Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin
Autor(a) principal: | |
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Data de Publicação: | 2011 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Revista Brasileira de Farmacognosia (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2011000600005 |
Resumo: | Cancer constitutes the second main mortality cause in the world, after cardiovascular diseases. In spite of the progresses in the chemotherapeutics treatments, many patients fail chemotherapy, mainly because of side effects or multi-drugs resistance, proving the need and importance of the research for new molecules with anticancer activity, more effective and with smaller adverse effects. Various compounds derived from plant secondary metabolites are commonly used in the chemotherapy against cancer and the natural products play an important role in the research for new molecules. Among several molecules of natural origin evaluated by MTT assay in murine tumor cell lines [breast (LM3) and lung (LP07)] the quinona-methide triterpenes tingenone and pristimerin showed marked cytotoxic activity presenting IC50 around 2 and 5 µM respectively. The structure-activity relationship suggests that rings A and B containing an α, ß-unsaturated carbonyl group are essential for the observed cytotoxic activity. The interaction between these positions and acetylcisteyne residues suggests a probable mechanism of action. The in vitro mutagenic activity was also evaluated by the Salmonella microsome assay (Ames test) for pristimerin and tingenone with and without metabolic activation (S9) in the strains TA98, TA97a, TA100 and TA102, none of which showed mutagenic potential in any strains. Estrogenic and anti-estrogenic activities were also studied by the e-screen assay in MCF-7 cells with negative results. The present data point to the importance of pristimerin and tingenone as representative of an emerging class of potential anticancer chemicals. |
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Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin(anti)estrogenic activitycytotoxic activitymutagenic activityplumericinpristimerintingenoneCancer constitutes the second main mortality cause in the world, after cardiovascular diseases. In spite of the progresses in the chemotherapeutics treatments, many patients fail chemotherapy, mainly because of side effects or multi-drugs resistance, proving the need and importance of the research for new molecules with anticancer activity, more effective and with smaller adverse effects. Various compounds derived from plant secondary metabolites are commonly used in the chemotherapy against cancer and the natural products play an important role in the research for new molecules. Among several molecules of natural origin evaluated by MTT assay in murine tumor cell lines [breast (LM3) and lung (LP07)] the quinona-methide triterpenes tingenone and pristimerin showed marked cytotoxic activity presenting IC50 around 2 and 5 µM respectively. The structure-activity relationship suggests that rings A and B containing an α, ß-unsaturated carbonyl group are essential for the observed cytotoxic activity. The interaction between these positions and acetylcisteyne residues suggests a probable mechanism of action. The in vitro mutagenic activity was also evaluated by the Salmonella microsome assay (Ames test) for pristimerin and tingenone with and without metabolic activation (S9) in the strains TA98, TA97a, TA100 and TA102, none of which showed mutagenic potential in any strains. Estrogenic and anti-estrogenic activities were also studied by the e-screen assay in MCF-7 cells with negative results. The present data point to the importance of pristimerin and tingenone as representative of an emerging class of potential anticancer chemicals.Sociedade Brasileira de Farmacognosia2011-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2011000600005Revista Brasileira de Farmacognosia v.21 n.6 2011reponame:Revista Brasileira de Farmacognosia (Online)instname:Sociedade Brasileira de Farmacognosia (SBFgnosia)instacron:SBFGNOSIA10.1590/S0102-695X2011005000153info:eu-repo/semantics/openAccessGomes,Juliana P. M.Cardoso,Cássia R. P.Varanda,Eliana A.Molina,José-ManuelFernandez,Mariana F.Olea,Nicolásarlos,Iracilda Z.Vilegas,Wagnereng2011-10-18T00:00:00Zoai:scielo:S0102-695X2011000600005Revistahttp://www.sbfgnosia.org.br/revista/https://old.scielo.br/oai/scielo-oai.phprbgnosia@ltf.ufpb.br1981-528X0102-695Xopendoar:2011-10-18T00:00Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia)false |
