Suppression of 5-lipoxygenase activity by anionic cholesterol derivatives
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5-Lipoxygenase (5-LO) is a key enzyme involved into biosynthesis of leukotrienes (LTs), mediating the host defense system, and acting simultaneously as inflammatory agents. In this work the effect of anionic cholesterol derivatives on 5-LO activity has been investigated. Cholesterol sulfate activates human polymorphonuclear leukocytes (PMNL) and stimulates their adhesion to endothelium and collagen. Cholesterol sulfate and cholesterol phosphate suppressed leukotriene production in PMNL and in rat basophil leukemia (RBL-1) cell line as well as in homogenates of these cells. Kinetic characteristics of the effect of anionic cholesterol derivatives on leukotriene synthesis have been obtained. In all experiments cholesterol phosphate (charge-2) was shown to be more potent inhibitor than cholesterol sulfate (charge-1). We believe that this fact highlights the importance of negatively charged ester groups for suppression of 5-LO activity.
Key wordsatherosclerosis inflammation neutrophil 5-lipoxygenase cholesterol sulfate cholesterol phosphate
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