Intestinal anti-inflammatory activity of coumarin and 4-hydroxycoumarin in the trinitrobenzenesulphonic acid model of rat colitis.
Coumarins represent an important class of phenolic compounds with multiple biological activities, including inhibition of lipidic peroxidation and neutrophil-dependent anion superoxide generation, anti-inflammatory and immunosuppressor actions. All of these proprieties are essential for that a drug may be used in the treatment of inflammatory bowel disease. The present study examined intestinal anti-inflammatory activity of coumarin and its derivative, the 4-hydroxycoumarin on experimental ulcerative colitis in rats. This was performed in two different experimental settings, i.e. when the colonic mucosa is intact or when the mucosa is in process of recovery after an initial insult. The results obtained revealed that the coumarin and 4-hydroxycoumarin, at doses of 5 and 25 mg/kg, significantly attenuated the colonic damage induced by trinitrobenzenesulphonic acid (TNBS) in both situations, as evidenced macroscopically, microscopically and biochemically. This effect was related to an improvement in the colonic oxidative status, since coumarin and 4-hydroxycoumarin prevented the glutathione depletion that occurred as a consequence of the colonic inflammation.
Luchini
Ana Carolina
AC
Laboratory of Phytomedicines, Department of Pharmacology, Instituto de Biociências, São Paulo State University (UNESP), Botucatu, SP, Brazil.
Rodrigues-Orsi
Patrícia
P
Cestari
Silvia Helena
SH
Seito
Leonardo Noboru
LN
Witaicenis
Aline
A
Pellizzon
Claudia Helena
CH
Di Stasi
Luiz Cláudio
LC
D015110:4-Hydroxycoumarins / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000208:Acute Disease; D000469:Alkaline Phosphatase / Q000378:metabolism; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use; D002908:Chronic Disease; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D003106:Colon / Q000473:pathology; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D003967:Diarrhea / Q000139:chemically induced / Q000517:prevention & control; D005765:Gastrointestinal Agents / Q000494:pharmacology; D005978:Glutathione / Q000378:metabolism; D008297:Male; D009929:Organ Size / Q000187:drug effects; D009195:Peroxidase / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D055502:Secondary Prevention; D012460:Sulfasalazine / Q000494:pharmacology; D014302:Trinitrobenzenesulfonic Acid
D015110:4-Hydroxycoumarins; D000893:Anti-Inflammatory Agents; D003374:Coumarins; D005765:Gastrointestinal Agents; D012460:Sulfasalazine; D014302:Trinitrobenzenesulfonic Acid; C030123:coumarin; D009195:Peroxidase; D000469:Alkaline Phosphatase; D005978:Glutathione; C068805:4-hydroxycoumarin