RT info:eu-repo/semantics/article
T1 (E)-Piplartine Isolated from Piper pseudoarboreum, a Lead Compound against Leishmaniasis
A1 Ticona, Juan C.
A1 Bilbao Ramos, Pablo
A1 Flores, Ninoska
A1 Dea Ayuela, M. Auxiliadora
A1 Bolás Fernández, Francisco
A1 Jiménez Díaz, Ignacio Antonio
A1 López Bazzocchi, Isabel
K1 Piper pseudoarboreum
K1 bioassay-guided fractionation
K1 leishmanicidal activity
K1 alkamides
K1 (E)-piplartine
AB The current therapies of leishmaniasis, the second most widespread neglected tropicaldisease, have limited e ectiveness and toxic side e ects. In this regard, natural products play animportant role in overcoming the current need for new leishmanicidal agents. The present studyreports a bioassay-guided fractionation of the ethanolic extract of leaves of Piper pseudoarboreumagainst 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. Compounds2 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 valuesranging 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 bya significant reduction of the lesion size footpad and spleen parasite burden, similar to those ofglucantime used as the reference drug. This study reinforces the therapeutic potential of (E)-piplartineas a promising lead compound against neglected infectious diseases caused by Leishmania parasites
YR 2020
FD 2020
LK http://riull.ull.es/xmlui/handle/915/36033
UL http://riull.ull.es/xmlui/handle/915/36033
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 26-dic-2024