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Exploring Mono and Bis-gold(I)-DTC Complexes Against Cancer and Leishmania

Thaiz Cristina Soares Dos Santos1, Patrícia Salvador Tessaro1, Ana Luiza de Andrade Querino1

  • 1Laboratório de Síntese e Interações Bioinorgânicas (SibLab), Departmento de Química, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.

Chemistry, an Asian Journal
|February 17, 2025
PubMed

Insights

New gold(I) complexes show potent anticancer and antileishmanial activities. These metallodrugs, particularly bis-gold(I) compounds, offer promising therapeutic potential against cancer and parasitic leishmaniasis.

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Nanotechnology

Background:

  • Cancer and leishmaniasis pose significant global health challenges, driving the need for novel therapeutic agents.
  • Gold(I)-based compounds are emerging as promising candidates for chemotherapy, necessitating the development of analogs with improved efficacy.
  • Dithiocarbamate ligands and triphenylphosphine are utilized in the design of novel gold(I) complexes.

Purpose of the Study:

  • To synthesize and characterize five new gold(I) complexes with potential biological applications.
  • To evaluate the antiproliferative activity of these complexes against breast tumor cell lines.
  • To assess the antileishmanial efficacy of the synthesized gold(I) complexes against various Leishmania species.

Main Methods:

  • Synthesis and characterization of five novel gold(I) complexes using dithiocarbamate ligands and triphenylphosphine.
  • In vitro antiproliferative assays using human breast tumor cell lines (MDA-MB-231, 4T1) and a non-tumorigenic breast cell line (MCF-10a).
  • In vitro antileishmanial assays against intracellular amastigotes of Leishmania (Viannia) braziliensis, L. (Leishmania) amazonensis, and L. (L.) infantum.

Main Results:

  • All synthesized gold(I) complexes exhibited enhanced cytotoxic activity against breast tumor cells compared to controls.
  • The bis-gold(I) complexes demonstrated particularly potent antiproliferative effects.
  • The complexes showed significant antileishmanial activity, with bis-gold(I) compounds displaying superior efficacy against Leishmania parasites.
  • Gold complexation was crucial for the observed biological activities.

Conclusions:

  • The novel gold(I) complexes possess significant antiproliferative and antileishmanial properties.
  • Bis-gold(I) complexes represent promising lead compounds for developing new metallodrugs against cancer and leishmaniasis.
  • The findings underscore the therapeutic potential of gold-based compounds in combating major global diseases.
Keywords:
anti-amastigotesantitumordithiocarbamatesgoldleishmaniasis

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