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Antimicrob Agents Chemother ; 60(5): 2732-8, 2016 05.
Article in English | MEDLINE | ID: mdl-26883711

ABSTRACT

Little has been done during the past 100 years to develop new antileishmanial drugs. Most infected individuals live in poor countries and have a low cash income to be attractive targets to pharmaceutical corporations. Two heterosidic steroids, solamargine and solasonine, initially identified as major components of the Brazilian plant Solanum lycocarpum, were tested for leishmanicidal activity. Both alkaloids killed intracellular and extracellular Leishmania mexicana parasites more efficiently than the reference drug sodium stibogluconate. A total of 10 µM each individual alkaloid significantly reduced parasite counts in infected macrophages and dendritic cells. In vivo treatment of C57BL/6 mice with a standardized topical preparation containing solamargine (45.1%) and solasonine (44.4%) gave significant reductions in lesion sizes and parasite counts recovered from lesions. Alkaloids present different immunochemical pathways in macrophages and dendritic cells. We conclude that this topical preparation is effective and a potential new and inexpensive treatment for cutaneous leishmaniasis.


Subject(s)
Antimony Sodium Gluconate/therapeutic use , Antiprotozoal Agents/therapeutic use , Plant Extracts/therapeutic use , Solanaceous Alkaloids/therapeutic use , Alkaloids/chemistry , Animals , Cell Survival/drug effects , Dendritic Cells/parasitology , Female , Flow Cytometry , Fruit/chemistry , Leishmania mexicana/drug effects , Leishmania mexicana/pathogenicity , Macrophages/parasitology , Male , Mice , Mice, Inbred C57BL , Plant Extracts/chemistry
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