Membrane-bound acetylcholinesterase (AChE) from the human erythrocyte is inhibited by chlorpromazine (CPZ) in a concentration range within this amphiphilic drug has been demonstrated to interact with erythrocyte membranes, causing a large spectrum of physical and structural effects; membrane solubilization with 0.5% Triton X-100 results in a complete loss of CPZ inhibitory potency. Although these observations might suggest a role of membrane lipid environment in mediating human erythrocyte AChE inhibition, we observed that CPZ retains its full inhibitory effect on the fraction of enzyme (5-6% of total) that is solubilized from erythrocytes upon treatment with phosphatidylinositol-specific phospholipase C (PI-PLC) from Bacillus thuringiensis; furthermore, Triton X-100 is able to reverse the CPZ effect also in the case of PI-PLC-solubilized enzyme. These results demonstrate unequivocally that CPZ inhibits human erythrocyte AChE through direct molecular interaction. The inhibition kinetics displayed by CPZ on human erythrocyte AChE are dependent on drug concentration: evidence is provided that this phenomenon may be related to formation of CPZ micellar aggregates.
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September 1991
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Research Article|
September 01 1991
A study of human erythrocyte acetylcholinesterase inhibition by chlorpromazine
A Spinedi;
A Spinedi
*Department of Biology, University of Rome ‘Tor Vergata’, 00173 Rome, Italy.
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L Pacini;
L Pacini
*Department of Biology, University of Rome ‘Tor Vergata’, 00173 Rome, Italy.
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C Limatola;
C Limatola
*Department of Biology, University of Rome ‘Tor Vergata’, 00173 Rome, Italy.
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P Luly;
P Luly
*Department of Biology, University of Rome ‘Tor Vergata’, 00173 Rome, Italy.
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R N Farias
R N Farias
†Instituto de Quimica Biologica, Facultad de Bioquimica, Quimica y Farmacia, Universidad Nacional de Tucuman, Chacabuco 461, 4000 San Miguel de Tucuman, Argentina.
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Publisher: Portland Press Ltd
Online ISSN: 1470-8728
Print ISSN: 0264-6021
© 1991 The Biochemical Society, London
1991
Biochem J (1991) 278 (2): 461–463.
Citation
A Spinedi, L Pacini, C Limatola, P Luly, R N Farias; A study of human erythrocyte acetylcholinesterase inhibition by chlorpromazine. Biochem J 1 September 1991; 278 (2): 461–463. doi: https://doi.org/10.1042/bj2780461
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