In vitro and in vivo antimalarial potential of oleoresin obtained from Copaifera reticulata Ducke (Fabaceae) in the Brazilian Amazon rainforest.
BACKGROUND
In view of the wide variety of the flora of the Amazon region, many plants have been studied in the search for new antimalarial agents. Copaifera reticulata is a tree distributed throughout the Amazon region which contains an oleoresin rich in sesquiterpenes and diterpenes with β-caryophyllene as the major compound. The oleoresin has demonstrated antiparasitic activity against Leishmania amazonensis. Because of this previously reported activity, this oleoresin would be expected to also have antimalarial activity.


OBJECTIVE
In this study we evaluated the in vitro and in vivo antimalarial potential of C. reticulata oleoresin.


METHODS
In vitro assays were done using P. falciparum W2 and 3D7 strains and the human fibroblast cell line 26VA Wi-4. For in vivo analysis, BALB/c mice were infected with approximately 106erythrocytes parasitized by P. berghei and their parasitemia levels were observed over 7 days of treatment with C. reticulata; hematological and biochemical parameters were analyzed at the end of experiment.


RESULTS
The oleoresin of C. reticulata containing the sesquiterpenes β-caryophyllene (41.7%) and β-bisabolene (18.6%) was active against the P. falciparum W2 and 3D7 strains (IC50= 1.66 and 2.54 µg/ml, respectively) and showed low cytotoxicity against the 26VA Wi-4 cell line (IC50> 100 µg/ml). The C. reticulata oleoresin reduced the parasitemia levels of infected animals and doses of 200 and 100 mg/kg/day reached a rate of parasitemia elimination resembling that obtained with artemisinin 100 mg/kg/day. In addition, treatment with oleoresin improved the hypoglycemic, hematologic, hepatic and renal parameters of the infected animals.


CONCLUSIONS
The oleoresin of C. reticulata has antimalarial properties and future investigations are necessary to elucidate its mechanism of action.
Laboratório de Farmacologia Experimental, Universidade Federal do Oeste do Pará - UFOPA, Brazil.
Giovana A G
GA
de Souza
Laboratório de Farmacologia Experimental, Universidade Federal do Oeste do Pará - UFOPA, Brazil.
Nazaré C
NC
da Silva
Laboratório de Farmacologia, Instituto Esperança de Ensino Superior - IESPES, Brazil.
Juarez
J
de Souza
Laboratório de Neurofarmacologia Experimental, Universidade Federal do Pará - UFPA, Brazil.
Karen R M
KR
de Oliveira
Laboratório de Bioquímica Medicinal, Universidade Federal de São João del-Rei - UFSJ, Brazil.
Amanda L
AL
da Fonseca
Faculdade de Farmácia, Universidade Federal do Rio de Janeiro - UFRJ, Brazil. Electronic address: leopoldo@pharma.ufrj.br.
Leopoldo C
LC
Baratto
Laboratório de Biotecnologia Vegetal, Universidade Federal do Oeste do Pará - UFOPA, Brazil.
Elaine C P
EC
de Oliveira
Laboratório de Bioquímica Medicinal, Universidade Federal de São João del-Rei - UFSJ, Brazil.
Fernando de Pilla
FP
Varotti
Laboratório de Farmacologia Experimental, Universidade Federal do Oeste do Pará - UFOPA, Brazil.
Waldiney P
WP
Moraes
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology / Q000627:therapeutic use*; D001938:Brazil; D002460:Cell Line; D007887:Fabaceae / Q000737:chemistry*; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology*; D010962:Plasmodium berghei / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects*; D065947:Rainforest
D000962:Antimalarials; D010936:Plant Extracts; C018620:oleoresins
Antimalarial activity; Copaifera reticulata; Malaria; Oleoresin; Plasmodium berghei; Plasmodium falciparum