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Cytotoxicity and in vitro anti Leishmania activity of antimony (V), bismuth (V) and tin (IV) complexes of lapanol

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Document pages: 7 pages

Abstract: Leishmania Amazonia is the pathogen of cutaneous and diffuse leishmaniasis, which is usually related to drug resistance. Lapanol [2-hydroxy-3 - (3 - methyl-2-butenol) - 1,4-naphthoquinone] has a wide range of antibacterial properties against a variety of pathogens. In this study, using the classical microscopic in vitro model, we analyzed the effects of a series of complexes of lapapol and chloride with antimony (V), bismuth (V) and tin (IV) on Lactobacillus Amazonia. All seven compounds have anti Leishmania activity, but most antimony (V) and bismuth (V) complexes are toxic to human HepG2 cells and mouse macrophages. The optimal IC50 values (0.17, 0.03 and 0.10, 0.11   tin (IV) complexes (3) [(LP) (ph3sn)] and (6) (ph3sncl2) were g ml, respectively). Their choiceive indexes (SIs) were 70.65 and 120.35 for HepG2 cells, respectively. However, while analyzing murine macrophages, the SI decreased. Those compounds were moderately toxic for HepG2 cells and toxic for murine macrophages, still underlying the need of chemical modification in this class of compounds.

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