Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs
AbstractThe aim of the study was to assess changes in the activity of anti-inflammatory terpenes from Chilean medicinal plants after the formation of derivatives incorporating synthetic anti-inflammatory agents. Ten new hybrid molecules were synthesized combining terpenes (ferruginol (1), imbricatolic acid (2) and oleanolic acid (3)) with ibuprofen (4) or naproxen (5). The topical anti-inflammatory activity of the compounds was assessed in mice by the arachidonic acid (AA) and 12-O-tetradecanoyl phorbol 13-acetate (TPA) induced ear edema assays. Basal cytotoxicity was determined towards human lung fibroblasts, gastric epithelial cells and hepatocytes. At 1.4 µmol/mouse, a strong anti-inflammatory effect in the TPA assay was observed for oleanoyl ibuprofenate 12 (79.9%) and oleanoyl ibuprofenate methyl ester 15 (80.0%). In the AA assay, the best activity was observed for 12 at 3.2 µmol/mouse, with 56.8% reduction of inflammation, in the same range as nimesulide (48.9%). All the terpenyl-synthetic anti-inflammatory hybrids showed better effects in the TPA assay, with best activity for 6, 12 and 15. The cytotoxicity of the compounds 8 and 10 with a free COOH, was higher than that of 2. The derivatives from 3 were less toxic than the triterpene. Several of the new compounds presented better anti-inflammatory effect and lower cytotoxicity than the parent terpenes. View Full-Text
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Theoduloz, C.; Delporte, C.; Valenzuela-Barra, G.; Silva, X.; Cádiz, S.; Bustamante, F.; Pertino, M.W.; Schmeda-Hirschmann, G. Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs. Molecules 2015, 20, 11219-11235.
Theoduloz C, Delporte C, Valenzuela-Barra G, Silva X, Cádiz S, Bustamante F, Pertino MW, Schmeda-Hirschmann G. Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs. Molecules. 2015; 20(6):11219-11235.Chicago/Turabian Style
Theoduloz, Cristina; Delporte, Carla; Valenzuela-Barra, Gabriela; Silva, Ximena; Cádiz, Solange; Bustamante, Fernanda; Pertino, Mariano W.; Schmeda-Hirschmann, Guillermo. 2015. "Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs." Molecules 20, no. 6: 11219-11235.