On the Reversible and Irreversible Inhibition of Rhodesain by Curcumin

Molecules

Dietmar Steverding¹ 

[1] Bob Champion Research and Education Building, Norwich Medical School, University of East Anglia, Norwich Research Park, James Watson Road, Norwich NR4 7UQ, UK;

关键词: rhodesain;    curcumin;    non-competitive inhibition;   

DOI  :  10.3390/molecules25010143

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown