Artículo
Assessment of sesquiterpene lactones isolated from Mikania plants species for their potential efficacy against Trypanosoma cruzi and Leishmania sp
Laurella, Laura Cecilia; Cerny, Natacha
; Bivona, Augusto Ernesto
; Sanchez Alberti, Andrés
; Giberti, Gustavo Carlos
; Malchiodi, Emilio Luis
; Martino, Virginia Susana
; Catalan, Cesar Atilio Nazareno
; Alonso, Maria del Rosario
; Cazorla, Silvia Ines
; Sülsen, Valeria Patricia
Fecha de publicación:
09/2017
Editorial:
Public Library of Science
Revista:
Neglected Tropical Diseases
e-ISSN:
1935-2735
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Four sesquiterpene lactones, mikanolide, deoxymikanolide, dihydromikanolide and scandenolide, were isolated by a bioassay-guided fractionation of Mikania variifolia and Mikania micrantha dichloromethane extracts. Mikanolide and deoxymikanolide were the major compounds in both extracts (2.2% and 0.4% for Mikania variifolia and 21.0% and 6.4% for Mikania micrantha respectively, calculated on extract dry weight). Mikanolide, deoxymikanolide and dihydromikanolide were active against Trypanosoma cruzi epimastigotes (50% inhibitory concentrations of 0.7, 0.08 and 2.5 μg/mL, for each compound respectively). These sesquiterpene lactones were also active against the bloodstream trypomastigotes (50% inhibitory concentrations for each compound were 2.1, 1.5 and 0.3 μg/mL, respectively) and against amastigotes (50% inhibitory concentrations for each compound were 4.5, 6.3 and 8.5 μg/mL, respectively). By contrast, scandenolide was not active on Trypanosoma cruzi. Besides, mikanolide and deoxymikanolide were also active on Leishmania braziliensis promastigotes (50% inhibitory concentrations of 5.1 and 11.5 μg/mL, respectively). The four sesquiterpene lactones were tested for their cytotoxicity on THP 1 cells. Deoxymikanolide presented the highest selectivity index for trypomastigotes (SI = 54) and amastigotes (SI = 12.5). In an in vivo model of Trypanosoma cruzi infection, deoxymikanolide was able to decrease the parasitemia and the weight loss associated to the acute phase of the parasite infection. More importantly, while 100% of control mice died by day 22 after receiving a lethal T. cruzi infection, 70% of deoxymikanolide-treated mice survived. We also observed that this compound increased TNF-α and IL-12 production by macrophages, which could contribute to control T. cruzi infection.
Palabras clave:
Mikania
,
Sesquiterpene
,
Lactones
,
Trypanosoma
,
Cruzi
,
Leishmania
Archivos asociados
Licencia
Identificadores
Colecciones
Articulos(CERELA)
Articulos de CENTRO DE REFERENCIA PARA LACTOBACILOS (I)
Articulos de CENTRO DE REFERENCIA PARA LACTOBACILOS (I)
Articulos(IDEHU)
Articulos de INST.DE EST.DE LA INMUNIDAD HUMORAL PROF.R.A.MARGNI
Articulos de INST.DE EST.DE LA INMUNIDAD HUMORAL PROF.R.A.MARGNI
Articulos(IQUIMEFA)
Articulos de INST.QUIMICA Y METABOLISMO DEL FARMACO (I)
Articulos de INST.QUIMICA Y METABOLISMO DEL FARMACO (I)
Citación
Laurella, Laura Cecilia; Cerny, Natacha; Bivona, Augusto Ernesto; Sanchez Alberti, Andrés; Giberti, Gustavo Carlos; et al.; Assessment of sesquiterpene lactones isolated from Mikania plants species for their potential efficacy against Trypanosoma cruzi and Leishmania sp; Public Library of Science; Neglected Tropical Diseases; 11; 9; 9-2017; 1-16; e0005929
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