title: Diplacone and mimulone ameliorate dextran sulfate sodium-induced colitis in rats.
abstract: Diplacone (1) and mimulone (2), two geranylated flavanones, have previously shown anti-inflammatory and antiradical activity in vitro. The present study aimed to evaluate their activity in vivo on a model of colitis induced in Wistar rats by an oral administration of dextran sulfate sodium (DSS). Diplacone (1) and mimulone (2) were administered at a bolus dose of 25mg/kg by gastric gavage 48 and 24h prior to the induction of colitis by DSS and every 24h on the following days of the experiment. The effect of the treatment was assessed by monitoring the disease activity index (DAI), histopathological examination, evaluation of the weight and length of the colon and by analysis of the levels and activities of cyclooxygenase-2 (COX-2), matrix metalloproteinase-2 (MMP2), superoxide dismutase-2 (SOD2), and catalase (CAT) in the inflamed tissue. Administration of the test compounds prior and after induction of colitis ameliorated the symptoms of colitis (diarrhea, presence of the blood in the stool) and delayed their onset. The ability of compounds 1 and 2 to reduce the levels of COX-2 and to increase the ratio of pro-MMP2/MMP2 activity correlates with the values of the DAI. The lowering of the levels of the antioxidant enzymes SOD2 and CAT reflects the ability of the test compounds to scavenge reactive oxygen species.
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Zora
authors.initials: Z
authors.lastname: Vochyánová
authors.affiliation: Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Ladislava
authors.initials: L
authors.lastname: Bartošová
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Veronika
authors.initials: V
authors.lastname: Bujdáková
authors.affiliation: Department of Pathological Morphology and Parasitology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Petr
authors.initials: P
authors.lastname: Fictum
authors.affiliation: Department of Veterinary Clinical Sciences, School of Veterinary Medicine, Louisiana State University, Baton Rouge, LA 70808, USA; International Clinical Research Center (ICRC), St. Anne's University Hospital Brno, Pekařská 53, 656 91 Brno, Czech Republic.
authors.forename: Roman
authors.initials: R
authors.lastname: Husník
authors.affiliation: Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Pavel
authors.initials: P
authors.lastname: Suchý
authors.affiliation: Department of Natural Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic.
authors.forename: Karel
authors.initials: K
authors.lastname: Šmejkal
authors.affiliation: Department of Molecular Biology and Pharmaceutical Biotechnology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, 612 42 Brno, Czech Republic. Electronic address: hosekj@vfu.cz.
authors.forename: Jan
authors.initials: J
authors.lastname: Hošek
mesh_terms: D000818:Animals; D002374:Catalase / Q000378:metabolism; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy*; D003106:Colon / Q000187:drug effects / Q000503:physiopathology; D051546:Cyclooxygenase 2 / Q000378:metabolism; D016264:Dextran Sulfate / Q000009:adverse effects; D004195:Disease Models, Animal; D044950:Flavanones / Q000494:pharmacology*; D008297:Male; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D015394:Molecular Structure; D017208:Rats, Wistar; D013482:Superoxide Dismutase / Q000378:metabolism; D000099156:Superoxide Dismutase 2
chemical_list: D002374:Catalase; D051546:Cyclooxygenase 2; D016264:Dextran Sulfate; D044950:Flavanones; D020778:Matrix Metalloproteinase 2; D013482:Superoxide Dismutase; D000099156:Superoxide Dismutase 2; C000597874:diplacone; C000597872:mimulone; C489691:Ptgs2 protein, rat; C522363:Mmp2 protein, rat
keywords: Dextran sulfate sodium (DSS); Diplacone; Diplacone (PubChem CID: 14539948); Geranylated flavanones; In vivo; Mimulone; Mimulone (PubChem CID: 5716903); Sulfasalazine (PubChem CID: 5353980); Ulcerative colitis