Evaluation of the anti-trypanosomal activity of tyropeptin A

Dietmar Steverding, Alexander J. Pemberton, Howard Royle, Robert W. Spackman, A. Jennifer Rivett

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


The natural compound tyropeptin A, a new peptidyl aldehyde proteasome inhibitor, was tested for its trypanocidal activity in vitro using culture-adapted bloodstream forms of Trypanosoma brucei. The concentrations of tyropeptin A required to reduce the growth rate by 50 % and to kill all cells were 10 and 100 times lower for bloodstream-form trypanosomes than for human leukaemia HL-60 cells, respectively. Enzymatic analysis showed that the trypsin-like activity of the trypanosome proteasome and the chymotrypsin-like activity of the mammalian proteasome are particularly sensitive to inhibition by tyropeptin A. The results suggest that natural compounds targeting the trypsin-like activity of the proteasome may serve as leads for rational drug development of novel anti-trypanosomal agents.
Original languageEnglish
Pages (from-to)761-763
Number of pages3
JournalPlanta Medica
Issue number8
Publication statusPublished - 2006

Cite this