Role of residual Sb(III) in meglumine antimoniate cytotoxicity and MRP1-mediated resistance

Chemico-biological Interactions
Simplice A DzamitikaFrédéric Frézard

Abstract

Despite the clinical use of pentavalent antimonials for more than half a century, their metabolism in mammals and mechanisms of action and toxicity remain poorly understood. It has been proposed that the more active and toxic trivalent antimony form Sb(III) plays a critical role in their antileishmanial activity and toxicity. The aim of this work was to investigate the role of residual Sb(III) both in the antileishmanial/antitumoral activities of the pentavalent meglumine antimoniate and in the MRP1 (multidrug resistance-associated protein 1)-mediated resistance to this drug. Samples of meglumine antimoniate differing in their amount of residual Sb(III) (meglumine antimoniate synthesized either from SbCl(5) or from KSb(OH)(6) as well as commercially-available meglumine antimoniate) were evaluated in vitro and in vivo on Leishmania amazonensis infections, as well as for their cytotoxicity to normal and MRP1-overexpressing GLC4 cell lines. Although in vitro the two most effective drugs contained the highest levels of Sb(III), no correlation was found in vivo between the antileishmanial activity of meglumine antimoniate and its residual Sb(III) content, suggesting that residual Sb(III) contributes only marginally to the drug antil...Continue Reading

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Citations

Apr 25, 2013·Analytical and Bioanalytical Chemistry·Pascal Salaün, Frédéric Frézard
Dec 17, 2011·Journal of Tropical Medicine·Fakhri JeddiCharles Mary
Jul 28, 2009·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Frédéric FrézardRaul R Ribeiro
Oct 30, 2010·Expert Opinion on Drug Delivery·Frédéric Frézard, Cynthia Demicheli
Aug 1, 2006·International Journal of Pharmaceutics·Patrícia S MartinsFrédéric Frézard
Nov 6, 2013·Antimicrobial Agents and Chemotherapy·Kelly C KatoFrédéric Frézard
Dec 28, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Betânia Mara AlvarengaJosé Dias Corrêa Junior
Jun 27, 2018·Antimicrobial Agents and Chemotherapy·Luís Cláudio Lima de JesusSilma Regina Ferreira Pereira

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