Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , , , , |
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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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 |
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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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1817552116880769024 |