Monitoring of MRP-like Activity in Human Erythrocytes: Inhibitory Effect of Isoflavones

ABSTRACT A method to fluorometrically monitor efflux of 2′,7′-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from human erythrocytes was developed. Genistein, daidzein, sophoraisoflavone A, and licoisoflavone A induced 50% inhibition (IC50) of BCPCF efflux at 15–70 μM. The IC50 value of the mos...

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Published in:Blood cells, molecules, & diseases molecules, & diseases, 2001-09, Vol.27 (5), p.894-900
Main Authors: Bobrowska-Hägerstrand, Małgorzata, Wróbel, Anna, Rychlik, Błażej, Bartosz, Grzegorz, Söderström, Thomas, Shirataki, Yoshiaki, Motohashi, Noboru, Molnár, Joseph, Michalak, Krystyna, Hägerstrand, Henry
Format: Article
Language:English
Subjects:
4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid - pharmacology
ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
BCPCF
DIDS
Dose-Response Relationship, Drug
erythrocyte
Erythrocytes - metabolism
Fluoresceins - pharmacokinetics
Fluorescent Dyes
Hemolysis - drug effects
Humans
indomethacin
Inhibitory Concentration 50
Isoflavones - pharmacology
Isoflavones - toxicity
isoflavonoid
Kinetics
multidrug resistance
probenecid
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Summary:ABSTRACT A method to fluorometrically monitor efflux of 2′,7′-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from human erythrocytes was developed. Genistein, daidzein, sophoraisoflavone A, and licoisoflavone A induced 50% inhibition (IC50) of BCPCF efflux at 15–70 μM. The IC50 value of the most efficient isoflavone, licoisoflavone A (15–25 μM), was comparable to that of indomethacin (∼10 μM) and markedly lower than for probenecid (100–200 μM), both known MRP1 inhibitors. Our results indicate that the human erythrocyte is a useful cell model in screening potential MRP inhibitors, that BCPCF is a good substrate for MRP, and that some isoflavones at low concentrations inhibit MRP-mediated efflux.
ISSN:1079-9796
1096-0961
DOI:10.1006/bcmd.2001.0459