Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line
Autor(a) principal: | |
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Data de Publicação: | 2009 |
Outros Autores: | , , , , , , |
Tipo de documento: | Relatório |
Idioma: | eng |
Título da fonte: | Journal of the Brazilian Chemical Society (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000300024 |
Resumo: | Activity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6α-acetoxi 7β-hydroxy-vouacapan 1 and four known diterpene furans 2, 3, 4, 5. The compounds were evaluated for in vitro cytotoxic activities against human normal cells and tumour cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-H460 (lung, non-small cells), OVCAR-03 (ovarian), PC-3 (prostate), HT-29 (colon), 786-0 (renal), K562 (leukemia) and NCI-ADR/RES (ovarian expressing phenotype multiple drugs resistance). Results were expressed by three concentration dependent parameters GI50 (concentration that produces 50% growth inhibition), TGI (concentration that produces total growth inhibition or cytostatic effect) and LC50 (concentration that produces -50% growth, a cytotoxicity parameter). Also, in vitro cytotoxicity was evaluated against 3T3 cell line (mouse embryonic fibroblasts). Antiproliferative properties of compounds 1, 4 and 5 are herein reported for the first time. These compounds showed selectivity in a concentration-dependent way against human PC-3. Compound 1 demonstrated selectivity 26 fold more potent than the positive control, doxorubicin, for PC-3 (prostrate) cell line based on GI50 values, causing cytostatic effect (TGI value) at a concentration fifteen times less than positive control. Moreover comparison of 50% lethal concentration (LC50 value) with positive control (doxorubicin) suggested that compound 1 was less toxic. |
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Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell linePterodon pubescensleguminosaefuranoditerpenesin vitro assayprostate cell linecytotoxicityActivity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6α-acetoxi 7β-hydroxy-vouacapan 1 and four known diterpene furans 2, 3, 4, 5. The compounds were evaluated for in vitro cytotoxic activities against human normal cells and tumour cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-H460 (lung, non-small cells), OVCAR-03 (ovarian), PC-3 (prostate), HT-29 (colon), 786-0 (renal), K562 (leukemia) and NCI-ADR/RES (ovarian expressing phenotype multiple drugs resistance). Results were expressed by three concentration dependent parameters GI50 (concentration that produces 50% growth inhibition), TGI (concentration that produces total growth inhibition or cytostatic effect) and LC50 (concentration that produces -50% growth, a cytotoxicity parameter). Also, in vitro cytotoxicity was evaluated against 3T3 cell line (mouse embryonic fibroblasts). Antiproliferative properties of compounds 1, 4 and 5 are herein reported for the first time. These compounds showed selectivity in a concentration-dependent way against human PC-3. Compound 1 demonstrated selectivity 26 fold more potent than the positive control, doxorubicin, for PC-3 (prostrate) cell line based on GI50 values, causing cytostatic effect (TGI value) at a concentration fifteen times less than positive control. Moreover comparison of 50% lethal concentration (LC50 value) with positive control (doxorubicin) suggested that compound 1 was less toxic.Sociedade Brasileira de Química2009-01-01info:eu-repo/semantics/reportinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000300024Journal of the Brazilian Chemical Society v.20 n.3 2009reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532009000300024info:eu-repo/semantics/openAccessSpindola,Humberto M.Carvalho,João E. deRuiz,Ana Lúcia T. G.Rodrigues,Rodney A. F.Denny,CarinaSousa,Ilza M. de OliveiraTamashiro,Jorge Y.Foglio,Mary Anneng2009-05-25T00:00:00Zoai:scielo:S0103-50532009000300024Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2009-05-25T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false |
dc.title.none.fl_str_mv |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
title |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
spellingShingle |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line Spindola,Humberto M. Pterodon pubescens leguminosae furanoditerpenes in vitro assay prostate cell line cytotoxicity |
title_short |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
title_full |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
title_fullStr |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
title_full_unstemmed |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
title_sort |
Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line |
author |
Spindola,Humberto M. |
author_facet |
Spindola,Humberto M. Carvalho,João E. de Ruiz,Ana Lúcia T. G. Rodrigues,Rodney A. F. Denny,Carina Sousa,Ilza M. de Oliveira Tamashiro,Jorge Y. Foglio,Mary Ann |
author_role |
author |
author2 |
Carvalho,João E. de Ruiz,Ana Lúcia T. G. Rodrigues,Rodney A. F. Denny,Carina Sousa,Ilza M. de Oliveira Tamashiro,Jorge Y. Foglio,Mary Ann |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Spindola,Humberto M. Carvalho,João E. de Ruiz,Ana Lúcia T. G. Rodrigues,Rodney A. F. Denny,Carina Sousa,Ilza M. de Oliveira Tamashiro,Jorge Y. Foglio,Mary Ann |
dc.subject.por.fl_str_mv |
Pterodon pubescens leguminosae furanoditerpenes in vitro assay prostate cell line cytotoxicity |
topic |
Pterodon pubescens leguminosae furanoditerpenes in vitro assay prostate cell line cytotoxicity |
description |
Activity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6α-acetoxi 7β-hydroxy-vouacapan 1 and four known diterpene furans 2, 3, 4, 5. The compounds were evaluated for in vitro cytotoxic activities against human normal cells and tumour cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-H460 (lung, non-small cells), OVCAR-03 (ovarian), PC-3 (prostate), HT-29 (colon), 786-0 (renal), K562 (leukemia) and NCI-ADR/RES (ovarian expressing phenotype multiple drugs resistance). Results were expressed by three concentration dependent parameters GI50 (concentration that produces 50% growth inhibition), TGI (concentration that produces total growth inhibition or cytostatic effect) and LC50 (concentration that produces -50% growth, a cytotoxicity parameter). Also, in vitro cytotoxicity was evaluated against 3T3 cell line (mouse embryonic fibroblasts). Antiproliferative properties of compounds 1, 4 and 5 are herein reported for the first time. These compounds showed selectivity in a concentration-dependent way against human PC-3. Compound 1 demonstrated selectivity 26 fold more potent than the positive control, doxorubicin, for PC-3 (prostrate) cell line based on GI50 values, causing cytostatic effect (TGI value) at a concentration fifteen times less than positive control. Moreover comparison of 50% lethal concentration (LC50 value) with positive control (doxorubicin) suggested that compound 1 was less toxic. |
publishDate |
2009 |
dc.date.none.fl_str_mv |
2009-01-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/report |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
report |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000300024 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000300024 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0103-50532009000300024 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
text/html |
dc.publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
dc.source.none.fl_str_mv |
Journal of the Brazilian Chemical Society v.20 n.3 2009 reponame:Journal of the Brazilian Chemical Society (Online) instname:Sociedade Brasileira de Química (SBQ) instacron:SBQ |
instname_str |
Sociedade Brasileira de Química (SBQ) |
instacron_str |
SBQ |
institution |
SBQ |
reponame_str |
Journal of the Brazilian Chemical Society (Online) |
collection |
Journal of the Brazilian Chemical Society (Online) |
repository.name.fl_str_mv |
Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ) |
repository.mail.fl_str_mv |
||office@jbcs.sbq.org.br |
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1750318169802670080 |