In vivo activity of pseudoguaianolide sesquiterpene lactones in acute and chronic inflammation
Autor: | José-Luis Ríos, J. R. de la Fuente, Salvador Máñez, Rosa-María Giner, M. Cerdá, L. Uriburu, María-Carmen Recio |
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Rok vydání: | 2000 |
Předmět: |
Pharmacology
Sesquiterpene lactone General Biochemistry Genetics and Molecular Biology chemistry.chemical_compound Mice In vivo Edema medicine Animals General Pharmacology Toxicology and Pharmaceutics Dexamethasone chemistry.chemical_classification Inflammation biology Chemistry Anti-Inflammatory Agents Non-Steroidal General Medicine Plants Carrageenan Myeloperoxidase Tetradecanoylphorbol Acetate Immunology Acute Disease Chronic Disease biology.protein Arachidonic acid Female medicine.symptom Sesquiterpenes medicine.drug |
Zdroj: | Life sciences. 66(26) |
ISSN: | 0024-3205 |
Popis: | The pseudoguaianolide sesquiterpene lactones 4-alpha-O-acetyl-pseudoguaian-6beta-olide (1), hymenin (2), ambrosanolide (3), tetraneurin A (4), parthenin (5), hysterin (6) and confertdiolide (7) were evaluated for their ability to affect the inflammation responses induced by different agents. All the compounds showed activity against the 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced mouse ear edema. The ethyl phenylpropiolate (EPP)-induced mouse ear edema was inhibited by compounds 3, 5 and 7. However, when sesquiterpene-lactones were assayed on the arachidonic acid (AA)-induced mouse ear edema, none of them were active. The only sesquiterpene lactone orally active against the paw mouse edema induced by carrageenan was 7, which gave a 46% edema inhibition after 3 h. On the other hand, compounds 3, 5 and 7 reduced the serotonin-induced paw edema in mice, although compound 7 was inactive in presence of cycloheximide. In addition, the sesquiterpene lactones were assayed against the chronic inflammation induced by repeated application of TPA on mouse ear. Confertdiolide was the most active compound; it reduced the edema by 87% and had a more moderate effect against the leukocyte recruitment (36% reduction in myeloperoxidase (MPO) levels). A histological study of ear the samples treated with 7 presented no detectable morphological lesions such as those treated with dexamethasone. On the oxazolone-induced delayed type hypersensitivity (DTH) only compounds 4 and 5 were active 24 h after the challenge. Compound 5 affected polymorphonuclear leukocyte infiltration (69% reduction in MPO levels). The results suggest that the especial chemical structure and spatial conformation of confertdiolide may facilitate its anti-inflammatory effect. |
Databáze: | OpenAIRE |
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