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Title: Effects of diterpenes isolated from the Brazilian marine alga Dictyota menstrualis on HIV-1 reverse transcriptase
Authors: Pereira, HDS
Leao-Ferreira, L. R.
Moussatche, N.
Teixeira, V. L.
Cavalcanti, D. N.
Costa, L. J. da
Diaz, R.
Paixao, LCP
Frugulhetti, ICPP
Universidade Federal Fluminense (UFF)
Universidade Federal do Rio de Janeiro (UFRJ)
Universidade Federal de São Paulo (UNIFESP)
Keywords: diterpenes
non-competitive inhibitors
uncompetitive inhibitors
Issue Date: 1-Nov-2005
Publisher: Georg Thieme Verlag Kg
Citation: Planta Medica. Stuttgart: Georg Thieme Verlag Kg, v. 71, n. 11, p. 1019-1024, 2005.
Abstract: 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.
ISSN: 0032-0943
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