title: Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis.
abstract: Seventeen sesquiterpene lactones (SLs) isolated from five species of the tribe Vernonieae were evaluated for their in vitro activity against promastigotes of Leishmania amazonensis and Leishmania braziliensis. Additionally, a quantitative structure activity relationship has been made, since all these natural compounds were found to have potent to mild antileishmanial properties. The most active compounds against L. braziliensis were 16 and 17 (IC50values 1.45 and 1.34 μM, respectively), followed by compound 15 with IC50value of 1.60 μM against L. amazonensis. The three glaucolide-type SLs (4-6) were the least active against both parasites. The computational study allowed us to establish that lipophilicity and polarisability play an important role in the antiparasitic activity. This is the first report of the known germacradiendiolides 16 and 17 from Elephantopus mollis. The activity data of the compounds 1-17 assayed against Leishmania parasites are reported here for the first time.
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.
authors.forename: Andrea M
authors.initials: AM
authors.lastname: Sosa
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.|b Facultad de Ciencias Exactas y Naturales , Universidad Nacional de Catamarca , Catamarca , Argentina.
authors.forename: Susana
authors.initials: S
authors.lastname: Amaya
authors.affiliation: c Instituto de Investigaciones Fármaco Bioquímicas , Universidad Mayor de San Andrés , La Paz , Bolivia.
authors.forename: Efrain
authors.initials: E
authors.lastname: Salamanca Capusiri
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.|d Instituto de Química del Noroeste Argentino - Consejo Nacional de Investigaciones Científicas y Técnicas (INQUINOA-CONICET) , Tucumán , Argentina.
authors.forename: Miguel
authors.initials: M
authors.lastname: Gilabert
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.|d Instituto de Química del Noroeste Argentino - Consejo Nacional de Investigaciones Científicas y Técnicas (INQUINOA-CONICET) , Tucumán , Argentina.
authors.forename: Alicia
authors.initials: A
authors.lastname: Bardón
authors.affiliation: c Instituto de Investigaciones Fármaco Bioquímicas , Universidad Mayor de San Andrés , La Paz , Bolivia.
authors.forename: Alberto
authors.initials: A
authors.lastname: Giménez
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.
authors.forename: Nancy R
authors.initials: NR
authors.lastname: Vera
authors.affiliation: a Facultad de Bioquímica, Química y Farmacia , Universidad Nacional de Tucumán , Tucumán , Argentina.|b Facultad de Ciencias Exactas y Naturales , Universidad Nacional de Catamarca , Catamarca , Argentina.
authors.forename: Susana A
authors.initials: SA
authors.lastname: Borkosky
keywords: Leishmania amazonensis; Leishmania braziliensis; Vernonieae; antileishmanial activity; sesquiterpene lactones