Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA
Autor(a) principal: | |
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Data de Publicação: | 2010 |
Outros Autores: | , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Journal of the Brazilian Chemical Society (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532010000700011 |
Resumo: | The antitumoral properties of PtII compounds and the favorable characteristics of tetracyclines led us to study PtII compounds of tetracycline (tc) and doxycycline (dox) as candidates for anticancer agents. [PtCl2(dox)], 1, is more potent than [PtCl2(tc)], 2, in inhibiting the growth of chronic myelogenous leukemia cells. Compounds 1 and 2 form a ternary complex with DNA withK values of 3.85×10(4) and 5.43×10(4), respectively. The compounds displace ethidium bromide from DNA sites, which points to an intercalative mechanism. Both complexes decrease DNA eletrophoretic mobility and melting temperature. After incubation of cells with 1 and 2, the DNA was extracted and the adducts formed were quantified. At the concentration that the compounds are cytotoxic to cancer cells, they do not affect macrophages viability. The rate of uptake of the doxycycline complex in cells is three times higher than that of the tetracycline complex and this seems to be determinant for its higher activity. |
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Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNAplatinum(II) compoundscytotoxicitycellular uptakeDNA bindingThe antitumoral properties of PtII compounds and the favorable characteristics of tetracyclines led us to study PtII compounds of tetracycline (tc) and doxycycline (dox) as candidates for anticancer agents. [PtCl2(dox)], 1, is more potent than [PtCl2(tc)], 2, in inhibiting the growth of chronic myelogenous leukemia cells. Compounds 1 and 2 form a ternary complex with DNA withK values of 3.85×10(4) and 5.43×10(4), respectively. The compounds displace ethidium bromide from DNA sites, which points to an intercalative mechanism. Both complexes decrease DNA eletrophoretic mobility and melting temperature. After incubation of cells with 1 and 2, the DNA was extracted and the adducts formed were quantified. At the concentration that the compounds are cytotoxic to cancer cells, they do not affect macrophages viability. The rate of uptake of the doxycycline complex in cells is three times higher than that of the tetracycline complex and this seems to be determinant for its higher activity.Sociedade Brasileira de Química2010-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532010000700011Journal of the Brazilian Chemical Society v.21 n.7 2010reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532010000700011info:eu-repo/semantics/openAccessSilva,Priscila P.Paula,Flávia C. S. deGuerra,WendellSilveira,Josianne N.Botelho,Françoise V.Vieira,Leda Q.Bortolotto,TiagoFischer,Franciele L.Bussi,GiselleTerenzi,HernánPereira-Maia,Elene C.eng2010-07-30T00:00:00Zoai:scielo:S0103-50532010000700011Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2010-07-30T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false |
dc.title.none.fl_str_mv |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
title |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
spellingShingle |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA Silva,Priscila P. platinum(II) compounds cytotoxicity cellular uptake DNA binding |
title_short |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
title_full |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
title_fullStr |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
title_full_unstemmed |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
title_sort |
Platinum(II) compounds of tetracyclines as potential anticancer agents: cytotoxicity, uptake and interactions with DNA |
author |
Silva,Priscila P. |
author_facet |
Silva,Priscila P. Paula,Flávia C. S. de Guerra,Wendell Silveira,Josianne N. Botelho,Françoise V. Vieira,Leda Q. Bortolotto,Tiago Fischer,Franciele L. Bussi,Giselle Terenzi,Hernán Pereira-Maia,Elene C. |
author_role |
author |
author2 |
Paula,Flávia C. S. de Guerra,Wendell Silveira,Josianne N. Botelho,Françoise V. Vieira,Leda Q. Bortolotto,Tiago Fischer,Franciele L. Bussi,Giselle Terenzi,Hernán Pereira-Maia,Elene C. |
author2_role |
author author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Silva,Priscila P. Paula,Flávia C. S. de Guerra,Wendell Silveira,Josianne N. Botelho,Françoise V. Vieira,Leda Q. Bortolotto,Tiago Fischer,Franciele L. Bussi,Giselle Terenzi,Hernán Pereira-Maia,Elene C. |
dc.subject.por.fl_str_mv |
platinum(II) compounds cytotoxicity cellular uptake DNA binding |
topic |
platinum(II) compounds cytotoxicity cellular uptake DNA binding |
description |
The antitumoral properties of PtII compounds and the favorable characteristics of tetracyclines led us to study PtII compounds of tetracycline (tc) and doxycycline (dox) as candidates for anticancer agents. [PtCl2(dox)], 1, is more potent than [PtCl2(tc)], 2, in inhibiting the growth of chronic myelogenous leukemia cells. Compounds 1 and 2 form a ternary complex with DNA withK values of 3.85×10(4) and 5.43×10(4), respectively. The compounds displace ethidium bromide from DNA sites, which points to an intercalative mechanism. Both complexes decrease DNA eletrophoretic mobility and melting temperature. After incubation of cells with 1 and 2, the DNA was extracted and the adducts formed were quantified. At the concentration that the compounds are cytotoxic to cancer cells, they do not affect macrophages viability. The rate of uptake of the doxycycline complex in cells is three times higher than that of the tetracycline complex and this seems to be determinant for its higher activity. |
publishDate |
2010 |
dc.date.none.fl_str_mv |
2010-01-01 |
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=S0103-50532010000700011 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532010000700011 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0103-50532010000700011 |
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.21 n.7 2010 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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1750318171072495616 |