Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis
This work reports the results of the in vitro assay against extracellular forms of Leishmania (viannia) braziliensis of eleven dibenzylbutyrolactone derivatives, either isolated from plants or obtained by synthesis. From these, only two showed relative biological activity against the parasite, the raceme mixtures of methylpluviatolide: IC50 = 496 mM and (-)-6,6'- dinitrocubebin: IC50 = 510,4 μM. Thus, it can be suggested that the metabolic pathway responsible for the biological activity of these compounds against this parasite genera differs from the one related to Trypanosoma cruzi, for which these compounds were quite active. This fact highly also suggests that this class of compounds is more selective against T. cruzi. Nevertheles, other lignans derivatives should be obtained to allow the fully evaluation of this class of lignans against Leishmaniosis.
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Sociedade Brasileira de Farmacognosia
2003
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oai:scielo:S0102-695X20030004000072009-09-25Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensisRoyo,V.A.Santos,F.F.Souza,V.A.Pereira,A.C.Da Silva,R.Vinhólis,A.H.C.Donate,P.M.Silva,M.L.A.Albuquerque,S.Bastos,J.K.This work reports the results of the in vitro assay against extracellular forms of Leishmania (viannia) braziliensis of eleven dibenzylbutyrolactone derivatives, either isolated from plants or obtained by synthesis. From these, only two showed relative biological activity against the parasite, the raceme mixtures of methylpluviatolide: IC50 = 496 mM and (-)-6,6'- dinitrocubebin: IC50 = 510,4 μM. Thus, it can be suggested that the metabolic pathway responsible for the biological activity of these compounds against this parasite genera differs from the one related to Trypanosoma cruzi, for which these compounds were quite active. This fact highly also suggests that this class of compounds is more selective against T. cruzi. Nevertheles, other lignans derivatives should be obtained to allow the fully evaluation of this class of lignans against Leishmaniosis.info:eu-repo/semantics/openAccessSociedade Brasileira de FarmacognosiaRevista Brasileira de Farmacognosia v.13 suppl.2 20032003-01-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2003000400007en10.1590/S0102-695X2003000400007 |
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Royo,V.A. Santos,F.F. Souza,V.A. Pereira,A.C. Da Silva,R. Vinhólis,A.H.C. Donate,P.M. Silva,M.L.A. Albuquerque,S. Bastos,J.K. |
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Royo,V.A. Santos,F.F. Souza,V.A. Pereira,A.C. Da Silva,R. Vinhólis,A.H.C. Donate,P.M. Silva,M.L.A. Albuquerque,S. Bastos,J.K. Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
author_facet |
Royo,V.A. Santos,F.F. Souza,V.A. Pereira,A.C. Da Silva,R. Vinhólis,A.H.C. Donate,P.M. Silva,M.L.A. Albuquerque,S. Bastos,J.K. |
author_sort |
Royo,V.A. |
title |
Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
title_short |
Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
title_full |
Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
title_fullStr |
Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
title_full_unstemmed |
Biological activity evaluation of dibenzilbutirolactones lignans derivatives against Leishmania braziliensis |
title_sort |
biological activity evaluation of dibenzilbutirolactones lignans derivatives against leishmania braziliensis |
description |
This work reports the results of the in vitro assay against extracellular forms of Leishmania (viannia) braziliensis of eleven dibenzylbutyrolactone derivatives, either isolated from plants or obtained by synthesis. From these, only two showed relative biological activity against the parasite, the raceme mixtures of methylpluviatolide: IC50 = 496 mM and (-)-6,6'- dinitrocubebin: IC50 = 510,4 μM. Thus, it can be suggested that the metabolic pathway responsible for the biological activity of these compounds against this parasite genera differs from the one related to Trypanosoma cruzi, for which these compounds were quite active. This fact highly also suggests that this class of compounds is more selective against T. cruzi. Nevertheles, other lignans derivatives should be obtained to allow the fully evaluation of this class of lignans against Leishmaniosis. |
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Sociedade Brasileira de Farmacognosia |
publishDate |
2003 |
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http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2003000400007 |
work_keys_str_mv |
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1756399198924701696 |