Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro

Karen Minori; Letícia B Rosa; Riccardo Bonsignore; Angela Casini; Danilo C Miguel

doi:10.1002/cmdc.202000536

Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro

ChemMedChem. 2020 Nov 18;15(22):2146-2150. doi: 10.1002/cmdc.202000536. Epub 2020 Sep 28.

Authors

Karen Minori¹, Letícia B Rosa¹, Riccardo Bonsignore², Angela Casini², Danilo C Miguel¹

Affiliations

¹ Department of Animal Biology, Biology Institute, University of Campinas (UNICAMP), Rua Monteiro Lobato, 255, 13083-862., Campinas, SP, Brazil.
² Department of Chemistry, Technical University of Munich (TUM), Lichtenbergstraße 4, 85748, Garching b. München, Germany.

Abstract

A series of mononuclear coordination or organometallic Au^I /Au^III complexes (1-9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, of Leishmania amazonensis and Leishmania braziliensis. One of the cationic Au^I bis-N-heterocyclic carbenes (3) has low EC₅₀ values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other Au^III complexes (6 and 7), the compound is also extremely effective in intracellular amastigotes from L. amazonensis. Initial mechanistic studies include an evaluation of the gold complexes' effect on L. amazonensis' plasma membrane integrity.

Keywords: amastigotes; antiprotozoal agents; gold compounds; leishmaniasis; promastigotes.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antiprotozoal Agents / chemistry
Antiprotozoal Agents / pharmacology*
Cells, Cultured
Leishmania / drug effects*
Mice
Mice, Inbred BALB C
Molecular Structure
Organogold Compounds / chemistry
Organogold Compounds / pharmacology*
Parasitic Sensitivity Tests

Substances

Antiprotozoal Agents
Organogold Compounds