Article

Download article 		Title: Increasing the activity of copper(II) complexes against Leishmania through lipophilicity and pro-oxidant ability
Author: Portas, Andressa Dos Santos; Miguel, Danilo Ciccone; Yokoyama-yasunaka, Jenicer K. U.; Uliana, Silvia Reni Bortolin; Espósito, Breno Pannia
Year: 2012
Is part of: JBIC. Journal of Biological Inorganic Chemistry (Print), v. 17, p. 107 - 112
DOI: https://doi.org/10.1007/s00775-011-0834-3

Citation: Portas, Andressa Dos Santos; Miguel, Danilo Ciccone; Yokoyama-yasunaka, Jenicer K. U.; Uliana, Silvia Reni Bortolin; Espósito, Breno Pannia; Increasing the activity of copper(II) complexes against Leishmania through lipophilicity and pro-oxidant ability. JBIC. Journal of Biological Inorganic Chemistry (Print), v.17, p. 107-112, 2012

Abstract: Copper complexes with fluorinated beta-diketones were synthesized and characterized in terms of lipophilicity and peroxide-assisted oxidation of dihydrorhodamine as an indicator of redox activity. The biological activity of the complexes was tested against promastigotes of Leishmania amazonensis. Inhibition of trypanosomatid-specific trypanothione reductase was also tested. It was found that the highly lipophilic and redox-active bis(trifluoroacetylacetonate) derivative had increased toxicity towards promastigotes. These results indicate that it is possible to modulate the activity of metallodrugs based on redox-active metals through the appropriate choice of lipophilic chelators in order to design new antileishmanials. Further work will be necessary to improve selectivity of these compounds against the parasite.



Funding: Raul Hernandez helped us with the statistical analysis. This project was funded by CNPq and FAPESP (Brazilian government agencies). 		Financed by: