In Vitro Susceptibility of Leishmania infantum to Artemisinin Derivatives and Selected Trioxolanes

Leishmaniasis is among the world's most neglected diseases. Currently available drugs for treatment present drawbacks, urging the need for more effective, safer, and cheaper drugs. A small library of artemisinin-derived trioxanes and synthetic trioxolanes was tested against promastigote and int...

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Published inAntimicrobial agents and chemotherapy Vol. 59; no. 8; pp. 5032 - 5035
Main Authors Cortes, Sofia, Albuquerque, Andreia, Cabral, Lília I L, Lopes, Liliana, Campino, Lenea, Cristiano, Maria L S
Format Journal Article
LanguageEnglish
Published United States American Society for Microbiology 01.08.2015
Subjects
Antiparasitic Agents
Antiparasitic Agents - pharmacology
Artemisinins
Artemisinins - pharmacology
Cell Proliferation - drug effects
Drug Resistance, Multiple
Heterocyclic Compounds, 1-Ring
Heterocyclic Compounds, 1-Ring - pharmacology
Humans
Leishmania infantum
Leishmania infantum - drug effects
Leishmaniasis
Leishmaniasis - drug therapy
Macrophages - parasitology
Parasitic Sensitivity Tests
Spiro Compounds
Spiro Compounds - pharmacology
Susceptibility
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Summary:Leishmaniasis is among the world's most neglected diseases. Currently available drugs for treatment present drawbacks, urging the need for more effective, safer, and cheaper drugs. A small library of artemisinin-derived trioxanes and synthetic trioxolanes was tested against promastigote and intramacrophage amastigote forms of Leishmania infantum. The trioxolanes LC50 and LC95 presented the best activity and safety profiles, showing potential for further studies in the context of leishmanial therapy. Our results indicate that the compounds tested exhibit peroxide-dependent activity.
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S.C., A.A., and L.I.L.C. contributed equally to this work.
Citation Cortes S, Albuquerque A, Cabral LIL, Lopes L, Campino L, Cristiano MLS. 2015. In vitro susceptibility of Leishmania infantum to artemisinin derivatives and selected trioxolanes. Antimicrob Agents Chemother 59:5032–5035. doi:10.1128/AAC.00298-15.
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.00298-15