Antileishmanial activity of diterpene acids in copaiba oil

Memórias do Instituto Oswaldo Cruz

Adriana Oliveira Dos Santos²  Erika Izumi²  Tânia Ueda-nakamura²  Benedito Prado Dias-filho²  Valdir Florêncio Da Veiga-júnior¹  Celso Vataru Nakamura² 

[1] ,Universidade Estadual de LondrinaLondrina PR ,Brasil

关键词: Leishmania amazonensis;    leishmaniasis;    Copaifera;    diterpene acids;   

DOI  :  10.1590/S0074-02762013000100010

来源: SciELO

【 摘 要 】

Leishmaniasis is a neglected tropical disease. According to the World Health Organization, there are approximately 1.5-two million new cases of cutaneous leishmaniasis each year worldwide. Chemotherapy against leishmaniasis is based on pentavalent antimonials, which were developed more than a century ago. The goals of this study were to investigate the antileishmanial activity of diterpene acids in copaiba oil, as well as some possible targets of their action against Leishmania amazonensis. Methyl copalate and agathic, hydroxycopalic, kaurenoic, pinifolic and polyaltic acids isolated from Copaifera officinales oleoresins were utilised. Ultrastructural changes and the specific organelle targets of diterpenes were investigated with electron microscopy and flow cytometry, respectively. All compounds had some level of activity against L. amazonensis. Hydroxycopalic acid and methyl copalate demonstrated the most activity against promastigotes and had 50% inhibitory concentration (IC50) values of 2.5 and 6.0 µg/mL, respectively. However, pinifolic and kaurenoic acid demonstrated the most activity against axenic amastigote and had IC50 values of 3.5 and 4.0 µg/mL, respectively. Agathic, kaurenoic and pinifolic acid caused significant increases in plasma membrane permeability and mitochondrial membrane depolarisation of the protozoan. In conclusion, copaiba oil and its diterpene acids should be explored for the development of new antileishmanial drugs.

【 授权许可】

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