Ethanol weakens cytochalasin B binding to the GLUT1 glucose transporter and drug partitioning into lipid bilayers.
Ethanol weakens the specific interaction between the human red blood cell (RBC) glucose transporter GLUT1 and the inhibitor cytochalasin B (CB). The chromatographic retention volume of cytochalasin B on stationary phases consisting of GLUT1-containing membranes decreased with increasing ethanol concentration in the eluent. The apparent Kd values for the ethanol-GLUT1 interaction were 0.37, 0.45 and 0.64 M for red blood cells, red blood cell membrane vesicles and proteoliposomes, respectively, all much higher than the Kd values for D-glucose or cytochalasin B interaction with GLUT1. Ethanol also decreased the partitioning of cytochalasin B and drugs into phospholipid bilayers.
Lagerquist Hägglund
Christine
C
Department of Biochemistry, Biomedical Center, Uppsala University, Box 576, SE-751 23 Uppsala, Sweden. christine.lagerquist@biokem.uu.se
Gottschalk
Ingo
I
Lundahl
Per
P
D002021:Buffers; D002846:Chromatography, Affinity; D003571:Cytochalasin B / Q000378:metabolism*; D004912:Erythrocytes / Q000378:metabolism; D000431:Ethanol / Q000494:pharmacology*; D051272:Glucose Transporter Type 1; D006801:Humans; D066298:In Vitro Techniques; D008051:Lipid Bilayers; D008081:Liposomes; D009004:Monosaccharide Transport Proteins / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D010743:Phospholipids / Q000737:chemistry; D011485:Protein Binding / Q000187:drug effects; D012995:Solubility
D002021:Buffers; D051272:Glucose Transporter Type 1; D008051:Lipid Bilayers; D008081:Liposomes; D009004:Monosaccharide Transport Proteins; D004364:Pharmaceutical Preparations; D010743:Phospholipids; C495677:SLC2A1 protein, human; D003571:Cytochalasin B; D000431:Ethanol