Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine

Detalhes bibliográficos
Autor(a) principal: Silva, Ana Teresa
Data de Publicação: 2020
Outros Autores: Lis, Lobo, Oliveira, Isabel S., Gomes, Joana, Teixeira, Cátia, Nogueira, Fátima, Marques, Eduardo F., Ferraz, Ricardo, Gomes, Paula
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10400.22/16528
Resumo: Ionic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug. The most potent ionic liquid was the laurate salt of chloroquine, which presented IC50 values of 4 and 110 nM against a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum, respectively, corresponding to an 11- and 6-fold increase in potency as compared to the reference chloroquine bisphosphate salt against the same strains. This unprecedented report opens new perspectives in both the fields of malaria chemotherapy and of surface-active ionic liquids derived from active pharmaceutical ingredients.
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spelling Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug ChloroquineAntimalarialChloroquineIonic liquidMalariaRescuingRepurposingSurface activeIonic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug. The most potent ionic liquid was the laurate salt of chloroquine, which presented IC50 values of 4 and 110 nM against a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum, respectively, corresponding to an 11- and 6-fold increase in potency as compared to the reference chloroquine bisphosphate salt against the same strains. This unprecedented report opens new perspectives in both the fields of malaria chemotherapy and of surface-active ionic liquids derived from active pharmaceutical ingredients.MDPIRepositório Científico do Instituto Politécnico do PortoSilva, Ana TeresaLis, LoboOliveira, Isabel S.Gomes, JoanaTeixeira, CátiaNogueira, FátimaMarques, Eduardo F.Ferraz, RicardoGomes, Paula2020-12-04T11:16:57Z20202020-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10400.22/16528engSilva, A. T. L., L.; Oliveira, I.S.; Gomes, J.; Teixeira, C.; Nogueira, F.; Marques, E.F.; Ferraz, R.; Gomes, P. (2020). Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine. International Journal of Molecular Sciences, 21(15), 5334. https://doi.org/https://doi.org/10.3390/ijms2115533410.3390/ijms21155334info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-03-13T13:03:41Zoai:recipp.ipp.pt:10400.22/16528Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T17:36:10.973160Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
title Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
spellingShingle Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
Silva, Ana Teresa
Antimalarial
Chloroquine
Ionic liquid
Malaria
Rescuing
Repurposing
Surface active
title_short Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
title_full Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
title_fullStr Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
title_full_unstemmed Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
title_sort Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
author Silva, Ana Teresa
author_facet Silva, Ana Teresa
Lis, Lobo
Oliveira, Isabel S.
Gomes, Joana
Teixeira, Cátia
Nogueira, Fátima
Marques, Eduardo F.
Ferraz, Ricardo
Gomes, Paula
author_role author
author2 Lis, Lobo
Oliveira, Isabel S.
Gomes, Joana
Teixeira, Cátia
Nogueira, Fátima
Marques, Eduardo F.
Ferraz, Ricardo
Gomes, Paula
author2_role author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório Científico do Instituto Politécnico do Porto
dc.contributor.author.fl_str_mv Silva, Ana Teresa
Lis, Lobo
Oliveira, Isabel S.
Gomes, Joana
Teixeira, Cátia
Nogueira, Fátima
Marques, Eduardo F.
Ferraz, Ricardo
Gomes, Paula
dc.subject.por.fl_str_mv Antimalarial
Chloroquine
Ionic liquid
Malaria
Rescuing
Repurposing
Surface active
topic Antimalarial
Chloroquine
Ionic liquid
Malaria
Rescuing
Repurposing
Surface active
description Ionic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug. The most potent ionic liquid was the laurate salt of chloroquine, which presented IC50 values of 4 and 110 nM against a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum, respectively, corresponding to an 11- and 6-fold increase in potency as compared to the reference chloroquine bisphosphate salt against the same strains. This unprecedented report opens new perspectives in both the fields of malaria chemotherapy and of surface-active ionic liquids derived from active pharmaceutical ingredients.
publishDate 2020
dc.date.none.fl_str_mv 2020-12-04T11:16:57Z
2020
2020-01-01T00:00:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10400.22/16528
url http://hdl.handle.net/10400.22/16528
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Silva, A. T. L., L.; Oliveira, I.S.; Gomes, J.; Teixeira, C.; Nogueira, F.; Marques, E.F.; Ferraz, R.; Gomes, P. (2020). Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine. International Journal of Molecular Sciences, 21(15), 5334. https://doi.org/https://doi.org/10.3390/ijms21155334
10.3390/ijms21155334
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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