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Clonidine increases membrane-associated phospholipase A2

Published online by Cambridge University Press:  25 November 2005

U. S. R. Helfrich ,
M. Schley ,
G. A. Petroianu ,
J. Schmeck  and
C. Konrad
U. S. R. Helfrich
Affiliation:
University of Heidelberg, Faculty of Clinical Medicine Mannheim, Department of Anaesthesiology and Operative Intensive Care Medicine, Mannheim, Germany
M. Schley
Affiliation:
University of Heidelberg, Faculty of Clinical Medicine Mannheim, Department of Anaesthesiology and Operative Intensive Care Medicine, Mannheim, Germany
G. A. Petroianu
Affiliation:
United Arab Emirates University, Department of Pharmacology, Al Ain, UAE
J. Schmeck
Affiliation:
University of Mainz, Department of Anaesthesiology, Faculty of Clinical Medicine Mannheim, Mainz, Germany
C. Konrad
Affiliation:
University of Heidelberg, Faculty of Clinical Medicine Mannheim, Department of Anaesthesiology and Operative Intensive Care Medicine, Mannheim, Germany
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Extract

Summary

Background and objective: An anti-inflammatory effect of α2-adrenoreceptor agonists has been suggested. Phospholipase A2 is a key enzyme in the production of precursors of inflammatory lipid mediators. The aim of the present study was to investigate the effect of clonidine on phospholipase A2 activity in an established in vitro model. Methods: Human being platelet membranes containing active phospholipase A2 were exposed to buffer control or to three increasing concentrations of clonidine. Phospholipase A2 was measured by a radioisotope technique. Results: A massive increase in phospholipase A2 activity was measured after clonidine exposure leading to final values of 92.5 ± 3.1 pmol mg protein−1 min−1 (4.5-fold higher than control values; P ≤ 0.01 vs. control). After clonidine exposure the maximal reaction velocity increased, while the Michaelis–Menten constant did not change. The Lineweaver–Burk representation suggested an interaction of clonidine with the phospholipase A2–substrate complex as well as the phospholipase A2 molecule. Conclusion: We conclude that the putative anti-inflammatory effect of clonidine was not caused by inhibition of phospholipase A2.

Keywords

PHOSPHOLIPASES A, phospholipase A2CLONIDINEINFLAMMATIONPLATELETS
Type
Original Article
Information
European Journal of Anaesthesiology , Volume 22 , Issue 12 , December 2005 , pp. 942 - 946
Copyright
© 2005 European Society of Anaesthesiology

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