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

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dc.contributor.authorPereira, HDS
dc.contributor.authorLeao-Ferreira, L. R.
dc.contributor.authorMoussatche, N.
dc.contributor.authorTeixeira, V. L.
dc.contributor.authorCavalcanti, D. N.
dc.contributor.authorCosta, L. J. da
dc.contributor.authorDiaz, R.
dc.contributor.authorPaixao, LCP
dc.contributor.authorFrugulhetti, ICPP
dc.contributor.institutionUniversidade Federal Fluminense (UFF)
dc.contributor.institutionUniversidade Federal do Rio de Janeiro (UFRJ)
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.date.accessioned2016-01-24T12:38:09Z
dc.date.available2016-01-24T12:38:09Z
dc.date.issued2005-11-01
dc.description.abstractIt 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.en
dc.description.affiliationUniv Fed Fluminense, Dept Biol Celular & Mol, Programa Neuroimunol, Niteroi, RJ, Brazil
dc.description.affiliationUniv Fed Fluminense, Inst Biol, Dept Biol Marinha, Niteroi, RJ, Brazil
dc.description.affiliationUniv Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, BR-21941 Rio de Janeiro, Brazil
dc.description.affiliationUniversidade Federal de São Paulo, UNIFESP, EPM, São Paulo, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, UNIFESP, EPM, São Paulo, Brazil
dc.description.sourceWeb of Science
dc.format.extent1019-1024
dc.identifierhttp://dx.doi.org/10.1055/s-2005-873113
dc.identifier.citationPlanta Medica. Stuttgart: Georg Thieme Verlag Kg, v. 71, n. 11, p. 1019-1024, 2005.
dc.identifier.doi10.1055/s-2005-873113
dc.identifier.issn0032-0943
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/28535
dc.identifier.wosWOS:000233940800006
dc.language.isoeng
dc.publisherGeorg Thieme Verlag Kg
dc.relation.ispartofPlanta Medica
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectditerpenesen
dc.subjectHIV-1 RTen
dc.subjectAMV-RTen
dc.subjectMMLV-RTen
dc.subjectnon-competitive inhibitorsen
dc.subjectuncompetitive inhibitorsen
dc.titleEffects of diterpenes isolated from the Brazilian marine alga Dictyota menstrualis on HIV-1 reverse transcriptaseen
dc.typeinfo:eu-repo/semantics/article
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