Cytotoxicity andIn VitroAntileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol
Year: 2013
Type: article
Abstract: Leishmania amazonensis is the etiologic agent of the cutaneous and diffuse leishmaniasis often associated with drug resistance. Lapachol [2-hydroxy-3-(3'-methyl-2-butenyl)-1,4-naphthoquinone] displays a wide range of antimicrobial properties against many pathogens. In this study, using the classic microscopic in vitro model, we have analyzed the effects of a series of lapachol and chlorides complexes with antimony (V), bismuth (V), and tin (IV) against L. amazonensis. All seven compounds exhibited antileishmanial activity, but most of the antimony (V) and bismuth (V) complexes were toxic against human HepG2 cells and murine macrophages. The best IC50 values (0.17 ± 0.03 and 0.10 ± 0.11 μg/mL) were observed for Tin (IV) complexes (3) [(Lp)(Ph3Sn)] and (6) (Ph3SnCl2), respectively. Their selective 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.
DOI: 10.1155/2013/961783
Language: English
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $1,630
Awards: G2245511111, G3568473137, ENSAIOS PRÉ-CLÍNICOS DE FORMULAÇÕES NANOESTRUTURADAS DE ANTIMONIAIS, G5323109872, GLICOBIOLOGIA DE LEISHMANIA AMAZONENSIS: PAPEL DO LIPOFOSFOGLICANO (LPG) NO PROCESSO DE INTERAÇÃO, G6093278904, G8224234723, G8321289703, DESENVOLVIMENTO E ENSAIOS PRÉ-CLÍNICOS DE FORMULAÇÕES NANOESTRUTURADAS PARA A TERAPÊUTICA DAS LEISHMANIOSES
OpenAlex ID: W2000865022