RT info:eu-repo/semantics/article
T1 Bio-guided isolation of leishmanicidal and trypanocidal constituents from Pituranthos battandieri aerial parts
A1 Mennai, Imad
A1 Sifaoui, Ines
A1 Esseid, Chahrazed
A1 L´ópez Arencibia, Atteneri
A1 Reyes Batlle, María
A1 Benayache, Fadila
A1 Benayache, Samir
A1 López Bazzocchi, Isabel
A1 Lorenzo Morales, Jacob
A1 Piñero Barroso, José Enrique
A1 Jiménez Díaz, Ignacio Antonio
K1 Pituranthos battandieri
K1 Bioguided isolation
K1 Leishmanicidal
K1 Trypanocidal
K1 Furanocoumarins
K1 Polyacetylenes
AB Protozoan pathogens that cause neglected tropical diseases are a major public health concern in tropical anddeveloping countries. In the course of our ongoing search for new lead compounds as potential antiprotozoalagents, this study aims to perform a bio-guided fractionation of Pituranthos battandieri, using an in vitro assayagainst Leishmania amazonensis and Trypanosoma cruzi. Two known polyacetylenes, (􀀀 )-panaxydiol (1) and(􀀀 )-falcarindiol (2) were identified from the ethanolic extract of the aerial parts of P. battandieri as the mainbioactive constituents. Compounds 1 and 2 showed similar potency (IC50 values of 5.76 and 5.68 μM, respectively)against L. amazonensis to miltefosine (IC50 value of 6.48 μM), the reference drug, and low toxicity onmacrophage cell lines J774. Moreover, compound 1 exhibited moderate activity (IC50 23.24 μM) against T. cruzi.In addition, three known furanocoumarins, 8-geranyloxypsoralen (3), 8-geranyloxy-5-methoxypsoralen (4), andphellopterin (5) were isolated. Their structures were elucidated by NMR and MS analysis. Compounds 1 and 2are described for the first time in the Pituranthos genus, and this is the first report on their antiprotozoal activity.These results highlight this type of polyacetylenes as an interesting scaffold for the development of novel antiparasiticdrugs.
YR 2021
FD 2021
LK http://riull.ull.es/xmlui/handle/915/35931
UL http://riull.ull.es/xmlui/handle/915/35931
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 23-nov-2024