Selective inhibition of human acetylcholinesterase by galanthamine in vitro and in vivo.
We investigated the inhibition of human cholinesterases by galanthamine, an alkaloid of the common snowdrop (galanthus nivalis). In vitro, the compound showed potent enzyme inhibition and 50-fold selectivity for acetylcholinesterase (EC 3.1.1.7) as opposed to butyrylcholinesterase (EC 3.1.1.8). There was no difference between enzyme inhibition by galanthamine in whole blood and separated fractions of plasma and erythrocytes. We conclude that galanthamine does not accumulate in large amounts in red blood cells. In vivo, administration of galanthamine in a healthy volunteer and in a patient who underwent long-term treatment confirmed the selectivity of galanthamine for acetylcholinesterase.
Thomsen
T
T
Institute of Clinical Pharmacology, Free University of Berlin, Klinikum Steglitz.
Kewitz
H
H
D000284:Administration, Oral; D000544:Alzheimer Disease / Q000188:drug therapy / Q000201:enzymology; D002091:Butyrylcholinesterase / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000627:therapeutic use; D004912:Erythrocytes / Q000201:enzymology; D005702:Galantamine / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D027801:Galanthus; D006801:Humans; D066298:In Vitro Techniques
D002800:Cholinesterase Inhibitors; D005702:Galantamine; D002091:Butyrylcholinesterase