Bobrowska-Hägerstrand Malgorzata, Wróbel Anna, Mrówczyńska Lucyna, Söderström Thomas, Hägerstrand Henry
Department of Biology, Abo Akademi University, FIN-20520 Abo/Turku, Finland.
Mol Membr Biol. 2003 Jul-Sep;20(3):255-9. doi: 10.1080/0968768031000106320.
The effect of membrane perturbing agents on the efflux (37 degrees C, 60 min) of the fluorescent probe 2', 7'-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from human erythrocytes was studied. Several anionic amphiphiles (detergents) markedly inhibited BCPCF efflux (IC50 < or = 40 microM). Most zwitter-ionic amphiphiles were inefficient inhibitors. Non-ionic and cationic amphiphiles had minor effects or increased efflux. Of the aliphatic inhibitors, C12-homologues were the most efficient. Hexanol, ethanol, methyl-beta-cyclodextrin (MbetaCD) and diamide (+ washing) did not influence BCPCF efflux. It is suggested that amphiphiles affect BCPCF efflux by modulating multi-drug resistance protein 1 (MRP1, ABCC1) activity. A negative charge of amphiphiles is essential for the inhibitory effect, while alkyl chain length modulates inhibition. MRP1-mediated BCPCF efflux appears to be relatively insensitive to non-specific plasma membrane modification.
研究了膜扰动剂对荧光探针2'，7'-双（羧丙基）-5（6）-羧基荧光素（BCPCF）从人红细胞外流（37℃，60分钟）的影响。几种阴离子两亲物（洗涤剂）显著抑制BCPCF外流（IC50≤40μM）。大多数两性离子两亲物是低效抑制剂。非离子和阳离子两亲物影响较小或增加外流。在脂肪族抑制剂中，C12同系物最有效。己醇、乙醇、甲基-β-环糊精（MβCD）和二酰胺（+洗涤）不影响BCPCF外流。提示两亲物通过调节多药耐药蛋白1（MRP1，ABCC1）活性影响BCPCF外流。两亲物的负电荷对抑制作用至关重要，而烷基链长度调节抑制作用。MRP1介导的BCPCF外流似乎对非特异性质膜修饰相对不敏感。
