The food dye FD&C Blue No. 1 is a selective inhibitor of the ATP release channel Panx1

Junjie Wang, David George Jackson, Gerhard Dahl

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

The food dye FD&C Blue No. 1 (Brilliant Blue FCF [BB FCF]) is structurally similar to the purinergic receptor antagonist Brilliant Blue G (BBG), which is a well-known inhibitor of the ionotropic P2X7 receptor (P2X7R). The P2X7R functionally interacts with the membrane channel protein pannexin 1 (Panx1) in inflammasome signaling. Intriguingly, ligands to the P2X7R, regardless of whether they are acting as agonists or antagonists at the receptor, inhibit Panx1 channels. Thus, because both P2X7R and Panx1 are inhibited by BBG, the diagnostic value of the drug is limited. Here, weshow that the food dye BB FCF is a selective inhibitor of Panx1 channels, with an IC50 of 0.27 μM.No significant effect was observed with concentrations as high as 100 μM of BB FCF on P2X7R. Differing by just one hydroxyl group from BB FCF, the food dye FD&C Green No. 3 exhibited similar selective inhibition of Panx1 channels. A reverse selectivity was observed for the P2X7R antagonist, oxidized ATP, which in contrast to other P2X7R antagonists had no significant inhibitory effect on Panx1 channels. Based on its selective action, BB FCF can be added to the repertoire of drugs to study the physiology of Panx1 channels. Furthermore, because Panx1 channels appear to be involved directly or indirectly through P2X7Rs in several disorders, BB FCF and derivatives of this "safe" food dye should be given serious consideration for pharmacological intervention of conditions such as acute Crohn's disease, stroke, and injuries to the central nervous system.

Original languageEnglish
Pages (from-to)649-656
Number of pages8
JournalJournal of General Physiology
Volume141
Issue number5
DOIs
StatePublished - May 1 2013

Fingerprint

Purinergic P2X7 Receptors
Coloring Agents
Adenosine Triphosphate
Food
Purinergic Antagonists
Inflammasomes
Acute Disease
Ion Channels
Crohn Disease
Pharmaceutical Preparations
Hydroxyl Radical
Inhibitory Concentration 50
brilliant blue
Membrane Proteins
Central Nervous System
Stroke
Pharmacology
Ligands
Wounds and Injuries

ASJC Scopus subject areas

  • Physiology

Cite this

The food dye FD&C Blue No. 1 is a selective inhibitor of the ATP release channel Panx1. / Wang, Junjie; Jackson, David George; Dahl, Gerhard.

In: Journal of General Physiology, Vol. 141, No. 5, 01.05.2013, p. 649-656.

Research output: Contribution to journalArticle

@article{e2f8f017a74f44d2903cc9cb6ea989a0,
title = "The food dye FD&C Blue No. 1 is a selective inhibitor of the ATP release channel Panx1",
abstract = "The food dye FD&C Blue No. 1 (Brilliant Blue FCF [BB FCF]) is structurally similar to the purinergic receptor antagonist Brilliant Blue G (BBG), which is a well-known inhibitor of the ionotropic P2X7 receptor (P2X7R). The P2X7R functionally interacts with the membrane channel protein pannexin 1 (Panx1) in inflammasome signaling. Intriguingly, ligands to the P2X7R, regardless of whether they are acting as agonists or antagonists at the receptor, inhibit Panx1 channels. Thus, because both P2X7R and Panx1 are inhibited by BBG, the diagnostic value of the drug is limited. Here, weshow that the food dye BB FCF is a selective inhibitor of Panx1 channels, with an IC50 of 0.27 μM.No significant effect was observed with concentrations as high as 100 μM of BB FCF on P2X7R. Differing by just one hydroxyl group from BB FCF, the food dye FD&C Green No. 3 exhibited similar selective inhibition of Panx1 channels. A reverse selectivity was observed for the P2X7R antagonist, oxidized ATP, which in contrast to other P2X7R antagonists had no significant inhibitory effect on Panx1 channels. Based on its selective action, BB FCF can be added to the repertoire of drugs to study the physiology of Panx1 channels. Furthermore, because Panx1 channels appear to be involved directly or indirectly through P2X7Rs in several disorders, BB FCF and derivatives of this {"}safe{"} food dye should be given serious consideration for pharmacological intervention of conditions such as acute Crohn's disease, stroke, and injuries to the central nervous system.",
author = "Junjie Wang and Jackson, {David George} and Gerhard Dahl",
year = "2013",
month = "5",
day = "1",
doi = "10.1085/jgp.201310966",
language = "English",
volume = "141",
pages = "649--656",
journal = "Journal of General Physiology",
issn = "0022-1295",
publisher = "Rockefeller University Press",
number = "5",

