Anti‐inflammatory and analgesic activities of cupressuflavone from Cupressus macrocarpa: Impact on pro‐inflammatory mediators

Hit, Lead & Candidate Discovery

Inflammation is a complex biological process that is generally occurs in response to pathological triggers. Both neurodegenerative diseases and cancer have been linked to inflammation. The analgesic and anti‐inflammatory effects of cupressuflavone (CUF) isolated from Cupressus macrocarpa were examined. The analgesic effects of CUF (40, 80 and 160 mg/kg po) were assessed in the acetic acid‐induced writhing and hot plate models in mice with diclofenac sodium as the reference standard (100 mg/kg). CUF dose‐dependently inhibited the writhing response in mice by 25, 48, and 62%, at the three CUF doses with 160 mg/kg being equivalent to the diclofenac control. CUF dose‐dependently increased the hot plate model reaction time with a maximal effect after 120 min. In the carrageenan‐induced paw edema model of inflammation, CUF demonstrated anti‐inflammatory activity by inhibiting paw edema by 55, 60, and 64% at doses of 40, 80, and 160 mg/kg po, respectively. CUF also reduced the plasma pro‐inflammatory mediators PGE₂ (44, 54, and 58%), TNF‐α (26, 37, and 53%), IL‐1β (19, 33, and 41%), and IL‐6 (32, 44, and 55%) at the three doses tested with the highest dose having similar effects to diclofenac sodium (100 mg/kg). This finding from this study indicates that CUF has both analgesic and anti‐inflammatory effects.