TY - JOUR
T1 - Inhibition of Leishmania mexicana growth by the tuberculosis drug SQ109
AU - García-García, Verónica
AU - Oldfield, Eric
AU - Benaim, Gustavo
N1 - Funding Information:
We thank Otto Geoffroy, Alchem Laboratories Corporation, for providing the SQ109. This work was supported by the Fondo Nacional de Ciencias, Tecnolog?a e Investigaci?n, Venezuela (FONACIT; grant 2011000884 to G.B.), by the Consejo de Desarrollo Cient?fico y Human?stico-Universidad Central de Venezuela (CDCH-UCV; grant PG-03-8728-2013/2 to G.B.), and in part by the U.S. Public Health Service (NIH grants CA158191 and GM065307 to E.O.), a Harriet A. Harlin Professorship (E.O.), and the University of Illinois Foundation/Oldfield Research Fund.
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
VL - 60
SP - 6386
EP - 6389
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
SN - 0066-4804
IS - 10
ER -