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Pharmaco-toxicological study of diterpenoids
Carla Delporte1, Nadine Backhouse, Pedro Salinas
1Departamento de Química Farmacológica y Toxicológica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, 233, 1-Santiago, Casilla, Chile. cdelpor@uchile.cl
Bioorganic & Medicinal Chemistry
|March 12, 2003
Summary
Andean plants Azorella compacta, Azorella yareta, and Laretia acaulis show anti-inflammatory and analgesic effects. Their diterpenoid compounds, azorellanol and 13-hydroxy-7-oxoazorellane, validated traditional medicine uses without toxicity.
Area of Science:
- Ethnobotany
- Pharmacology
- Natural Product Chemistry
Background:
- Traditional use of Andean Apiaceae species (Azorella compacta, Azorella yareta, Laretia acaulis) for respiratory ailments with inflammation and pain.
- Lack of scientific validation for the therapeutic benefits and toxicity of these medicinal plants.
- Identification of three diterpenoids: azorellanol, 13-hydroxy-7-oxoazorellane, and 7-deacetylazorellanol, previously isolated from these species.
Purpose of the Study:
- To validate the traditional medicinal uses of Azorella compacta, Azorella yareta, and Laretia acaulis.
- To discover novel anti-inflammatory and analgesic molecules from these plant species.
- To evaluate the farmaco-toxicological profile of isolated diterpenoids.
Main Methods:
- Farmaco-toxicological evaluation of azorellanol, 13-hydroxy-7-oxoazorellane, and 7-deacetylazorellanol in mice.
- Assessment of topical anti-inflammatory activity using arachidonic acid (AA) and 12-deoxyphorbol 13-tetradecanoate (TPA) induced edema models.
- Evaluation of analgesic activity and acute toxicity.
Main Results:
- No toxic or side effects were observed in mice for any of the tested compounds.
- All three diterpenoids demonstrated dose-dependent inhibition of pain.
- Azorellanol showed significant topical anti-inflammatory effects comparable to reference drugs, potentially via cyclooxygenase inhibition. 13-hydroxy-7-oxoazorellane was the most potent analgesic.
- 13-hydroxy-7-oxoazorellane exhibited the strongest analgesic effect, though less potent than sodium naproxen.
Conclusions:
- The study scientifically validates the traditional anti-inflammatory and analgesic uses of Azorella compacta, Azorella yareta, and Laretia acaulis.
- Azorellanol and 13-hydroxy-7-oxoazorellane are promising candidates for further development as anti-inflammatory and analgesic agents.
- The findings support the ethnobotanical use of these Andean plants in folk medicine for treating inflammatory conditions.