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Antileishmanial activity of diterpene acids in copaiba oil
Santos, Adriana Oliveira dos; Izumi, Erika; Ueda-Nakamura, Tânia; Dias-Filho, Benedito Prado; Veiga-Júnior, Valdir Florêncio da; Nakamura, Celso Vataru.
  • Santos, Adriana Oliveira dos; Universidade Estadual de Londrina. Londrina. BR
  • Izumi, Erika; Universidade Estadual de Londrina. Londrina. BR
  • Ueda-Nakamura, Tânia; Universidade Estadual de Londrina. Londrina. BR
  • Dias-Filho, Benedito Prado; Universidade Estadual de Londrina. Londrina. BR
  • Veiga-Júnior, Valdir Florêncio da; Universidade Estadual de Londrina. Londrina. BR
  • Nakamura, Celso Vataru; Universidade Estadual de Londrina. Londrina. BR
Mem. Inst. Oswaldo Cruz ; 108(1): 59-64, Feb. 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-666045
ABSTRACT
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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Full text: Available Index: LILACS (Americas) Main subject: Balsams / Leishmania mexicana / Antiprotozoal Agents Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2013 Type: Article Affiliation country: Brazil Institution/Affiliation country: Universidade Estadual de Londrina/BR

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Full text: Available Index: LILACS (Americas) Main subject: Balsams / Leishmania mexicana / Antiprotozoal Agents Limits: Animals / Humans Language: English Journal: Mem. Inst. Oswaldo Cruz Journal subject: Tropical Medicine / Parasitology Year: 2013 Type: Article Affiliation country: Brazil Institution/Affiliation country: Universidade Estadual de Londrina/BR