In vitro evaluation of antileishmanial activity of copper (I) complexes

Ana Flávia da Silva Chagas; Marina Porchia; Francesco Tisato; Pauline de Faria Soldera; Claudia Dantas Comandolli Wyrepkowski; Maricleide de Farias Naiff; Antonia Maria Ramos Franco

doi:10.22571/2526-4338474

Ana Flávia da Silva Chagas Programa de Pós-Graduação em Biotecnologia, Universidade Federal do Amazonas, Manaus, Amazonas, Brasil http://orcid.org/0000-0002-6677-9833
Marina Porchia Institute of Condensed Matter Chemistry and Technologies for Energy, National Research Council, Pádua, Corso Stati Uniti, Itália http://orcid.org/0000-0003-0435-6576
Francesco Tisato Institute of Condensed Matter Chemistry and Technologies for Energy, National Research Council, Pádua, Corso Stati Uniti, Itália http://orcid.org/0000-0002-1635-3121
Pauline de Faria Soldera Programa de Pós-Graduação em Biotecnologia, Universidade Federal do Amazonas, Manaus, 69067-005, Amazonas, Brasil http://orcid.org/0000-0003-1730-0029
Claudia Dantas Comandolli Wyrepkowski Instituto Federal de Pesquisas da Amazônia, Manaus, Amazonas, Brasil http://orcid.org/0000-0001-9699-7308
Maricleide de Farias Naiff Instituto Federal de Pesquisas da Amazônia, Manaus, Amazonas, Brasil http://orcid.org/0000-0002-9221-5759
Antonia Maria Ramos Franco Instituto Federal de Pesquisas da Amazônia, Manaus, Amazonas, Brasil http://orcid.org/0000-0002-4300-5325

DOI: https://doi.org/10.22571/2526-4338474

Abstract

In the research for the development of new drugs for the therapy of American tegumentary leishmaniasis, copper has been studied for its antileishmania activity. This study aims to report the activity of three copper(I) complexes on parasites of the species L. amazonensis and L. guyanensis. The metal complexes were tested according to in vitro antileishmanial assays, against promastigote and amastigote forms of the most prevalent species in the state of Amazonas, Brazil. Cytotoxicity of the complexes was evaluated in murine macrophage-like cell line (MJ774). The results of the in vitro assays indicated that, among the copper complexes tested, the homoleptic phosphine complex [Cu(thp)₄][PF₆](thp=tris-hydroxymethylphosphine) presented promising activity against the evolutionary forms of L. amazonensis, and obtained a IC₅₀ of 26.45 and 24.61 µM in a period of 48 and 72 h, respectively. The results for copper complex at concentration 160 µM in amastigote forms showed a decrease in the infection index (32% of infected cells) and, in the cytotoxicity assay with MJ774, 52.43% of cell viability was observed. The results showed that the complex [Cu(thp)₄][PF₆] presented significant biological activity, indicating a need for future in vivo studies.

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