S.
Pharmacology, Toxicology and Pharmaceutical Science
2
10%
Chemistry
2
10%
Veterinary Science and Veterinary Medicine
1
5%
Other
2
10%
Unknown
4
20%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 08 December 2012.
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