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/10362/116628 |
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 liquidMalariaRepurposingRescuingSurface activeMolecular BiologyDrug DiscoveryParasitologySDG 3 - Good Health and Well-beingIonic 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.Global Health and Tropical Medicine (GHTM)Instituto de Higiene e Medicina Tropical (IHMT)Vector borne diseases and pathogens (VBD)RUNSilva, Ana TeresaLobo, LisOliveira, Isabel S.Gomes, JoanaTeixeira, CátiaNogueira, FátimaMarques, Eduardo F.Ferraz, RicardoGomes, Paula2021-05-01T22:52:55Z2020-07-272020-07-27T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article9application/pdfhttp://hdl.handle.net/10362/116628eng1661-6596PURE: 26671128https://doi.org/10.3390/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:RCAAP2024-03-11T04:59:18Zoai:run.unl.pt:10362/116628Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:43:10.816540Repositório 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 Repurposing Rescuing Surface active Molecular Biology Drug Discovery Parasitology SDG 3 - Good Health and Well-being |
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 Lobo, Lis Oliveira, Isabel S. Gomes, Joana Teixeira, Cátia Nogueira, Fátima Marques, Eduardo F. Ferraz, Ricardo Gomes, Paula |
author_role |
author |
author2 |
Lobo, Lis 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 |
Global Health and Tropical Medicine (GHTM) Instituto de Higiene e Medicina Tropical (IHMT) Vector borne diseases and pathogens (VBD) RUN |
dc.contributor.author.fl_str_mv |
Silva, Ana Teresa Lobo, Lis 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 Repurposing Rescuing Surface active Molecular Biology Drug Discovery Parasitology SDG 3 - Good Health and Well-being |
topic |
Antimalarial Chloroquine Ionic liquid Malaria Repurposing Rescuing Surface active Molecular Biology Drug Discovery Parasitology SDG 3 - Good Health and Well-being |
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 |
2020-07-27 2020-07-27T00:00:00Z 2021-05-01T22:52:55Z |
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/10362/116628 |
url |
http://hdl.handle.net/10362/116628 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
1661-6596 PURE: 26671128 https://doi.org/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 |
9 application/pdf |
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 |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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