Effects of diterpenes isolated from the Brazilian marine alga Dictyota menstrualis on HIV-1 reverse transcriptase

Effects of diterpenes isolated from the Brazilian marine alga Dictyota menstrualis on HIV-1 reverse transcriptase

Autor Pereira, HDS Google Scholar
Leao-Ferreira, L. R. Google Scholar
Moussatche, N. Google Scholar
Teixeira, V. L. Google Scholar
Cavalcanti, D. N. Google Scholar
Costa, L. J. da Google Scholar
Diaz, R. Google Scholar
Paixao, LCP Google Scholar
Frugulhetti, ICPP Google Scholar
Instituição Universidade Federal Fluminense (UFF)
Universidade Federal do Rio de Janeiro (UFRJ)
Universidade Federal de São Paulo (UNIFESP)
Resumo It has been recently demonstrated that HIV-1 reverse transcriptase is the target of two diterpenes, (6R)-6-hydroxydichotoma3,14-diene-1,17-dial (compound 1) and (6R)-6-acetoxydichotoma-3,14-diene-1,17-dial (compound 2), that inhibit HIV-1 replication in vitro. in this work, the effects of both diterpenes on the kinetic properties of the recombinant HIV-1 reverse transcriptase (RT) enzyme were evaluated. RNA-dependent DNA-polymerase (RDDP) activity assays demonstrated that both diterpenes behave as non-competitive inhibitors with respect to dTTP and uncompetitive inhibitors with respect to poly(rA).oligo(dT) template primers. the K, values obtained for compounds 1 and 2 were 10 and 35 mu M, respectively. Neither of these diterpenes affected the DNA-dependent DNA-polymerase (DDDP) activity of the HIV-1 RT. the RDDP activities of AMV-RTand MMLV-RT enzymes were also inhibited by compounds 1 and 2. in contrast to the HIV-1 enzyme, the DDDP activities of AMV-RT and MMLV-RT enzymes were significantly reduced by compound 1. Taken together, our results demonstrate that compound 1 is a more effective inhibitor of the viral reverse transcriptases from HIV-1, AMV and MMLV than compound 2. the kinetic behavior analyses of the HIV-1 RT demonstrate that both diterpenes have similar mechanisms of inhibition of RDDP activity.
Palavra-chave diterpenes
HIV-1 RT
AMV-RT
MMLV-RT
non-competitive inhibitors
uncompetitive inhibitors
Idioma Inglês
Data de publicação 2005-11-01
Publicado em Planta Medica. Stuttgart: Georg Thieme Verlag Kg, v. 71, n. 11, p. 1019-1024, 2005.
ISSN 0032-0943 (Sherpa/Romeo, fator de impacto)
Publicador Georg Thieme Verlag Kg
Extensão 1019-1024
Fonte http://dx.doi.org/10.1055/s-2005-873113
Direito de acesso Acesso restrito
Tipo Artigo
Web of Science WOS:000233940800006
Endereço permanente http://repositorio.unifesp.br/handle/11600/28535

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