Evaluation of the anti-trypanosomal activity of tyropeptin A

Steverding, Dietmar, Pemberton, Alexander J., Royle, Howard, Spackman, Robert W. and Rivett, A. Jennifer (2006) Evaluation of the anti-trypanosomal activity of tyropeptin A. Planta Medica, 72 (8). pp. 761-763. ISSN 1439-0221

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Abstract

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.

Item Type: Article
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Depositing User: EPrints Services
Date Deposited: 25 Nov 2010 11:08
Last Modified: 21 Apr 2020 19:53
URI: https://ueaeprints.uea.ac.uk/id/eprint/11501
DOI: 10.1055/s-2006-931600

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