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Antileishmanial activity of diterpene acids in copaiba oil
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 centur...
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Published in: | Memórias do Instituto Oswaldo Cruz 2013-02, Vol.108 (1), p.59-64 |
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Main Authors: | , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | 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. |
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ISSN: | 1678-8060 0074-0276 1678-8060 0074-0276 |
DOI: | 10.1590/S0074-02762013000100010 |