Anti-trypanosomal activity of cationic N-heterocyclic carbene gold(I) complexes

Publication date: Available online 15 May 2017 Source:Molecular and Biochemical Parasitology Author(s): Isabel Winter, Julia Lockhauserbäumer, Gertrud Lallinger-Kube, Rainer Schobert, Klaus Ersfeld, Bernhard Biersack Two gold(I) N-heterocyclic carbene complexes 1a and 1b were tested for their anti-trypanosomal activity against Trypanosoma brucei brucei parasites. Both gold compounds exhibited excellent anti-trypanosomal activity (IC50 =0.9-3.0nM). The effects of the gold complexes 1a and 1b on the T. b. brucei cytoskeleton were evaluated. Rapid detachment of the flagellum from the cell body occurred after treatment with the gold complexes. In addition, a quick and complete degeneration of the parasitic cytoskeleton was induced by the gold complexes, only the microtubules of the detached flagellum remained intact. Both gold compounds 1a and 1b feature selective anti-trypanosomal agents and were distinctly more active against T. b. brucei cells than against human HeLa cells. Thus, the gold complexes 1a and 1b feature promising drug candidates for the treatment of trypanosome infections such as sleeping sickness (human African Trypanosomiasis caused by Trypanosoma brucei parasites). Graphical abstract
Source: Molecular and Biochemical Parasitology - Category: Parasitology Source Type: research