Protective effect of bergapten in acetic acid-induced colitis in rats

Abstract

Bergapten (5-methoxysporalen) is a furanocoumarin extracted from several species of citrus and bergamot oil. Bergamot essential oil is used traditionally in the management of inflammatory conditions. Previous studies on bergapten have explored mainly its in vitro anti-inflammatory activities which include suppression of the expression and release of pro-inflammatory cytokines such as TNF-α and interleukins as well as prostaglandins. Bergapten enhances the clearance of neutrophils and macrophages from the site of inflammation and reduces oxidative stress by inhibition of reactive oxygen species (ROS). Bergapten was assessed for its anti-inflammatory properties in acetic acid-induced colitis. Animals were obtained and randomly placed in six (6) groups (n = 5) after acclimatization. Colitis was induced by rectal administration using 4% v / v acetic acid in Sprague Dawley rats after pre-treatment for 5 days. Bergapten was administered at doses of 3, 10, and 30 mg kg −1 p.o . while the control group received saline 5 mL kg −1 p.o. and the standard drug employed was sulphasalazine at a dose of 500 mg kg −1 . Assessments made for colon-weight-to-length ratio, colonic injury, and mucosal mast cell degranulation. There were reduced colon-weight-to-length ratios in animals treated with bergapten which was significant ( p < 0.5 ) for doses 10 and 30 mg kg −1 compared to the disease control group Both macroscopic and microscopic damage were reduced as well, with a lesser percentage of degranulated mast cells. Macroscopic damage was reduced for bergapten at doses 10 and 30 mg kg −1 significantly at p < 0.5 and p < 0.001, respectively. Similarly, microscopic damage was reduced at p < 0.01 and p < 0.001 respectively for bergapten 10 and 30 mg kg −1 . The reduction of degranulation by bergapten was significant at p < 0.001 . There was generally reduced damage at inflammatory sites as well as decreased infiltration of inflammatory cells. Overall, bergapten reduces inflammation in acetic acid-induced colitis.

Pharmacological Properties of Bergapten: Mechanistic and Therapeutic Aspects

“…In another study, the anti-inflammatory effects of BP were investigated in a rat model of acetic acid-induced colitis [ 34 ]. Oral administration of BP (3, 10, and 30 mg/kg) normalized colon weight-to-length and significantly reduced tissue damage and the number of degranulated mast cells.…”

Protective Effect of Bergapten against Human Erythrocyte Hemolysis and Protein Denaturation In Vitro

“…Bergapten (5-methoxypsoralen), a furocoumarin found in medicinal plants, has become a compound of considerable interest in current research [ 16 , 17 ]. Accumulated reports have demonstrated the potential therapeutic effects of bergapten in various disease conditions including psoriasis and vitiligo [ 18 , 19 ], Alzheimer's disease (AD) [ 20 ], depression [ 21 ], osteoporosis [ 22 ], cancer [ 23 ], colitis [ 24 ], and asthma [ 25 ]. Prior in vitro studies on human peripheral blood mononuclear cells (PBMCs) showed that bergapten could suppress the release of lipopolysaccharide- (LPS-) stimulated proinflammatory cytokines such as tumour necrosis factor-alpha (TNF- α ) and interleukin 6 (IL-6) production [ 26 ].…”

Mesenchymal stem cells have ameliorative effect on the colitis model via Nrf2/HO-1 pathway

“…Macroscopic changes in colon related to acetic acid include thickening of intestinal walls, ulceration, and necrosis. Mucosal lining damage, necrosis of tissues with hemorrhages, goblet cells loss, and infiltration of inflammatory cells have been reported in histopathological examination of colitis 12 , 13 , 28 . Biochemical results revealed significant increase in inflammatory cytokines IL-1β, TNF-α, IL-6 and also decrease in IL-10 29 .…”