Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Parasitology ; 141(8): 1031-43, 2014 Jul.
Article in English | MEDLINE | ID: mdl-24636142

ABSTRACT

The 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.


Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania braziliensis/drug effects , Leishmania infantum/drug effects , Leishmaniasis/drug therapy , Pyrazoles/pharmacology , Superoxide Dismutase/drug effects , Animals , Antiprotozoal Agents/chemistry , Cell Line , Cell Survival/drug effects , Erythrocytes/drug effects , Female , Humans , Leishmania braziliensis/enzymology , Leishmania braziliensis/ultrastructure , Leishmania infantum/enzymology , Leishmania infantum/ultrastructure , Leishmaniasis/parasitology , Macrocyclic Compounds/chemistry , Macrocyclic Compounds/pharmacology , Macrophages/drug effects , Mice, Inbred BALB C , Microscopy, Electron, Transmission , Models, Molecular , Polyamines/chemistry , Polyamines/pharmacology , Protozoan Proteins/drug effects , Protozoan Proteins/metabolism , Pyrazoles/chemistry , Superoxide Dismutase/metabolism
SELECTION OF CITATIONS
SEARCH DETAIL
...