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

Molecular and Biochemical Parasitology
Isabel WinterBernhard Biersack

Abstract

Two gold(I) N-heterocyclic carbene complexes 1a and 1b were tested for their anti-trypanosomal activity against Trypanosoma 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).

Citations

Nov 27, 2018·Chemical Society Reviews·Malka MoraRenso Visbal
Mar 10, 2020·Archiv der Pharmazie·Waleed S KokoBernhard Biersack
Dec 6, 2019·Chemistry & Biodiversity·Jana JentzschBernhard Biersack
Nov 25, 2020·Chemistry & Biodiversity·Ibrahim S Al NasrBernhard Biersack

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African trypanosomiasis, also known as sleeping sickness, is an insect-borne parasitic disease of humans and other animals. It is caused by protozoa of the species Trypanosoma brucei and almost invariably progresses to death unless treated. Discover the latest research on African trypanosomiasis here.