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|Title:||GC-MS profiling of the phytochemical constituents of the oleoresin from Copaifera langsdorffii Desf. and a preliminary in vivo evaluation of its antipsoriatic effect.||Authors:||Fabrizio, Gelmini
Roberto Maffei, Facino
|Keywords:||Copaifera langsdorffii Desf.; Chemical composition; GC-MS analysis; Diterpenes and diterpene acids; Cytokines secretion; Nf-kB translocation; Psoriasis||Issue Date:||2013||Project:||None||Journal:||INTERNATIONAL JOURNAL OF PHARMACEUTICS||Abstract:||
Copaiba is the oleoresin (OR) obtained from Copaifera (Fabaceae), a neotropical tree which grows inAmazon regions. The balsam, constituted by an essential oil and a resinous fraction is used as folkloristicremedy in the treatment of several inflammatory diseases and for its antioxidant and antibacterialproperties. Aim of this work was (a) to carry out a characterization by GC–MS of the volatile and nonvolatileconstituents of Copaifera langsdorffii Desf. oleoresin (OR); (b) to investigate the mechanism ofits anti-inflammatory activity; (c) to evaluate its antipsoriatic effect after oral intake/topical application.The volatile fraction (yield: 22.51%, w/w) shows: -bergamotene (48.38%), -himachalene (11.17%), -selinene (5.00%) and -caryophyllene (5.47%). The OR residue (77.49%, w/w), after derivatization, showedas main constituents the following compounds: copalic, abietic, daniellic, lambertinic, labd-7-en-15-oic,pimaric, isopimaric acids and kaur16-en18-oic acid.Preincubation of LPS-stimulated human THP-1 monocytes with increasing concentrations of the ORpurified fraction (OR-PF), containing diterpene acids, diterpenes and sesquiterpenes, reduced the releaseof pro-inflammatory cytokines (IL-1, IL-6, TNF) in a dose-range of 0.1–10 M.In addition, in cell culture system of human THP-1 monocytes, 1 M OR-PF counteracts LPS-drivenNF-B nuclear translocation.In a preliminary clinical trial three patients affected by chronic psoriasis, treated with oral intake ortopical application of the OR, exhibited a significant improvement of the typical signs of this disease, i.e.erythema, skin thickness, and scaliness.In conclusion, the results of this work, beside an extensive analytical characterization of the OR chemicalcomposition, provide strong evidences that its anti-inflammatory activity is related to the inhibition ofthe NF-B nuclear translocation, and consequently of proinflammatory cytokines secretion.
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