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In vitro leishmanicidal activity of pyrazole-containing polyamine macrocycles which inhibit the Fe-SOD enzyme of Leishmania infantum and Leishmania braziliensis species

AuthorsNavarro, P.; Sánchez-Moreno, M.; Marín, Clotilde; García-España, E.; Ramírez-Macías, Inmaculada; Olmo, F.; Rosales, M. J.; Gómez-Contreras, F.; Yunta, M. J. R.; Gutierrez-Sánchez, Ramón
KeywordsLeishmania braziliensis
Leishmania infantum
Iron superoxide dismutase
Leishmanicidal activity
Polyamine macrocycle
Issue Date2014
PublisherCambridge University Press
CitationParasitology 141: 1031- 1043 (2014)
AbstractThe in vitro leishmanicidal activity and cytotoxicity of pyrazole-containing macrocyclic polyamines 1-4 was assayed on Leishmania infantum and Leishmania braziliensis species. Compounds 1-4 were more active and less toxic than glucantime and both infection rates and ultrastructural alterations confirmed that 1 and 2 were highly leishmanicidal and induced extensive parasite cell damage. Modifications in the excretion products of parasites treated with 1-3 were also consistent with substantial cytoplasm alterations. Compound 2 was highlighted as a potent inhibitor of Fe-SOD in both species, whereas its effect on human CuZn-SOD was poor. Molecular modelling suggested that 2 could deactivate Fe-SOD due to a sterically favoured enhanced ability to interact with the H-bonding net that supports the enzyme's antioxidant features. © Cambridge University Press 2014.
Identifiersdoi: 10.1017/S0031182014000201
issn: 0031-1820
e-issn: 1469-8161
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