[Effect of 3-decyloxycarbonylmethyl-4-methyl-5-(beta-hydroxyethyl)thiazole chloride on nystatin-created K(+)-current across bilayer lipid membrane].
The application of 0.1 mM of vitamin B1 (thiamine) structural analogue, 3-decyloxycarbonylmethyl-4-methyl-5-(beta-hydroxyethyl)thiazole chloride (DMHT) from the cis-side of cholesterol-containing phospholipid bilayer membrane in symmetric solution of 100 mM KCl reversibly reduced the conductance of nystatin channels, reconstituted from the same side of membrane, by 67 +/- 3%. The conductance of nystatin channels applied to the cis-side of bilayer membrane remained unaffected, when DMHT was introduced separately to the opposite trans-side of modified membrane. The kinetics of nystatin channels inhibition with DMHT showed no cooperativity allowing to expect that negatively charged ionogenic groups of these channels formed one DMHT binding site per channel. Relatively high pK of binding with nystatin channels (5,17) suggests that this site provides specific interaction with DMHT.
Shaturs'kyĭ
O Ia
OIa
Romanenko
O V
OV
Himmel'reĭkh
N H
NH
D020134:Catalytic Domain; D007473:Ion Channels / Q000037:antagonists & inhibitors*; D008051:Lipid Bilayers / Q000737:chemistry / Q000378:metabolism*; D008564:Membrane Potentials / Q000187:drug effects; D015394:Molecular Structure; D009761:Nystatin / Q000494:pharmacology*; D010743:Phospholipids / Q000737:chemistry; D011188:Potassium / Q000378:metabolism*; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology; D013831:Thiamine / Q000031:analogs & derivatives / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology*
C548112:3-decyloxycarbonylmethyl-4-methyl-5-(beta-hydroxyethyl)thiazolium chloride; D007473:Ion Channels; D008051:Lipid Bilayers; D010743:Phospholipids; D000644:Quaternary Ammonium Compounds; D013844:Thiazoles; D009761:Nystatin; C027917:tetramethylammonium; D011188:Potassium; D013831:Thiamine