Estimation of the Anti-inflammatory Effect of Coumarin Derivatives

Abstract

Background: Inflammation is the body’s natural defense mechanism for removing noxious stimuli. According to the benzopyran substitutions, Coumarins are extensively dispersed in nature and have varied biological effects. Purpose: The purpose of this study is to estimate the anti-inflammatory effect of some Coumarin derivatives using RAW 264.7 macrophage cell lines including the inhibitory effect of these derivatives on cyclooxygenase-2 enzyme, interleukin-1β, and interleukin-6. Methods: In the present investigation, RAW 264.7 cells were treated with varying concentrations (0.15-100μM) of three Coumarin derivatives. After 72 hours, the half-maximal inhibitory concentration (IC50) was determined using the MTT assay to assess the cytotoxicity of these derivatives. The levels of cyclooxygenase-2, interleukin-1β, and interleukin-6 were also evaluated using the ELISA technique. Results: The half–maximal inhibitory concentrations for C1, C2, C3, and Diclofenac were 32 μM, 25.09 μM, 12.2 μM, and 30.42 μM, respectively. At concentrations 2.5, 5, 7.5, and 10 mg/ml of these derivatives, cyclooxygenase-2 activity was decreased significantly by C2 and C3 more than the Diclofenac (Reference compound) (p˂0.05). C2 and C3 significantly reduced the level of interleukin-1β induced by lipopolysaccharide compared with the lipopolysaccharide alone (p˂0.05). The inhibitory effects of C1, C2 and C3 were significantly more potent on interleukin-6 level induced by lipopolysaccharide compared with lipopolysaccharide alone (p˂0.05).Conclusions: C2 and C3 had better anti-inflammatory effects than Diclofenac as they had a significantly higher inhibitory effect on the cyclooxygenase-2 activity than the inhibitory activity of Diclofenac and significantly inhibited interleukin-1β and interleukin-6 induced by lipopolysaccharide compared with the lipopolysaccharide (LPS) alone.