RT Journal Article
T1 Library of Seleno-Compounds as Novel Agents against Leishmania Species
A1 Martin-Montes, Alvaro
A1 Plano, Daniel
A1 Martin-Escolano, Ruben
A1 Alcolea, Veronica
A1 Diaz, Marta
A1 Perez-Silanes, Silvia
A1 Espuelas, Socorro
A1 Moreno, Esther
A1 Marin, Clotilde
A1 Gutierrez-Sanchez, Ramon
A1 Sanmartin, Carmen
A1 Sanchez-Moreno, Manuel
K1 Leishmania
K1 glucose metabolism
K1 Potent antileishmanial agents
K1 Visceral leishmaniasis
K1 In-vitro
K1 Redox modulators
K1 Drug-resistance
K1 Trypanosomatids
K1 Promastigotes
K1 Diselenides
K1 Metabolism
K1 Organoselenocyanates
AB The in vitro leishmanicidal activities of a series of 48 recently synthesized selenium derivatives against Leishmania infantum and Leishmania braziliensis parasites were tested using promastigotes and intracellular amastigote forms. The cytotoxicity of the tested compounds for J774.2 macrophage cells was also measured in order to establish their selectivity. Six of the tested compounds (compounds 8, 10, 11, 15, 45, and 48) showed selectivity indexes higher than those of the reference drug, meglumine antimonate (Glucantime), for both Leishmania species; in the case of L. braziliensis, compound 20 was also remarkably selective. Moreover, data on infection rates and amastigote numbers per macrophage showed that compounds 8, 10, 11, 15, 45, and 48 were the most active against both Leishmania species studied. The observed changes in the excretion product profile of parasites treated with these six compounds were also consistent with substantial cytoplasmic alterations. On the other hand, the most active compounds were potent inhibitors of Fe superoxide dismutase (Fe-SOD) in the two parasite species considered, whereas their impact on human CuZn-SOD was low. The high activity, low toxicity, stability, low cost of the starting materials, and straightforward synthesis make these compounds appropriate molecules for the development of affordable antileishmanicidal agents.
PB American Society for Microbiology
SN 0066-4804
YR 2017
FD 2017-03-12
LK http://hdl.handle.net/10668/19014
UL http://hdl.handle.net/10668/19014
LA en
NO Martín-Montes Á, Plano D, Martín-Escolano R, Alcolea V, Díaz M, Pérez-Silanes S, et al. Library of Seleno-Compounds as Novel Agents against Leishmania Species. Antimicrob Agents Chemother. 2017 May 24;61(6):e02546-16.
DS RISalud
RD Apr 18, 2025