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Antimalarial activity terpenes

R H Goulart F L D'Alexandre; R Tonhosolo; C S Macedo; A S Couto; E A Kimura; V J Peres; Alejandro Miguel Katzin; Congresso Instituto Ciências Biomédicas, IV (2002 São Paulo)

Resumos São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP, 2002

São Paulo Comissão de Cultura e Extensão Universitária do ICB/USP 2002

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  • Título:
    Antimalarial activity terpenes
  • Autor: R H Goulart
  • F L D'Alexandre; R Tonhosolo; C S Macedo; A S Couto; E A Kimura; V J Peres; Alejandro Miguel Katzin; Congresso Instituto Ciências Biomédicas, IV (2002 São Paulo)
  • Assuntos: HISTOLOGIA; PARASITOLOGIA
  • É parte de: Resumos São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP, 2002
  • Notas Locais: Disponível em CD-ROM
  • Descrição: Malaria represents nowadays one of the most important health problems in the world. It is estimated that almost 300 clinical cases occur every year, with over one million of fatalities (World Health Reported 1999, WHO). This parasite is becoming resistant to most of the drug currently in use in malaria therapeutics, so it is essential to find new drugs targets for the development of new treatments. Recently were demonstrated that the inhibition of isoprenoid pathway in P. falciparum could be an excellent target for develops antimalarial drugs. In our laboratory we are studying the enzymes downstream of isopentenyl-PP (IPP) in isoprenoid pathway, as potential target for develop new antimalarial. We assayed different terpenes in cultures of P. falciparum (isolated NF 54, clone 3 D7). The values of IC50 were: a) nerolidol 760 nM, b) farnesol 64 mM and c) linalool 280 mM. Biosynthesis of dolichol was inhibiting in parasite treated with nerolidol and farnesol in the three-intraerythrocytic stages of P. falciparum. Isoprenic chain attached to coenzyme Q was inhibited when cultures of P. falciparum were treated with nerolidol, but upstream products of the isoprenic pathway (geranyl-PP, farnesyl-PP) were synthesized. One explanation of this observation could be that nerolidol interferes in the elongation involved in the biosynthesis of dolichol and the isoprenic chain attached to benzoquinone ring of coenzyme Q. Antimalarial effects of nerolidol were
    evaluated also in vivo. Balb/C inoculated with 2.5 x 104 ring forms of Plasmodium chabaudi were treated with 30mg/Kg for 7 days. In mice treated with nerolidol, parasitaemia were 50% lower and animals died 2 days after untreated controls. These preliminary results suggest that terpenes could be anew group of antimalarial drugs
  • Editor: São Paulo Comissão de Cultura e Extensão Universitária do ICB/USP
  • Data de criação/publicação: 2002
  • Formato: 1. (várias paginações) poster 121.
  • Idioma: Inglês
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  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

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