On the reversible and irreversible inhibition of rhodesain by curcumin

Steverding, Dietmar (2019) On the reversible and irreversible inhibition of rhodesain by curcumin. Molecules, 25. ISSN 1420-3049

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Abstract

Previously, it was suggested that the natural compound curcumin is an irreversible inhibitor of rhodesain, the major lysosomal cysteine protease of the protozoan parasite Trypanosoma brucei. The suggestion was based on a time-dependent inhibition of the enzyme by curcumin and a lack of recovery of activity of the enzyme after pre-incubation with curcumin. This study provides clear evidence that curcumin is a reversible, non-competitive inhibitor of rhodesain. In addition, the study also shows that the apparent irreversible inhibition of curcumin is only observed when no thiol-reducing reagent is included in the measuring buffer and insufficient solubilising agent is added to fully dissolve curcumin in the aqueous solution. Thus, the previous observation that curcumin acts as an irreversible inhibitor for rhodesain was based on a misinterpretation of experimental findings.

Item Type:	Article
Faculty \ School:	Faculty of Medicine and Health Sciences > Norwich Medical School
UEA Research Groups:	Faculty of Medicine and Health Sciences > Research Groups > Gastroenterology and Gut Biology
Depositing User:	LivePure Connector
Date Deposited:	04 Jan 2020 04:08
Last Modified:	22 Oct 2022 05:39
URI:	https://ueaeprints.uea.ac.uk/id/eprint/73485
DOI:	10.3390/molecules25010143

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