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Título : E-Piplartine isolated from "Piper pseudoarboreum", a lead compound against "Leishmaniasis"
Autor : Ticona H., Juan Carlos.
Bilbao Ramos, Pablo.
Flores, Ninoska.
Dea Ayuela, María Auxiliadora.
Bolás Fernández, Francisco.
Jiménez Díaz, Ignacio Antonio.
Bazzocchi, Isabel L.
Materias: Leishmaniasis - Treatment.Toxoplasma gondii.Alcaloides.Alkaloids.Piperáceas - Uso terapéutico.Piperaceae - Therapeutic use.Fitoquímica.Botanical chemistry.Herbal medicine.Leishmaniasis - Tratamiento.Communicable diseases - Treatment.Fitoterapia.Giardia lamblia.Cryptosporidium spp.Enfermedades infecciosas - Tratamiento.
Fecha de publicación : 7-sep-2020
Editorial : MDPI.
Citación : Ticona, J.C., Bilbao-Ramos, P., Flores, N., Dea-Ayuela, M.A., Bolás-Fernández, F., Jiménez, I.A. et al. (2020). (E)-Piplartine isolated from "Piper pseudoarboreum", a lead compound against "Leishmaniasis". Foods, vol. 9, i. 9 (07 sep.), art. 1250. DOI: https://doi.org/10.3390/foods9091250
Resumen : The current therapies of leishmaniasis, the second most widespread neglected tropical disease, have limited e ectiveness and toxic side e ects. In this regard, natural products play an important role in overcoming the current need for new leishmanicidal agents. The present study reports a bioassay-guided fractionation of the ethanolic extract of leaves of Piper pseudoarboreum against four species of Leishmania spp. promastigote forms, which a orded six known alkamides (1–6). Their structures were established on the basis of spectroscopic and spectrometric analysis. Compounds 2 and 3 were identified as the most promising ones, displaying higher potency against Leishmania spp. promastigotes (IC50 values ranging from 1.6 to 3.8 M) and amastigotes of L. amazonensis (IC50 values ranging from 8.2 to 9.1 M) than the reference drug, miltefosine. The e cacy of (E)-piplartine (3) against L. amazonensis infection in an in vivo model for cutaneous leishmaniasis was evidenced by a significant reduction of the lesion size footpad and spleen parasite burden, similar to those of glucantime used as the reference drug. This study reinforces the therapeutic potential of (E)-piplartine as a promising lead compound against neglected infectious diseases caused by Leishmania parasites.
Descripción : Este artículo se encuentra disponible en la siguiente URL: https://www.mdpi.com/2304-8158/9/9/1250
Este artículo pertenece al número especial "Isolation and identification of bioactive secondary metabolites".
URI : http://hdl.handle.net/10637/12671
Derechos: http://creativecommons.org/licenses/by/4.0/deed.es
ISSN : 2304-8158 (Electrónico).
Aparece en las colecciones: Dpto. Farmacia

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