pentavalent antimonials new perspectives for old drugs五价的锑的新视角对旧药物.pdfVIP

Molecules 2009, 14, 2317-2336; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Review Pentavalent Antimonials: New Perspectives for Old Drugs Frédéric Frézard 1,*, Cynthia Demicheli 2 and Raul R. Ribeiro 1 1 Departamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Av. Antônio Carlos 6627, Pampulha, 31270-901 Belo Horizonte, MG, Brazil; E-mail: raulrio@ufmg.br (R.R.) 2 Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, Av. Antônio Carlos 6627, Pampulha, 31270-901 Belo Horizonte, MG, Brazil; E-mail: demichel@netuno.lcc.ufmg.br (C.D.) * Author to whom correspondence should be addressed; E-mail: frezard@icb.ufmg.br Received: 23 April 2009; in revised form: 15 June 2009 / Accepted: 22 June 2009 / Published: 30 June 2009 Abstract: Pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the first-line drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and mechanism of action are still being investigated. Some recent studies suggest that pentavalent antimony acts as a prodrug that is converte