TY - JOUR
T1 - Inhibition of Leishmania mexicana growth by the tuberculosis drug SQ109
AU - García-García, Verónica
AU - Oldfield, Eric
AU - Benaim, Gustavo
N1 - Publisher Copyright:
Copyright © 2016, American Society for Microbiology. All Rights Reserved.
PY - 2016/10
Y1 - 2016/10
N2 - We report that the tuberculosis drug SQ109 [N-adamantan-2-yl-N′-((E)-3,7-dimethyl-octa-2,6-dienyl)-ethane-1,2-diamine] has potent activity against the intracellular amastigote form of Leishmania mexicana (50% inhibitory concentration [IC50], ∼11 nM), with a good selectivity index (>500). It is also active against promastigotes (IC50, ∼500 nM) and acts as a protonophore uncoupler, in addition to disrupting Ca2+ homeostasis by releasing organelle Ca2+ into the cytoplasm, and as such, it is an interesting new leishmaniasis drug hit candidate.
AB - We report that the tuberculosis drug SQ109 [N-adamantan-2-yl-N′-((E)-3,7-dimethyl-octa-2,6-dienyl)-ethane-1,2-diamine] has potent activity against the intracellular amastigote form of Leishmania mexicana (50% inhibitory concentration [IC50], ∼11 nM), with a good selectivity index (>500). It is also active against promastigotes (IC50, ∼500 nM) and acts as a protonophore uncoupler, in addition to disrupting Ca2+ homeostasis by releasing organelle Ca2+ into the cytoplasm, and as such, it is an interesting new leishmaniasis drug hit candidate.
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U2 - 10.1128/AAC.00945-16
DO - 10.1128/AAC.00945-16
M3 - Article
C2 - 27458218
AN - SCOPUS:84992640317
SN - 0066-4804
VL - 60
SP - 6386
EP - 6389
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
IS - 10
ER -