Inhibition of cytochrome P450c11 by biogenic amines and an aziridine precursor, 2-(4-acetoxyphenyl_-2-chloro-n-methyl-ethylammonium chloride
Date
2000
Authors
Louw, Ann
Allie, F.
Swart, A. C.
Swart, P.
Journal Title
Journal ISSN
Volume Title
Publisher
Informa Healthcare
Abstract
The interaction of several biogenic amines and Compound A (2-(4-acetoxyphenyl)-2-chloro- N-methyl-ethylammonium chloride), an analogue of the active substance in a HPLC fraction isolated from the shrub, Salsola tuberculatiformis Botsch., with cytochrome P450c11 was investigated. Noradrenaline, octopamine and Compound A inhibited the type I DOC induced difference spectrum of P450c11 and elicited a type II difference spectrum when added alone. The Ks-values for noradrenaline, octopamine, and Compound A were 0.8 mM, 0.16 mM and 0.36 mM, respectively. Dopamine, adrenaline and synephrine did not interact with, or inhibit, P450c11. Further investigation of Compound A indicated that it is a mixed inhibitor of sheep P450c11 with a stronger competitive (Kic = 106-110 µM) than uncompetitive (Kiu = 667-737 µM) element.
Description
The original publication is available at http://informahealthcare.com
Keywords
Biogenic amine interaction, Compound A, Cytochrome P-450
Citation
Louw, A., Allie, F., Swart, A. C. & Swart, P 2000. Inhibition of cytochrome P450c11 by biogenic amines and an aziridine precursor, 2-(4-acetoxyphenyl_-2-chloro-n-methyl-ethylammonium chloride. Endocrine Research, 26(4), 729-736.