RT info:eu-repo/semantics/article
T1 New phenalenone analogues with improved activity against Leishmania species.
A1 López Arencibia, Atteneri
A1 Bethencourt Estrella, Carlos Javier
A1 Blanco Freijo, Mónica
A1 Reyes Batlle, María
A1 Sifaoui, Inés
A1 San Nicolás Hernández, Desirée
A1 McNaughton Smith, Grant
A1 Lorenzo Morales, Jacob
A1 Abad-Grillo, Teresa
A1 Piñero Barroso, José Enrique
K1 Phenalenones
K1 Leishmania amazonensis
K1 apoptosis-like
K1 chemotherapy
AB The in vitro activity against Leishmania spp. of five novel designed compounds, phenalenone derivatives, is described in this study. Previous works have shown that some phenalenones present leishmanicidal activity, some of which could induce programmed cell death events in L. amazonensis parasites. In this research, we focused on the determination of the programmed cell death evidence by detecting the characteristic features of the apoptosis-like process, such as phosphatidylserine exposure and mitochondrial membrane potential, among others. The results showed that the new derivatives have comparable or better activity and selectivity than the commonly prescribed anti-leishmanial drug. This result was obtained by inducing stronger mitochondrial depolarization or more intense phosphatidylserine exposure than miltefosine, highlighting compound 8 with moreover 9-times better selectivity index. In addition, the new five molecules activated the apoptosis-like process in the parasite. All the signals observed were indicative of the death process that the parasites were undergoing.
SN 0753-3322
YR 2020
FD 2020
LK http://riull.ull.es/xmlui/handle/915/35821
UL http://riull.ull.es/xmlui/handle/915/35821
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 02-jun-2024