Anti-ulcerogenic activity of xanthanolide sesquiterpenes from Xanthium cavanillesii in rats
| Autor: | Laura S. Favier, Graciela Haydée Wendel, Carlos E. Tonn, Eduardo Jorge Borkowski, Oscar S. Giordano, Lilian Eugenia Pelzer, A. O. M. María |
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| Rok vydání: | 2005 |
| Předmět: |
Male
Models Molecular Magnetic Resonance Spectroscopy Chemical Phenomena Stereochemistry Molecular Conformation Anti ulcerogenic Biology Pharmacognosy Sesquiterpene Inhibitory postsynaptic potential Xanthium Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Gastric mucosa medicine Animals Sodium Hydroxide Stomach Ulcer Rats Wistar Pharmacology Ethanol Chemistry Physical Plant Extracts Stomach Central Nervous System Depressants Anti-Ulcer Agents biology.organism_classification Rats medicine.anatomical_structure chemistry Hydrochloric Acid Monte Carlo Method Sesquiterpenes |
| Zdroj: | Journal of Ethnopharmacology. 100:260-267 |
| ISSN: | 0378-8741 |
| Popis: | The preventive effect of natural xanthanolides as well as a series of synthetic derivatives on ulcer formation induced by absolute ethanol in rats was examined. Among the compounds tested, xanthatin gave the strongest protective activity. The inhibitory action exerted by this molecule on the lesions induced by 0.6N HCl and 0.2N NaOH was highly significant, reducing ulceration in the range of 58–96% at a dose from 12.5 to 100 mg/kg. These results appear to confirm that the presence of a non-hindered α,β-unsaturated carbonyl group seems to be an essential structural requirement for the gastric cytoprotective activity of these compounds. In order to explore this possibility, a theoretical conformational analysis was performed. We suggest that the mechanism of protection would involve, at least in part, a nucleophylic attack of the sulfhydryl group from the biological molecules present in the gastric mucosa to electrophylic carbons accessible in suitable Michael acceptors. |
| Databáze: | OpenAIRE |
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