Monitoring of MRP-like activity in human erythrocytes:: Inhibitory effect of isoflavones

被引：36

作者：

Bobrowska-Hagerstrand, M

Wróbel, A

Rychlik, B

Bartosz, G

Söderström, T

Shirataki, Y

Motohashi, N

Molnár, J

Michalak, K

Hägerstrand, H ^{[1
]}

机构：

[1] Abo Akad Univ, Dept Biol, FIN-20520 Turku, Finland

[2] Wroclaw Univ Technol, Inst Phys, PL-50370 Wroclaw, Poland

[3] Univ Lodz, Dept Mol Biophys, PL-90237 Lodz, Poland

[4] Univ Turku, Turku Ctr Biotechnol, FIN-20520 Turku, Finland

[5] Abo Akad Univ, Turku Ctr Biotechnol, FIN-20520 Turku, Finland

[6] Josai Univ, Fac Pharmaceut Sci, Sakado, Saitama 3500295, Japan

[7] Meiji Pharmaceut Univ, Tokyo 2048588, Japan

[8] Albert Szent Gyorgyi Med Univ, Dept Microbiol, H-6720 Szeged, Hungary

[9] Wroclaw Med Univ, PL-50368 Wroclaw, Poland

来源：

BLOOD CELLS MOLECULES AND DISEASES | 2001年 / 27卷 / 05期

关键词：

multidrug resistance; erythrocyte; BCPCF; isoflavonoid; indomethacin; probenecid; DIDS;

D O I：

10.1006/bcmd.2001.0459

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

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 muM. The IC50 value of the most efficient isoflavone, licoisoflavone A (15-25 muM), was comparable to that of indomethacin (similar to 10 muM) and markedly lower than for probenecid (100-200 muM), 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. (C) 2001 Academic Press.

引用

页码：894 / 900

页数：7

共 32 条

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