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The food colorant erythrosine is a promiscuous protein-protein interaction inhibitor.
- Source :
-
Biochemical pharmacology [Biochem Pharmacol] 2011 Mar 15; Vol. 81 (6), pp. 810-8. Date of Electronic Publication: 2011 Jan 08. - Publication Year :
- 2011
-
Abstract
- Following our observation that erythrosine B (FD&C Red No. 3) is a relatively potent inhibitor of the TNF-R-TNFα and CD40-CD154 protein-protein interactions, we investigated whether this inhibitory activity extends to any other protein-protein interactions (PPI) as well as whether any other approved food colors possess such inhibitory activity. We found erythrosine, a poly-iodinated xanthene dye, to be a non-specific promiscuous inhibitor of a number of PPIs within the tumor necrosis factor superfamily (TNF-R-TNFα, CD40-CD154, BAFF-R-BAFF, RANK-RANKL, OX40-OX40L, 4-1BB-4-1BBL) as well as outside of it (EGF-R-EGF) with a remarkably consistent median inhibitory concentration (IC(50)) in the 2-20 μM (approximately 2-20mg/L) range. In agreement with this, erythrosine also showed cellular effects including clear cytotoxic effects around this concentration range (IC₅₀≈50 μM). Among the seven FDA-approved food colorants, only erythrosine showed consistent PPI inhibitory activity in the sub-100 μM range, which might also explain (at least partially) why it also has the lowest approved acceptable daily intake (ADI) (0.1 mg/kg body weight/day). Among a number of xanthene structural analogs of erythrosine tested for activity, rose Bengal, a food colorant approved in Japan, showed similar, maybe even more pronounced, promiscuous inhibitory activity, whereas fluorescein was inactive and gallein, phloxine, and eosin were somewhat active in some of the assays.<br /> (Copyright © 2011 Elsevier Inc. All rights reserved.)
- Subjects :
- Cells, Cultured
Dose-Response Relationship, Drug
Erythrosine pharmacology
Food Coloring Agents pharmacology
Humans
Myeloid Cells drug effects
Protein Binding drug effects
Protein Binding physiology
Protein Interaction Domains and Motifs drug effects
Rose Bengal metabolism
Rose Bengal pharmacology
Tumor Necrosis Factors metabolism
Erythrosine metabolism
Food Coloring Agents metabolism
Myeloid Cells metabolism
Protein Interaction Domains and Motifs physiology
Tumor Necrosis Factor Inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1873-2968
- Volume :
- 81
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Biochemical pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 21219880
- Full Text :
- https://doi.org/10.1016/j.bcp.2010.12.020