Antimalarial activity terpenes (2002)
- Authors:
- USP affiliated authors: WUNDERLICH, GERHARD - ICB ; KIMURA, EDNA TERUKO - ICB ; KATZIN, ALEJANDRO MIGUEL - ICB
- Unidade: ICB
- Subjects: HISTOLOGIA; PARASITOLOGIA
- Language: Inglês
- Abstract: 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 wereevaluated 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
- Imprenta:
- Publisher: Comissão de Cultura e Extensão Universitária do ICB/USP
- Publisher place: São Paulo
- Date published: 2002
- Source:
- Título do periódico: Resumos
- Conference titles: Congresso Instituto Ciências Biomédicas, IV
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ABNT
GOULART, R H et al. Antimalarial activity terpenes. 2002, Anais.. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP, 2002. . Acesso em: 16 maio 2024. -
APA
Goulart, R. H., D'Alexandre, F. L., Tonhosolo, R., Macedo, C. S., Couto, A. S., Kimura, E. A., et al. (2002). Antimalarial activity terpenes. In Resumos. São Paulo: Comissão de Cultura e Extensão Universitária do ICB/USP. -
NLM
Goulart RH, D'Alexandre FL, Tonhosolo R, Macedo CS, Couto AS, Kimura EA, Peres VJ, Katzin AM. Antimalarial activity terpenes. Resumos. 2002 ;[citado 2024 maio 16 ] -
Vancouver
Goulart RH, D'Alexandre FL, Tonhosolo R, Macedo CS, Couto AS, Kimura EA, Peres VJ, Katzin AM. Antimalarial activity terpenes. Resumos. 2002 ;[citado 2024 maio 16 ] - Characterization of the GGIS encoding geranylgeranyl-isoprenyl synthetase responsable for the isoprenic chain biosynthesis of coenzyme Q of plasmodium falciparum
- Caracterização funcional da farnesil difosfato sintase e efeito de compostos bifosfonatos nos estágios intraeritrocitários de Plasmodium falciparum
- Carotenoid biosynthesis in intraerythrocytic stages of Plasmodium falciparum
- Limonene arrests parasite development and inhibits isoprenylation of proteins in plasmodium falciparum
- Carotenoid biosynthesis in the intraerythrocytic stages of Plasmodium falciparum
- Effect of fosmidomycin on metabolic and transcript profiles of the methylerythritol phosphate pathway in Plasmodium falciparum
- Protein dolichylation in Plasmodium falciparum
- Inhibition of the proteolytic activity of the proteasome by terpenes in cultures of the Plasmodium falciparum
- Identification and characterization of the ge encoding geranylgeranyl synthesis (GGSI) responsable for the isoprenic chain biosynthesis of coenzime Q of P. falciparum
- Carotenoid biosynthesis in intraerythrocytic stages of Plasmodium
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