Abstract
Antimony(Sb)-yeast mannan complexes were synthesized as a strategy to introduce Sb into macrophages infected with Leishmania amastigotes. The complexes were taken up by endocytosis after specific recognition by alpha-D-mannosyl receptors on the macrophage membrane. About 90% of the intracellular parasites were destroyed by Sb-mannan in vitro, whereas the corresponding Sb concentration used as the pentavalent antimonial drug glucantime destroyed about 60% of the amastigotes. None of the Sb complexes prepared with mannan acid or basic derivatives was as effective as the simple Sb-mannan complex in clearing macrophage infection by Leishmania (L) amazonensis. The leishmanicidal effect of Sb-mannan was also demonstrated in vivo with infected hamsters. The alternative use of Sb-mannan complex in the treatment of human leishmaniasis is envisaged on the basis of parasite-killing efficiency and the use of a low antimony dose.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimony / chemistry
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Antimony / pharmacokinetics
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Antimony / pharmacology*
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacokinetics
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Antiprotozoal Agents / pharmacology*
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Carbohydrate Sequence
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Cricetinae
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Drug Carriers
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Lectins, C-Type*
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Leishmania / drug effects*
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Leishmaniasis / drug therapy
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Macrophages / metabolism
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Macrophages / parasitology*
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Mannans* / chemistry
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Mannose / pharmacology
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Mannose Receptor
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Mannose-Binding Lectins*
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Meglumine / pharmacology
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Meglumine Antimoniate
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Mice
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Molecular Sequence Data
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Organometallic Compounds / pharmacology
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Receptors, Cell Surface*
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Receptors, Immunologic / metabolism
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Saccharomyces cerevisiae / chemistry
Substances
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Antiprotozoal Agents
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Drug Carriers
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Lectins, C-Type
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Mannans
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Mannose Receptor
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Mannose-Binding Lectins
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Organometallic Compounds
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Receptors, Cell Surface
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Receptors, Immunologic
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Meglumine
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Meglumine Antimoniate
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Antimony
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Mannose