Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol
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 m...
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| Format: | Article |
| Language: | English |
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Wiley
2013-01-01
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| Series: | Bioinorganic Chemistry and Applications |
| Online Access: | http://dx.doi.org/10.1155/2013/961783 |
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| author | Marcele Neves Rocha Paula Monalisa Nogueira Cynthia Demicheli Ludmila Gonçalvez de Oliveira Meiriane Mariano da Silva Frédéric Frézard Maria Norma Melo Rodrigo Pedro Soares |
| author_facet | Marcele Neves Rocha Paula Monalisa Nogueira Cynthia Demicheli Ludmila Gonçalvez de Oliveira Meiriane Mariano da Silva Frédéric Frézard Maria Norma Melo Rodrigo Pedro Soares |
| author_sort | Marcele Neves Rocha |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-7fb3d48ea47949309a21eb316250e497 |
| institution | Kabale University |
| issn | 1565-3633 1687-479X |
| language | English |
| publishDate | 2013-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Bioinorganic Chemistry and Applications |
| spelling | doaj-art-7fb3d48ea47949309a21eb316250e4972025-02-03T05:47:17ZengWileyBioinorganic Chemistry and Applications1565-36331687-479X2013-01-01201310.1155/2013/961783961783Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of LapacholMarcele Neves Rocha0Paula Monalisa Nogueira1Cynthia Demicheli2Ludmila Gonçalvez de Oliveira3Meiriane Mariano da Silva4Frédéric Frézard5Maria Norma Melo6Rodrigo Pedro Soares7Centro de Pesquisas René Rachou, Fundação Oswaldo Cruz/FIOCRUZ, 30190-002 Belo Horizonte, MG, BrazilCentro de Pesquisas René Rachou, Fundação Oswaldo Cruz/FIOCRUZ, 30190-002 Belo Horizonte, MG, BrazilDepartamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, BrazilDepartamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, BrazilDepartamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, BrazilDepartamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, BrazilDepartamento de Parasitologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, BrazilCentro de Pesquisas René Rachou, Fundação Oswaldo Cruz/FIOCRUZ, 30190-002 Belo Horizonte, MG, BrazilLeishmania 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.http://dx.doi.org/10.1155/2013/961783 |
| spellingShingle | Marcele Neves Rocha Paula Monalisa Nogueira Cynthia Demicheli Ludmila Gonçalvez de Oliveira Meiriane Mariano da Silva Frédéric Frézard Maria Norma Melo Rodrigo Pedro Soares Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol Bioinorganic Chemistry and Applications |
| title | Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol |
| title_full | Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol |
| title_fullStr | Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol |
| title_full_unstemmed | Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol |
| title_short | Cytotoxicity and In Vitro Antileishmanial Activity of Antimony (V), Bismuth (V), and Tin (IV) Complexes of Lapachol |
| title_sort | cytotoxicity and in vitro antileishmanial activity of antimony v bismuth v and tin iv complexes of lapachol |
| url | http://dx.doi.org/10.1155/2013/961783 |
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