}

TY - JOUR

T1 - The food dye FD&C Blue No. 1 is a selective inhibitor of the ATP release channel Panx1

AU - Wang, Junjie

AU - Jackson, David George

AU - Dahl, Gerhard

PY - 2013/5/1

Y1 - 2013/5/1

N2 - The food dye FD&C Blue No. 1 (Brilliant Blue FCF [BB FCF]) is structurally similar to the purinergic receptor antagonist Brilliant Blue G (BBG), which is a well-known inhibitor of the ionotropic P2X7 receptor (P2X7R). The P2X7R functionally interacts with the membrane channel protein pannexin 1 (Panx1) in inflammasome signaling. Intriguingly, ligands to the P2X7R, regardless of whether they are acting as agonists or antagonists at the receptor, inhibit Panx1 channels. Thus, because both P2X7R and Panx1 are inhibited by BBG, the diagnostic value of the drug is limited. Here, weshow that the food dye BB FCF is a selective inhibitor of Panx1 channels, with an IC50 of 0.27 μM.No significant effect was observed with concentrations as high as 100 μM of BB FCF on P2X7R. Differing by just one hydroxyl group from BB FCF, the food dye FD&C Green No. 3 exhibited similar selective inhibition of Panx1 channels. A reverse selectivity was observed for the P2X7R antagonist, oxidized ATP, which in contrast to other P2X7R antagonists had no significant inhibitory effect on Panx1 channels. Based on its selective action, BB FCF can be added to the repertoire of drugs to study the physiology of Panx1 channels. Furthermore, because Panx1 channels appear to be involved directly or indirectly through P2X7Rs in several disorders, BB FCF and derivatives of this "safe" food dye should be given serious consideration for pharmacological intervention of conditions such as acute Crohn's disease, stroke, and injuries to the central nervous system.

AB - The food dye FD&C Blue No. 1 (Brilliant Blue FCF [BB FCF]) is structurally similar to the purinergic receptor antagonist Brilliant Blue G (BBG), which is a well-known inhibitor of the ionotropic P2X7 receptor (P2X7R). The P2X7R functionally interacts with the membrane channel protein pannexin 1 (Panx1) in inflammasome signaling. Intriguingly, ligands to the P2X7R, regardless of whether they are acting as agonists or antagonists at the receptor, inhibit Panx1 channels. Thus, because both P2X7R and Panx1 are inhibited by BBG, the diagnostic value of the drug is limited. Here, weshow that the food dye BB FCF is a selective inhibitor of Panx1 channels, with an IC50 of 0.27 μM.No significant effect was observed with concentrations as high as 100 μM of BB FCF on P2X7R. Differing by just one hydroxyl group from BB FCF, the food dye FD&C Green No. 3 exhibited similar selective inhibition of Panx1 channels. A reverse selectivity was observed for the P2X7R antagonist, oxidized ATP, which in contrast to other P2X7R antagonists had no significant inhibitory effect on Panx1 channels. Based on its selective action, BB FCF can be added to the repertoire of drugs to study the physiology of Panx1 channels. Furthermore, because Panx1 channels appear to be involved directly or indirectly through P2X7Rs in several disorders, BB FCF and derivatives of this "safe" food dye should be given serious consideration for pharmacological intervention of conditions such as acute Crohn's disease, stroke, and injuries to the central nervous system.

UR - http://www.scopus.com/inward/record.url?scp=84878558857&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84878558857&partnerID=8YFLogxK

U2 - 10.1085/jgp.201310966

DO - 10.1085/jgp.201310966

M3 - Article

VL - 141

SP - 649

EP - 656

JO - Journal of General Physiology

JF - Journal of General Physiology

SN - 0022-1295

IS - 5

ER -