Highly active ozonides selected against drug resistant malaria

Detalhes bibliográficos
Autor(a) principal: Lobo, Lis
Data de Publicação: 2016
Outros Autores: Sousa, Bruno de, Cabral, Lília, Cristiano, Maria L. S., Nogueira, Fátima
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10316/46910
https://doi.org/10.1590/0074-02760160077
Resumo: Ever increasing multi-drug resistance by Plasmodium falciparum is creating new challenges in malaria chemotherapy. In the absence of licensed vaccines, treatment and prevention of malaria is heavily dependent on drugs. Potency, range of activity, safety, low cost and ease of administration are crucial issues in the design and formulation of antimalarials. We have tested three synthetic ozonides NAC89, LC50 and LCD67 in vitro and in vivo against multidrug resistant Plasmodium. In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin. All three ozonides showed high efficacy in clearing parasitaemia in mice, caused by multi-drug resistant Plasmodium chabaudi strains, by subcutaneous administration, demonstrating high efficacy in vivo against ART and artesunate resistant parasites.
id RCAP_bf893eef4401eb3dec9f5d1eafca2d60
oai_identifier_str oai:estudogeral.uc.pt:10316/46910
network_acronym_str RCAP
network_name_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository_id_str 7160
spelling Highly active ozonides selected against drug resistant malariaAnimalsAntimalarialsArtemisininsChloroquineDisease Models, AnimalFemaleHumansMalaria, FalciparumMefloquineMiceParasitemiaPlasmodium falciparumEver increasing multi-drug resistance by Plasmodium falciparum is creating new challenges in malaria chemotherapy. In the absence of licensed vaccines, treatment and prevention of malaria is heavily dependent on drugs. Potency, range of activity, safety, low cost and ease of administration are crucial issues in the design and formulation of antimalarials. We have tested three synthetic ozonides NAC89, LC50 and LCD67 in vitro and in vivo against multidrug resistant Plasmodium. In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin. All three ozonides showed high efficacy in clearing parasitaemia in mice, caused by multi-drug resistant Plasmodium chabaudi strains, by subcutaneous administration, demonstrating high efficacy in vivo against ART and artesunate resistant parasites.2016info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/46910http://hdl.handle.net/10316/46910https://doi.org/10.1590/0074-02760160077engLobo, LisSousa, Bruno deCabral, LíliaCristiano, Maria L. S.Nogueira, Fátimainfo: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:RCAAP2021-08-20T10:36:31Zoai:estudogeral.uc.pt:10316/46910Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:53:01.110336Repositório 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 Highly active ozonides selected against drug resistant malaria
title Highly active ozonides selected against drug resistant malaria
spellingShingle Highly active ozonides selected against drug resistant malaria
Lobo, Lis
Animals
Antimalarials
Artemisinins
Chloroquine
Disease Models, Animal
Female
Humans
Malaria, Falciparum
Mefloquine
Mice
Parasitemia
Plasmodium falciparum
title_short Highly active ozonides selected against drug resistant malaria
title_full Highly active ozonides selected against drug resistant malaria
title_fullStr Highly active ozonides selected against drug resistant malaria
title_full_unstemmed Highly active ozonides selected against drug resistant malaria
title_sort Highly active ozonides selected against drug resistant malaria
author Lobo, Lis
author_facet Lobo, Lis
Sousa, Bruno de
Cabral, Lília
Cristiano, Maria L. S.
Nogueira, Fátima
author_role author
author2 Sousa, Bruno de
Cabral, Lília
Cristiano, Maria L. S.
Nogueira, Fátima
author2_role author
author
author
author
dc.contributor.author.fl_str_mv Lobo, Lis
Sousa, Bruno de
Cabral, Lília
Cristiano, Maria L. S.
Nogueira, Fátima
dc.subject.por.fl_str_mv Animals
Antimalarials
Artemisinins
Chloroquine
Disease Models, Animal
Female
Humans
Malaria, Falciparum
Mefloquine
Mice
Parasitemia
Plasmodium falciparum
topic Animals
Antimalarials
Artemisinins
Chloroquine
Disease Models, Animal
Female
Humans
Malaria, Falciparum
Mefloquine
Mice
Parasitemia
Plasmodium falciparum
description Ever increasing multi-drug resistance by Plasmodium falciparum is creating new challenges in malaria chemotherapy. In the absence of licensed vaccines, treatment and prevention of malaria is heavily dependent on drugs. Potency, range of activity, safety, low cost and ease of administration are crucial issues in the design and formulation of antimalarials. We have tested three synthetic ozonides NAC89, LC50 and LCD67 in vitro and in vivo against multidrug resistant Plasmodium. In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin. All three ozonides showed high efficacy in clearing parasitaemia in mice, caused by multi-drug resistant Plasmodium chabaudi strains, by subcutaneous administration, demonstrating high efficacy in vivo against ART and artesunate resistant parasites.
publishDate 2016
dc.date.none.fl_str_mv 2016
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/10316/46910
http://hdl.handle.net/10316/46910
https://doi.org/10.1590/0074-02760160077
url http://hdl.handle.net/10316/46910
https://doi.org/10.1590/0074-02760160077
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
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
_version_ 1799133817003311104

Registros relacionados