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Biomed Res Int. 2018 Apr 4;2018:9781724. doi: 10.1155/2018/9781724. eCollection 2018.

Development of Nanoemulsions to Enhance the Antileishmanial Activity of Copaifera paupera Oleoresins.

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Department of Natural Products and Food, School of Pharmacy, Federal University of Rio de Janeiro, 21941-590 Rio de Janeiro, RJ, Brazil.
Laboratory of Medicinal Plants and Derivatives, Rua Sizenando Nabuco 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
Pharmacy Faculty, Federal Fluminense University, R. Dr. Mario Vianna 523, Santa Rosa, 24241-002 Niterói, RJ, Brazil.
FUNTAC, Av. das Acácias, Lote 01, Zona A, Distrito Industrial, 69917-100 Rio Branco, AC, Brazil.
Chromatography Laboratory, Chemistry Department, Federal University of Amazonas, Av. Rodrigo Otávio 3000, Japiim, 69077-00 Manaus, AM, Brazil.


Based on the ethnopharmacological evidences about the antileishmanial activity of Copaifera spp. oleoresins, the effects of crude extracts and fractions of oleoresin of two specimens from Copaifera paupera were evaluated on Leishmania amazonensis and Leishmania infantum strains. The oleoresin rich in α-copaene (38.8%) exhibited the best activity against L. amazonensis (IC50 = 62.5 μg/mL) and against L. infantum (IC50 = 65.9 μg/mL). The sesquiterpene α-copaene isolated was tested alone and exhibited high antileishmanial activity in vitro with IC50 values for L. amazonensis and L. infantum of 17.2 and 11.4 μg/mL, respectively. In order to increase antileishmanial activity, nanoemulsions containing copaiba oleoresin and α-copaene were developed and assayed against L. amazonensis and L. infantum promastigotes. The nanoemulsion containing α-copaene (NANOCOPAEN) showed the best activity against both species, with IC50 of 2.5 and 2.2 μg/mL, respectively. This is the first report about the antileishmanial activity of α-copaene.

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