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Antimicrob Agents Chemother ; 60(5): 2732-8, 2016 05.
Artigo em Inglês | MEDLINE | ID: mdl-26883711

RESUMO

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.


Assuntos
Gluconato de Antimônio e Sódio/uso terapêutico , Antiprotozoários/uso terapêutico , Extratos Vegetais/uso terapêutico , Alcaloides de Solanáceas/uso terapêutico , Alcaloides/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Dendríticas/parasitologia , Feminino , Citometria de Fluxo , Frutas/química , Leishmania mexicana/efeitos dos fármacos , Leishmania mexicana/patogenicidade , Macrófagos/parasitologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/química
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