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: Lobo, Lis, 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/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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spelling 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
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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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
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