Evaluation of anti-inflammatory activity of kaurenol: Experimental evaluation and mechanistic insights

Fundam Clin Pharmacol. 2024 Apr;38(2):252-261. doi: 10.1111/fcp.12957. Epub 2023 Sep 21.

Abstract

Background: Kaurenol, a diterpene alcohol found in Copaifera langsdorffii Desf. (known as "copaiba"), is historically used in traditional medicine for inflammatory conditions.

Objectives: This study aims to comprehensively assess the potential anti-inflammatory and antinociceptive properties of kaurenol.

Methods: To 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.

Results: Kaurenol 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.

Conclusion: The 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.

Keywords: Copaifera langsdorffii; antiedematogenic activity; diterpene alcohol; nociception.

MeSH terms

  • Acetic Acid / adverse effects
  • Analgesics / toxicity
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Carrageenan
  • Dextrans / adverse effects
  • Diterpenes* / adverse effects
  • Edema / chemically induced
  • Edema / drug therapy
  • Humans
  • Interleukin-10*
  • Interleukin-6
  • Pain / chemically induced
  • Pain / drug therapy
  • Plant Extracts / pharmacology

Substances

  • Carrageenan
  • Interleukin-10
  • kaur-16-en-15-ol
  • Interleukin-6
  • Dextrans
  • Anti-Inflammatory Agents
  • Analgesics
  • Diterpenes
  • Plant Extracts
  • Acetic Acid