Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells

Detalhes bibliográficos
Autor(a) principal: Amaro,Bolivar R.
Data de Publicação: 2020
Outros Autores: Alves,Caio C. S., Ferreira,Gabriella F., Carvalho,Paloma E., Silva,Jeferson G. da, Souza,Cleonice A., Cardoso Jr.,Oswaldo, Carli,Alessandra P., Machado,Fabiana S., Denadai,Ângelo M. L., Castro,Sandra B. R.
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=S0103-50532020001202628
Resumo: The ofloxacin (OFLOX) is a second-generation synthetic antibiotic that can be classified as a multifunctional drug, but is a poorly soluble drug, which influences its efficiency. The inclusion complexes of OFLOX with β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD) can improve the chemical characteristics of the drug; however, studies showing the biological activity of these inclusion complexes are still scarce. The present work aimed to investigate the multifunctionality of the OFLOX and their inclusion complexes. Thus, the 1:1 βCD/OFLOX or HPβCD/OFLOX were prepared and analyzed by Fourier transform infrared spectroscopy (FTIR), thermogravimetric and differential thermal analysis (TGA and DTA), 1H nuclear magnetic resonance (NMR) and isothermal titration calorimetry (ITC). The antitumor and antibacterial effects were assessed. The results confirm the formation of the inclusion complexes, which had lower minimum inhibitory concentration (MIC) values, higher cytotoxicity and promoted the apoptosis. The present study showed, for the first time, the promising effects of the inclusion complexes as antitumor, improving the biological activities of the uncomplexed ofloxacin.
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spelling Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 CellscomplexationMTTflow cytometrytoxicityMICThe ofloxacin (OFLOX) is a second-generation synthetic antibiotic that can be classified as a multifunctional drug, but is a poorly soluble drug, which influences its efficiency. The inclusion complexes of OFLOX with β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD) can improve the chemical characteristics of the drug; however, studies showing the biological activity of these inclusion complexes are still scarce. The present work aimed to investigate the multifunctionality of the OFLOX and their inclusion complexes. Thus, the 1:1 βCD/OFLOX or HPβCD/OFLOX were prepared and analyzed by Fourier transform infrared spectroscopy (FTIR), thermogravimetric and differential thermal analysis (TGA and DTA), 1H nuclear magnetic resonance (NMR) and isothermal titration calorimetry (ITC). The antitumor and antibacterial effects were assessed. The results confirm the formation of the inclusion complexes, which had lower minimum inhibitory concentration (MIC) values, higher cytotoxicity and promoted the apoptosis. The present study showed, for the first time, the promising effects of the inclusion complexes as antitumor, improving the biological activities of the uncomplexed ofloxacin.Sociedade Brasileira de Química2020-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532020001202628Journal of the Brazilian Chemical Society v.31 n.12 2020reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.21577/0103-5053.20200145info:eu-repo/semantics/openAccessAmaro,Bolivar R.Alves,Caio C. S.Ferreira,Gabriella F.Carvalho,Paloma E.Silva,Jeferson G. daSouza,Cleonice A.Cardoso Jr.,OswaldoCarli,Alessandra P.Machado,Fabiana S.Denadai,Ângelo M. L.Castro,Sandra B. R.eng2020-12-09T00:00:00Zoai:scielo:S0103-50532020001202628Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2020-12-09T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false
dc.title.none.fl_str_mv Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
title Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
spellingShingle Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
Amaro,Bolivar R.
complexation
MTT
flow cytometry
toxicity
MIC
title_short Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
title_full Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
title_fullStr Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
title_full_unstemmed Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
title_sort Multifunctionality of βCD/Ofloxacin and HPβCD/Ofloxacin Complexes: Improvement of the Antimicrobial Activity and Apoptosis Induction on Lung Adenocarcinoma A549 Cells
author Amaro,Bolivar R.
author_facet Amaro,Bolivar R.
Alves,Caio C. S.
Ferreira,Gabriella F.
Carvalho,Paloma E.
Silva,Jeferson G. da
Souza,Cleonice A.
Cardoso Jr.,Oswaldo
Carli,Alessandra P.
Machado,Fabiana S.
Denadai,Ângelo M. L.
Castro,Sandra B. R.
author_role author
author2 Alves,Caio C. S.
Ferreira,Gabriella F.
Carvalho,Paloma E.
Silva,Jeferson G. da
Souza,Cleonice A.
Cardoso Jr.,Oswaldo
Carli,Alessandra P.
Machado,Fabiana S.
Denadai,Ângelo M. L.
Castro,Sandra B. R.
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Amaro,Bolivar R.
Alves,Caio C. S.
Ferreira,Gabriella F.
Carvalho,Paloma E.
Silva,Jeferson G. da
Souza,Cleonice A.
Cardoso Jr.,Oswaldo
Carli,Alessandra P.
Machado,Fabiana S.
Denadai,Ângelo M. L.
Castro,Sandra B. R.
dc.subject.por.fl_str_mv complexation
MTT
flow cytometry
toxicity
MIC
topic complexation
MTT
flow cytometry
toxicity
MIC
description The ofloxacin (OFLOX) is a second-generation synthetic antibiotic that can be classified as a multifunctional drug, but is a poorly soluble drug, which influences its efficiency. The inclusion complexes of OFLOX with β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD) can improve the chemical characteristics of the drug; however, studies showing the biological activity of these inclusion complexes are still scarce. The present work aimed to investigate the multifunctionality of the OFLOX and their inclusion complexes. Thus, the 1:1 βCD/OFLOX or HPβCD/OFLOX were prepared and analyzed by Fourier transform infrared spectroscopy (FTIR), thermogravimetric and differential thermal analysis (TGA and DTA), 1H nuclear magnetic resonance (NMR) and isothermal titration calorimetry (ITC). The antitumor and antibacterial effects were assessed. The results confirm the formation of the inclusion complexes, which had lower minimum inhibitory concentration (MIC) values, higher cytotoxicity and promoted the apoptosis. The present study showed, for the first time, the promising effects of the inclusion complexes as antitumor, improving the biological activities of the uncomplexed ofloxacin.
publishDate 2020
dc.date.none.fl_str_mv 2020-12-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532020001202628
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532020001202628
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.21577/0103-5053.20200145
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.31 n.12 2020
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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