AbstractBackgroundKaurenol, a diterpene alcohol found in Copaifera langsdorffii Desf. (known as “copaiba”), is historically used in traditional medicine for inflammatory conditions.ObjectivesThis study aims to comprehensively assess the potential anti‐inflammatory and antinociceptive properties of kaurenol.MethodsTo this end, the following experiments were conducted to evaluated toxicity: locomotor performance and acute toxicity; nociception: acetic acid‐induced writhing and formalin‐induced antinociception; and anti‐inflammatory activity: carrageenan and dextran‐induced paw edema at 10, 20, and 40 mg/kg, and measurement of nitric oxide (NO), tumor necrosis factor alpha (TNF‐α), interleukin‐6 (IL‐6), and interleukin‐10 (IL‐10) in macrophages at 1, 3, and 9 μg/ml.ResultsKaurenol did not show significant locomotor changes, acute toxicity, and central analgesic activity in the first phase of formalin test at dosages tested. Kaurenol showed 53%, 64%, 64%, and 58% of inhibition in the acetic acid‐induced writhing, second phase of formalin test, carrageenan and dextran‐induced paw edema, respectively.ConclusionThe anti‐inflammatory activity was associated with the regulation of NO release and probably with the regulation of mediators, such as serotonin and prostaglandin in vascular permeability, as well as by being associated with the regulation of IL‐6 and IL‐10. Kaurenol display anti‐inflammatory activity but has no analgesic activity.