Pharmaco-toxicological study of diterpenoids

Delporte, Carla; Backhouse, Nadine; Salinas, Pedro; San-Martı́n, Aurelio; Bórquez, Jorge; Loyola, Alberto

doi:10.1016/s0968-0896(02)00645-4

Cited by 35 publications

(25 citation statements)

References 9 publications

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“…where Wc and Ws are the different median values of the weights of the right and the left ear sections of the control and the treated animals, respectively [32].…”

Section: Topical Anti-inflammatory Effectmentioning

confidence: 99%

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

et al. 2015

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Abstract:The 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 OPEN ACCESSMolecules 2015, 20 11220 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.

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“…where Wc and Ws are the different median values of the weights of the right and the left ear sections of the control and the treated animals, respectively [32].…”

Section: Topical Anti-inflammatory Effectmentioning

confidence: 99%

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

et al. 2015

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“…Table 3 shows the results for the pharmacological assays of the various extracts, together with the maximum effect of SN for the per os antiinflammatory and analgesic activities, and the antiinflammatory dermal maximum effect of nimesulide (NM) and indomethacin (IND) (Delporte et al, 2003).…”

Section: Antiinflammatory (Per Os and Topic) And Analgesic Propertiesmentioning

confidence: 99%

Analgesic–antiinflammatory properties of Proustia pyrifolia

Delporte

Backhouse

Erazo

et al. 2005

Journal of Ethnopharmacology

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“…1) (Loyola et al 1990a(Loyola et al , b, 1991(Loyola et al , 1996(Loyola et al , 1997a(Loyola et al , b, 1998(Loyola et al , 2002. These diterpenoids have displayed a wide variety of interesting biological activities, including antiprotozoal (Neira et al 1998;Loyola et al 2001aLoyola et al , b, 2004, antibacterial (Wächter et al 1999), antiviral (Abdel-Malek et al 1996, spermicidal (Morales et al 2003), cytotoxic (Mongelli et al 1997(Mongelli et al , 2000, antihyperglycemic (Fuentes et al 2005), antiinflammatory and analgesic (Delporte et al 2003;Bórquez et al 2007), and at least one mulinane diterpenoid, 9,12-cyclomulin-13-ol (1), has been reported as having antituberculosis activity (Wächter et al 1998). As a result of this, and as part of a project directed towards the search for natural antituberculosis agents, we have recently investigated the in vitro antituberculosis activity of a series of natural and semisynthetic azorellane and mulinane diterpenoids, when tested against two strains of Mycobacterium tuberculosis using the Alamar-blue assay (MolinaSalinas et al 2006(MolinaSalinas et al , 2010a.…”

Section: Introductionmentioning

confidence: 99%

Bioactive metabolites from the Andean flora. Antituberculosis activity of natural and semisynthetic azorellane and mulinane diterpenoids

et al. 2010

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Natural products are recognized as an important source of new and better pharmaceuticals for the treatment of diseases such as tuberculosis. The azorellane and mulinane diterpenoids represent an interesting group of bioactive metabolites produced by Andean plants belonging to the Azorella, Mulinum, Laretia and Bolax genus. Testing of natural and semisynthetic azorellanes and mulinanes against two Mycobacterium tuberculosis strains showed that while most changes in the structure of the natural metabolites result in the loss of antituberculosis activity, methylation of the C-20 carboxyl group improves the biological activity of the corresponding derivatives.

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Pharmaco-toxicological study of diterpenoids

Cited by 35 publications

References 9 publications

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

Analgesic–antiinflammatory properties of Proustia pyrifolia

Bioactive metabolites from the Andean flora. Antituberculosis activity of natural and semisynthetic azorellane and mulinane diterpenoids

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