dc.title.none.fl_str_mv |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
title |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
spellingShingle |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin Gomes,Juliana P. M. (anti)estrogenic activity cytotoxic activity mutagenic activity plumericin pristimerin tingenone |
title_short |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
title_full |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
title_fullStr |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
title_full_unstemmed |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
title_sort |
Antitumoral, mutagenic and (anti)estrogenic activities of tingenone and pristimerin |
author |
Gomes,Juliana P. M. |
author_facet |
Gomes,Juliana P. M. Cardoso,Cássia R. P. Varanda,Eliana A. Molina,José-Manuel Fernandez,Mariana F. Olea,Nicolás arlos,Iracilda Z. Vilegas,Wagner |
author_role |
author |
author2 |
Cardoso,Cássia R. P. Varanda,Eliana A. Molina,José-Manuel Fernandez,Mariana F. Olea,Nicolás arlos,Iracilda Z. Vilegas,Wagner |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Gomes,Juliana P. M. Cardoso,Cássia R. P. Varanda,Eliana A. Molina,José-Manuel Fernandez,Mariana F. Olea,Nicolás arlos,Iracilda Z. Vilegas,Wagner |
dc.subject.por.fl_str_mv |
(anti)estrogenic activity cytotoxic activity mutagenic activity plumericin pristimerin tingenone |
topic |
(anti)estrogenic activity cytotoxic activity mutagenic activity plumericin pristimerin tingenone |
description |
Cancer constitutes the second main mortality cause in the world, after cardiovascular diseases. In spite of the progresses in the chemotherapeutics treatments, many patients fail chemotherapy, mainly because of side effects or multi-drugs resistance, proving the need and importance of the research for new molecules with anticancer activity, more effective and with smaller adverse effects. Various compounds derived from plant secondary metabolites are commonly used in the chemotherapy against cancer and the natural products play an important role in the research for new molecules. Among several molecules of natural origin evaluated by MTT assay in murine tumor cell lines [breast (LM3) and lung (LP07)] the quinona-methide triterpenes tingenone and pristimerin showed marked cytotoxic activity presenting IC50 around 2 and 5 µM respectively. The structure-activity relationship suggests that rings A and B containing an α, ß-unsaturated carbonyl group are essential for the observed cytotoxic activity. The interaction between these positions and acetylcisteyne residues suggests a probable mechanism of action. The in vitro mutagenic activity was also evaluated by the Salmonella microsome assay (Ames test) for pristimerin and tingenone with and without metabolic activation (S9) in the strains TA98, TA97a, TA100 and TA102, none of which showed mutagenic potential in any strains. Estrogenic and anti-estrogenic activities were also studied by the e-screen assay in MCF-7 cells with negative results. The present data point to the importance of pristimerin and tingenone as representative of an emerging class of potential anticancer chemicals. |
publishDate |
2011 |
dc.date.none.fl_str_mv |
2011-12-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2011000600005 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2011000600005 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0102-695X2011005000153 |
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 Farmacognosia |
publisher.none.fl_str_mv |
Sociedade Brasileira de Farmacognosia |
dc.source.none.fl_str_mv |
Revista Brasileira de Farmacognosia v.21 n.6 2011 reponame:Revista Brasileira de Farmacognosia (Online) instname:Sociedade Brasileira de Farmacognosia (SBFgnosia) instacron:SBFGNOSIA |
instname_str |
Sociedade Brasileira de Farmacognosia (SBFgnosia) |
instacron_str |
SBFGNOSIA |
institution |
SBFGNOSIA |
reponame_str |
Revista Brasileira de Farmacognosia (Online) |
collection |
Revista Brasileira de Farmacognosia (Online) |
repository.name.fl_str_mv |
Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia) |
repository.mail.fl_str_mv |
rbgnosia@ltf.ufpb.br |
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1752122466158772224 |