title: Ethanol weakens cytochalasin B binding to the GLUT1 glucose transporter and drug partitioning into lipid bilayers.
abstract: 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.
authors.affiliation: Department of Biochemistry, Biomedical Center, Uppsala University, Box 576, SE-751 23 Uppsala, Sweden. christine.lagerquist@biokem.uu.se
authors.forename: Christine
authors.initials: C
authors.lastname: Lagerquist Hägglund
authors.forename: Ingo
authors.initials: I
authors.lastname: Gottschalk
authors.forename: Per
authors.initials: P
authors.lastname: Lundahl
mesh_terms: 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
chemical_list: 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